Details of the Drug

General Information of Drug (ID: DMS8IFC)

Drug Name
Sorafenib
Synonyms
Nexavar; Sorafenibum; Sorafenib [INN]; Nexavar (TN); Sorafenib (INN); N-[4-Chloro-3-(trifluoromethyl)phenyl]-N'-[4-[2-(N-methylcarbamoyl)-4-pyridyloxy]phenyl]urea; N-(4-Chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea; N-(4-chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcar bamoyl)-4-pyridyloxy)phenyl)urea; 4(4-{3-[4-Chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N(sup 2)-methylpyridine-2-carboxamide; 4-(4-((((4-Chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl-2-pyridinecarboxamide; 4-(4-(3-(4-chloro-3-trifluoromethylphenyl)ureido)phenoxy)pyridine-2-carboxyllic acid methyamide-4-methylbenzenesulfonate; 4-(4-{3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido}phenoxy)-N(sup 2)-methylpyridine-2-carboxamide; 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide; 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide; 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide; 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide; 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE; Sorafenib (Pan-TK inhibitor)
Indication
Disease Entry ICD 11 Status REF
Hepatocellular carcinoma 2C12.02 Approved [1], [2]
Renal cell carcinoma 2C90 Approved [1], [3]
Myelodysplastic syndrome 2A37 Phase 2 [1], [2]
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 464.8
Topological Polar Surface Area (xlogp) 4.1
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Elimination
0% of drug is excreted from urine in the unchanged form [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 25 - 48 hours [5]
Metabolism
The drug is metabolized via the liver [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 12.29315 micromolar/kg/day [7]
Chemical Identifiers
Formula
C21H16ClF3N4O3
IUPAC Name
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
Canonical SMILES
CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
InChI
InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
InChIKey
MLDQJTXFUGDVEO-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
216239
ChEBI ID
CHEBI:50924
CAS Number
284461-73-0
DrugBank ID
DB00398
TTD ID
D0W5HK
VARIDT ID
DR00304
INTEDE ID
DR1500
ACDINA ID
D00635

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [8]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Modulator [9], [3]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Modulator [9], [3]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [9], [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
RalBP1-associated Eps domain-containing protein 2 (RALBP1) DTYEM9B REPS2_HUMAN Substrate [10]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [11]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [12]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [13]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [14]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [14]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [15]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [16]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [17]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [18]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [16]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [18]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Substrate [19]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Hepatocellular carcinoma
ICD Disease Classification 2C12.02
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Tyrosine-protein kinase Kit (KIT) DTT KIT 2.06E-01 -0.1 -0.14
Vascular endothelial growth factor receptor 2 (KDR) DTT KDR 1.98E-01 0.11 0.2
Platelet-derived growth factor receptor beta (PDGFRB) DTT PDGFRB 5.35E-10 0.36 0.89
P-glycoprotein 1 (ABCB1) DTP P-GP 9.39E-02 1.07E-01 2.80E-01
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 8.54E-01 1.24E-02 7.20E-02
Breast cancer resistance protein (ABCG2) DTP BCRP 9.45E-01 -5.34E-02 -9.01E-02
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.16E-01 -1.28E-02 -6.06E-02
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 9.69E-01 1.16E-03 3.56E-03
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 8.15E-01 6.20E-03 5.61E-02
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.82E-04 -1.35E-01 -5.84E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.36E-01 1.62E-02 1.08E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.96E-01 -3.17E-03 -1.84E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Sorafenib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [143]
Metreleptin DM1NOEK Moderate Increased metabolism of Sorafenib caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [144]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Sorafenib and Ivosidenib. Acute myeloid leukaemia [2A60] [145]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Midostaurin. Acute myeloid leukaemia [2A60] [146]
Idarubicin DMM0XGL Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Idarubicin. Acute myeloid leukaemia [2A60] [147]
Daunorubicin DMQUSBT Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Daunorubicin. Acute myeloid leukaemia [2A60] [147]
Arn-509 DMT81LZ Moderate Increased metabolism of Sorafenib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [144]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Gilteritinib. Acute myeloid leukaemia [2A60] [148]
Mitotane DMU1GX0 Moderate Increased metabolism of Sorafenib caused by Mitotane mediated induction of CYP450 enzyme. Adrenal cancer [2D11] [144]
Framycetin DMF8DNE Moderate Altered absorption of Sorafenib due to GI flora changes caused by Framycetin. Alcoholic liver disease [DB94] [143]
Galantamine DMEO794 Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Galantamine. Alzheimer disease [8A20] [146]
Rivastigmine DMG629M Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Rivastigmine. Alzheimer disease [8A20] [146]
Donepezil DMIYG7Z Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Donepezil. Alzheimer disease [8A20] [146]
Metronidazole DMTIVEN Minor Increased risk of prolong QT interval by the combination of Sorafenib and Metronidazole. Amoebiasis [1A36] [143]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Sorafenib and Ivabradine. Angina pectoris [BA40] [149]
Bepridil DM0RKS4 Major Increased risk of prolong QT interval by the combination of Sorafenib and Bepridil. Angina pectoris [BA40] [146]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Sorafenib and Dronedarone. Angina pectoris [BA40] [146]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Sorafenib and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [150]
Methylphenobarbital DMDSWAG Moderate Increased metabolism of Sorafenib caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [151]
Hydroxyzine DMF8Y74 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Hydroxyzine. Anxiety disorder [6B00-6B0Z] [146]
Promazine DMZAL7W Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Promazine. Appearance/behaviour symptom [MB23] [146]
Cilostazol DMZMSCT Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Cilostazol. Arterial occlusive disease [BD40] [146]
Voriconazole DMAOL2S Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Voriconazole. Aspergillosis [1F20] [146]
Posaconazole DMUL5EW Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Posaconazole. Aspergillosis [1F20] [146]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Levalbuterol. Asthma [CA23] [152]
Terbutaline DMD4381 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Terbutaline. Asthma [CA23] [153]
Pirbuterol DMI5678 Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Pirbuterol. Asthma [CA23] [153]
Salbutamol DMN9CWF Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Salbutamol. Asthma [CA23] [152]
Formoterol DMSOURV Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Formoterol. Asthma [CA23] [153]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [149]
Ofloxacin DM0VQN3 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Ofloxacin. Bacterial infection [1A00-1C4Z] [146]
Oritavancin DM28D05 Moderate Increased metabolism of Sorafenib caused by Oritavancin mediated induction of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [144]
Ciprofloxacin XR DM2NLS9 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Ciprofloxacin XR. Bacterial infection [1A00-1C4Z] [146]
Clarithromycin DM4M1SG Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Clarithromycin. Bacterial infection [1A00-1C4Z] [146]
Sulfamethoxazole DMB08GE Minor Increased risk of prolong QT interval by the combination of Sorafenib and Sulfamethoxazole. Bacterial infection [1A00-1C4Z] [146]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Sorafenib and Sparfloxacin. Bacterial infection [1A00-1C4Z] [154]
Gemifloxacin DMHT34O Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Gemifloxacin. Bacterial infection [1A00-1C4Z] [146]
Norfloxacin DMIZ6W2 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Norfloxacin. Bacterial infection [1A00-1C4Z] [146]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Levofloxacin. Bacterial infection [1A00-1C4Z] [146]
Lomefloxacin DMVRH9C Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Lomefloxacin. Bacterial infection [1A00-1C4Z] [146]
Telithromycin DMZ4P3A Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Telithromycin. Bacterial infection [1A00-1C4Z] [146]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Retigabine. Behcet disease [4A62] [146]
Pexidartinib DMS2J0Z Major Decreased metabolism of Sorafenib caused by Pexidartinib mediated inhibition of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [155]
Loperamide DMOJZQ9 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Loperamide. Bowel habit change [ME05] [156]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Eribulin. Breast cancer [2C60-2C6Y] [146]
Talazoparib DM1KS78 Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [157]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Lapatinib. Breast cancer [2C60-2C6Y] [146]
Tucatinib DMBESUA Moderate Decreased metabolism of Sorafenib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [158]
Tamoxifen DMLB0EZ Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Tamoxifen. Breast cancer [2C60-2C6Y] [146]
Toremifene DMQYUWG Major Increased risk of prolong QT interval by the combination of Sorafenib and Toremifene. Breast cancer [2C60-2C6Y] [146]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Bosutinib. Breast cancer [2C60-2C6Y] [146]
Sotalol DML60TN Major Increased risk of prolong QT interval by the combination of Sorafenib and Sotalol. Cardiac arrhythmia [BC9Z] [146]
Secobarbital DM14RF5 Moderate Increased metabolism of Sorafenib caused by Secobarbital mediated induction of CYP450 enzyme. Chronic insomnia [7A00] [144]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [159]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Olodaterol. Chronic obstructive pulmonary disease [CA22] [153]
Salmeterol DMIEU69 Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Salmeterol. Chronic obstructive pulmonary disease [CA22] [153]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Indacaterol. Chronic obstructive pulmonary disease [CA22] [153]
Arformoterol DMYM974 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Arformoterol. Chronic obstructive pulmonary disease [CA22] [153]
Fidaxomicin DMFP6MV Minor Decreased clearance of Sorafenib due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [143]
Anisindione DM2C48U Moderate Increased risk of bleeding by the combination of Sorafenib and Anisindione. Coagulation defect [3B10] [160]
Irinotecan DMP6SC2 Moderate Decreased metabolism of Sorafenib caused by Irinotecan mediated inhibition of UGT. Colorectal cancer [2B91] [144]
Oxaliplatin DMQNWRD Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Oxaliplatin. Colorectal cancer [2B91] [146]
Isoproterenol DMK7MEY Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Isoproterenol. Conduction disorder [BC63] [152]
Halothane DM80OZ5 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Halothane. Corneal disease [9A76-9A78] [146]
Propofol DMB4OLE Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Propofol. Corneal disease [9A76-9A78] [161]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Sevoflurane. Corneal disease [9A76-9A78] [146]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Probucol. Coronary atherosclerosis [BA80] [146]
Clofazimine DMEBOFW Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Clofazimine. Crohn disease [DD70] [162]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Sorafenib and Pasireotide. Cushing syndrome [5A70] [146]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Osilodrostat. Cushing syndrome [5A70] [146]
Lumacaftor DMCLWDJ Moderate Increased metabolism of Sorafenib caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [163]
Sertraline DM0FB1J Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Sertraline. Depression [6A70-6A7Z] [146]
Trimipramine DM1SC8M Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Trimipramine. Depression [6A70-6A7Z] [146]
Imipramine DM2NUH3 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Imipramine. Depression [6A70-6A7Z] [146]
Fluoxetine DM3PD2C Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Fluoxetine. Depression [6A70-6A7Z] [146]
Nortriptyline DM4KDYJ Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Nortriptyline. Depression [6A70-6A7Z] [146]
Clomipramine DMINRKW Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Clomipramine. Depression [6A70-6A7Z] [146]
Amoxapine DMKITQE Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Amoxapine. Depression [6A70-6A7Z] [146]
Doxepin DMPI98T Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Doxepin. Depression [6A70-6A7Z] [146]
Maprotiline DMPWB7T Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Maprotiline. Depression [6A70-6A7Z] [146]
Griseofulvin DMK54YG Moderate Increased metabolism of Sorafenib caused by Griseofulvin mediated induction of CYP450 enzyme. Dermatophytosis [1F28] [144]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [146]
Deutetrabenazine DMUPFLI Moderate Additive CNS depression effects by the combination of Sorafenib and Deutetrabenazine. Dystonic disorder [8A02] [164]
Ingrezza DMVPLNC Moderate Additive CNS depression effects by the combination of Sorafenib and Ingrezza. Dystonic disorder [8A02] [165]
Primidone DM0WX6I Moderate Increased metabolism of Sorafenib caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Felbamate DM1V5ZS Moderate Increased metabolism of Sorafenib caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Sorafenib caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Cenobamate DMGOVHA Moderate Increased metabolism of Sorafenib caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Sorafenib caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Rufinamide DMWE60C Moderate Increased metabolism of Sorafenib caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Phenobarbital DMXZOCG Moderate Increased metabolism of Sorafenib caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Carbamazepine DMZOLBI Moderate Increased metabolism of Sorafenib caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Sorafenib caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [144]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Cannabidiol. Epileptic encephalopathy [8A62] [149]
Tazemetostat DMWP1BH Moderate Increased metabolism of Sorafenib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [144]
Pentamidine DMHZJCG Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Pentamidine. Fungal infection [1F29-1F2F] [146]
Ketoconazole DMPZI3Q Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Ketoconazole. Fungal infection [1F29-1F2F] [146]
Cisapride DMY7PED Major Increased risk of prolong QT interval by the combination of Sorafenib and Cisapride. Gastro-oesophageal reflux disease [DA22] [146]
Ripretinib DM958QB Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Ripretinib. Gastrointestinal stromal tumour [2B5B] [143]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Sunitinib. Gastrointestinal stromal tumour [2B5B] [146]
Sulfinpyrazone DMEV954 Moderate Increased metabolism of Sorafenib caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [144]
Rifampin DMA8J1G Moderate Increased metabolism of Sorafenib caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [163]
Brentuximab vedotin DMWLC57 Moderate Decreased metabolism of Sorafenib caused by Brentuximab vedotin mediated inhibition of CYP450 enzyme. Hodgkin lymphoma [2B30] [166]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [146]
Efavirenz DMC0GSJ Major Increased risk of prolong QT interval by the combination of Sorafenib and Efavirenz. Human immunodeficiency virus disease [1C60-1C62] [167]
Dolutegravir DMCZGRE Minor Decreased metabolism of Sorafenib caused by Dolutegravir mediated inhibition of UGT. Human immunodeficiency virus disease [1C60-1C62] [168]
Saquinavir DMG814N Major Increased risk of prolong QT interval by the combination of Sorafenib and Saquinavir. Human immunodeficiency virus disease [1C60-1C62] [169]
Etravirine DMGV8QU Moderate Increased metabolism of Sorafenib caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [144]
Lopinavir DMITQS0 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Lopinavir. Human immunodeficiency virus disease [1C60-1C62] [146]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [146]
Maraviroc DMTL94F Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Maraviroc. Human immunodeficiency virus disease [1C60-1C62] [170]
Raltegravir DMYURI6 Minor Decreased metabolism of Sorafenib caused by Raltegravir mediated inhibition of UGT. Human immunodeficiency virus disease [1C60-1C62] [171]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Sorafenib and Mipomersen. Hyper-lipoproteinaemia [5C80] [172]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Sorafenib and Teriflunomide. Hyper-lipoproteinaemia [5C80] [146]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Sorafenib and BMS-201038. Hyper-lipoproteinaemia [5C80] [173]
Aliskiren DM1BV7W Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [146]
Tolvaptan DMIWFRL Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [174]
Lesinurad DMUR64T Moderate Increased metabolism of Sorafenib caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [144]
Berotralstat DMWA2DZ Major Decreased clearance of Sorafenib due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [175]
Amobarbital DM0GQ8N Moderate Increased metabolism of Sorafenib caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [144]
ITI-007 DMUQ1DO Moderate Decreased metabolism of Sorafenib caused by ITI-007 mediated inhibition of UGT. Insomnia [7A00-7A0Z] [176]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Polyethylene glycol. Irritable bowel syndrome [DD91] [149]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Phenolphthalein. Irritable bowel syndrome [DD91] [146]
Naloxegol DML0B41 Minor Decreased metabolism of Sorafenib caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [177]
Methotrexate DM2TEOL Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Methotrexate. Leukaemia [2A60-2B33] [149]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Sorafenib and Crizotinib. Lung cancer [2C25] [178]
Brigatinib DM7W94S Moderate Increased metabolism of Sorafenib caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [144]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Sorafenib and Ceritinib. Lung cancer [2C25] [146]
PF-06463922 DMKM7EW Moderate Increased metabolism of Sorafenib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [144]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Sorafenib and Osimertinib. Lung cancer [2C25] [179]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Sorafenib and Selpercatinib. Lung cancer [2C25] [149]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Sorafenib and Lumefantrine. Malaria [1F40-1F45] [143]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Sorafenib and Halofantrine. Malaria [1F40-1F45] [180]
Chloroquine DMSI5CB Major Increased risk of prolong QT interval by the combination of Sorafenib and Chloroquine. Malaria [1F40-1F45] [181]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Sorafenib and Hydroxychloroquine. Malaria [1F40-1F45] [181]
Quinine DMSWYF5 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Quinine. Malaria [1F40-1F45] [146]
Primaquine DMWQ16I Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Primaquine. Malaria [1F40-1F45] [146]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [149]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [182]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Idelalisib. Mature B-cell leukaemia [2A82] [183]
GDC-0199 DMH0QKA Major Decreased clearance of Sorafenib due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [143]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Clofarabine. Mature B-cell lymphoma [2A85] [184]
Arry-162 DM1P6FR Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Arry-162. Melanoma [2C30] [143]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Sorafenib and Vemurafenib. Melanoma [2C30] [146]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and LGX818. Melanoma [2C30] [146]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Sorafenib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [149]
Exjade DMHPRWG Moderate Increased metabolism of Sorafenib caused by Exjade mediated induction of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [144]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Sorafenib and Panobinostat. Multiple myeloma [2A83] [185]
Thalidomide DM70BU5 Moderate Increased risk of peripheral neuropathy by the combination of Sorafenib and Thalidomide. Multiple myeloma [2A83] [143]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Sorafenib and Siponimod. Multiple sclerosis [8A40] [143]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Sorafenib and Fingolimod. Multiple sclerosis [8A40] [146]
Rifabutin DM1YBHK Moderate Increased metabolism of Sorafenib caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [144]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Romidepsin. Mycosis fungoides [2B01] [146]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Sorafenib and Nilotinib. Myeloproliferative neoplasm [2A20] [146]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Dasatinib. Myeloproliferative neoplasm [2A20] [146]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive myelosuppressive effects by the combination of Sorafenib and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [186]
Modafinil DMYILBE Moderate Increased metabolism of Sorafenib caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [144]
Prochlorperazine DM53SRA Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Prochlorperazine. Nausea/vomiting [MD90] [146]
Dolasetron DMMG26Z Major Increased risk of prolong QT interval by the combination of Sorafenib and Dolasetron. Nausea/vomiting [MD90] [146]
Ondansetron DMOTQ1I Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Ondansetron. Nausea/vomiting [MD90] [146]
Levomethadyl Acetate DM06HG5 Major Increased risk of prolong QT interval by the combination of Sorafenib and Levomethadyl Acetate. Opioid use disorder [6C43] [149]
Lofexidine DM1WXA6 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Lofexidine. Opioid use disorder [6C43] [146]
Olaparib DM8QB1D Moderate Increased metabolism of Sorafenib caused by Olaparib mediated induction of CYP450 enzyme. Ovarian cancer [2C73] [143]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Rucaparib. Ovarian cancer [2C73] [146]
Dextropropoxyphene DM23HCX Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Dextropropoxyphene. Pain [MG30-MG3Z] [146]
Buprenorphine DMPRI8G Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Buprenorphine. Pain [MG30-MG3Z] [146]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Triclabendazole. Parasitic worm infestation [1F90] [146]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Pimavanserin. Parkinsonism [8A00] [187]
Famotidine DMRL3AB Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Famotidine. Peptic ulcer [DA61] [143]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Sorafenib and Macimorelin. Pituitary gland disorder [5A60-5A61] [188]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Sorafenib and Lefamulin. Pneumonia [CA40] [189]
Ritodrine DM4V6RL Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Ritodrine. Preterm labour/delivery [JB00] [153]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Degarelix. Prostate cancer [2C82] [149]
Nilutamide DMFN07X Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Nilutamide. Prostate cancer [2C82] [149]
Enzalutamide DMGL19D Moderate Increased metabolism of Sorafenib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [144]
Flutamide DMK0O7U Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Flutamide. Prostate cancer [2C82] [149]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Relugolix. Prostate cancer [2C82] [149]
Bicalutamide DMZMSPF Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Bicalutamide. Prostate cancer [2C82] [149]
Levomepromazine DMIKFEL Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Levomepromazine. Psychotic disorder [6A20-6A25] [146]
Fluphenazine DMIT8LX Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Fluphenazine. Psychotic disorder [6A20-6A25] [146]
Triflupromazine DMKFQJP Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Triflupromazine. Psychotic disorder [6A20-6A25] [146]
Bosentan DMIOGBU Moderate Increased metabolism of Sorafenib caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [144]
Gatifloxacin DMSL679 Major Increased risk of prolong QT interval by the combination of Sorafenib and Gatifloxacin. Respiratory infection [CA07-CA4Z] [190]
Dexamethasone DMMWZET Moderate Increased metabolism of Sorafenib caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [144]
Nafcillin DMN9RPO Moderate Increased metabolism of Sorafenib caused by Nafcillin mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [144]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Sorafenib and Leflunomide. Rheumatoid arthritis [FA20] [146]
Quetiapine DM1N62C Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Quetiapine. Schizophrenia [6A20] [146]
Mesoridazine DM2ZGAN Major Increased risk of prolong QT interval by the combination of Sorafenib and Mesoridazine. Schizophrenia [6A20] [146]
Thioridazine DM35M8J Major Increased risk of prolong QT interval by the combination of Sorafenib and Thioridazine. Schizophrenia [6A20] [146]
Aripiprazole DM3NUMH Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Aripiprazole. Schizophrenia [6A20] [143]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Sorafenib and Iloperidone. Schizophrenia [6A20] [146]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Paliperidone. Schizophrenia [6A20] [146]
Haloperidol DM96SE0 Major Increased risk of prolong QT interval by the combination of Sorafenib and Haloperidol. Schizophrenia [6A20] [146]
Perphenazine DMA4MRX Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Perphenazine. Schizophrenia [6A20] [146]
Chlorpromazine DMBGZI3 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Chlorpromazine. Schizophrenia [6A20] [146]
Trifluoperazine DMKBYWI Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Trifluoperazine. Schizophrenia [6A20] [146]
Risperidone DMN6DXL Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Risperidone. Schizophrenia [6A20] [146]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Sorafenib and Amisulpride. Schizophrenia [6A20] [191]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Asenapine. Schizophrenia [6A20] [146]
Pimozide DMW83TP Major Increased risk of prolong QT interval by the combination of Sorafenib and Pimozide. Schizophrenia [6A20] [149]
Vardenafil DMTBGW8 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Vardenafil. Sexual dysfunction [HA00-HA01] [146]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Sorafenib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [151]
PDX-101 DM6OC53 Moderate Decreased metabolism of Sorafenib caused by PDX-101 mediated inhibition of UGT. Solid tumour/cancer [2A00-2F9Z] [192]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [149]
Armodafinil DMGB035 Moderate Increased metabolism of Sorafenib caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [144]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Sorafenib and LEE011. Solid tumour/cancer [2A00-2F9Z] [146]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [149]
Taxol DMUOT9V Moderate Decreased metabolism of Sorafenib caused by Taxol mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [149]
Doxorubicin DMVP5YE Moderate Decreased clearance of Sorafenib due to the transporter inhibition by Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [149]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [146]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Sorafenib and Naltrexone. Substance abuse [6C40] [193]
Warfarin DMJYCVW Moderate Increased risk of bleeding by the combination of Sorafenib and Warfarin. Supraventricular tachyarrhythmia [BC81] [160]
Adenosine DMM2NSK Moderate Increased risk of ventricular arrhythmias by the combination of Sorafenib and Adenosine. Supraventricular tachyarrhythmia [BC81] [146]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Sorafenib caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [194]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Lenvatinib. Thyroid cancer [2D10] [146]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Sorafenib and Cabozantinib. Thyroid cancer [2D10] [149]
Papaverine DMCA9QP Major Increased risk of prolong QT interval by the combination of Sorafenib and Papaverine. Tonus and reflex abnormality [MB47] [195]
Tacrolimus DMZ7XNQ Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Tacrolimus. Transplant rejection [NE84] [146]
Dapagliflozin DM28UJG Minor Decreased metabolism of Sorafenib caused by Dapagliflozin mediated inhibition of UGT. Type 2 diabetes mellitus [5A11] [196]
Elagolix DMB2C0E Moderate Increased metabolism of Sorafenib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [144]
Astemizole DM2HN6Q Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Astemizole. Vasomotor/allergic rhinitis [CA08] [146]
Trimeprazine DMEMV9D Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [146]
Procainamide DMNMXR8 Major Increased risk of prolong QT interval by the combination of Sorafenib and Procainamide. Ventricular tachyarrhythmia [BC71] [146]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Propafenone. Ventricular tachyarrhythmia [BC71] [146]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Sorafenib and Flecainide. Ventricular tachyarrhythmia [BC71] [146]
Amiodarone DMUTEX3 Major Increased risk of prolong QT interval by the combination of Sorafenib and Amiodarone. Ventricular tachyarrhythmia [BC71] [146]
⏷ Show the Full List of 226 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carmellose sodium E00625 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Magnesium stearate E00208 11177 lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Sorafenib 200 mg tablet 200 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5711).
2 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
3 Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612.
4 BDDCS applied to over 900 drugs
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
7 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
9 Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
10 Rlip76 transports sunitinib and sorafenib and mediates drug resistance in kidney cancer. Int J Cancer. 2010 Mar 15;126(6):1327-38.
11 Multidrug resistance protein 2 implicates anticancer drug-resistance to sorafenib. Biol Pharm Bull. 2011;34(3):433-5.
12 Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma
13 Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier. Mol Pharm. 2011 Apr 4;8(2):571-82.
14 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
15 Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation. Mol Cancer Ther. 2010 Feb;9(2):319-26.
16 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
17 Ontogeny and sorafenib metabolism. Clin Cancer Res. 2012 Oct 15;18(20):5788-95.
18 Drug Interactions Flockhart Table
19 Pharmacokinetic interaction involving sorafenib and the calcium-channel blocker felodipine in a patient with hepatocellular carcinoma. Invest New Drugs. 2011 Dec;29(6):1511-4.
20 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
21 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
22 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
23 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
24 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
25 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
26 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
27 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
28 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
29 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
30 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
31 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
32 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
33 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
34 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
35 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
36 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
37 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
38 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
39 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
40 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
41 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
42 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
43 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
44 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
45 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
46 16Alpha-hydroxylation of estrone by human cytochrome P4503A4/5. Carcinogenesis. 1998 May;19(5):867-72.
47 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
48 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
49 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
50 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
51 Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers.
52 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
53 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
54 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
55 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
56 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
57 Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87.
58 Polymorphic expression of UGT1A9 is associated with variable acetaminophen glucuronidation in neonates: a population pharmacokinetic and pharmacogenetic study. Clin Pharmacokinet. 2018 Oct;57(10):1325-1336.
59 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
60 The evolution of population pharmacokinetic models to describe the enterohepatic recycling of mycophenolic acid in solid organ transplantation and autoimmune disease. Clin Pharmacokinet. 2011 Jan;50(1):1-24.
61 The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003 Apr 18;278(16):13975-83.
62 S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
63 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
64 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
65 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
66 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
67 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
68 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
69 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
70 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
71 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
72 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
73 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
74 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
75 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
76 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
77 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
78 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
79 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
80 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
81 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
82 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
83 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
84 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
85 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
86 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
87 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
88 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
89 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
90 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
91 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
92 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
93 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
94 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
95 FDA Drug Development and Drug Interactions
96 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
97 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
98 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
99 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
100 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
101 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
102 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
103 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
104 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
105 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
106 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
107 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
108 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
109 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
110 Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46.
111 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
112 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
113 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
114 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
115 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
116 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
117 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
118 National Cancer Institute Drug Dictionary (drug id 452042).
119 Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
120 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
121 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
122 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
123 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
124 Company report (Neuronova)
125 Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
126 RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
127 Bcr-Abl tyrosine kinase inhibitors: a patent review.Expert Opin Ther Pat. 2015 Apr;25(4):397-412.
128 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
129 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
130 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
131 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
132 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
133 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
134 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
135 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
136 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
137 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
138 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
139 Clinical pipeline report, company report or official report of Exelixis (2011).
140 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
141 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
142 YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.
143 Cerner Multum, Inc. "Australian Product Information.".
144 Product Information. Nexavar (sorafenib). Bayer Pharmaceutical Inc, West Haven, CT.
145 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
146 Canadian Pharmacists Association.
147 Multum Information Services, Inc. Expert Review Panel.
148 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
149 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
150 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
151 Product Information. Diabinese (chlorpropamide). Pfizer US Pharmaceuticals, New York, NY.
152 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
153 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
154 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
155 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
156 Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747]
157 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
158 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
159 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
160 Laber DA, Mushtaq M "Compassionate use of sorafenib in patients with advanced renal cell cancer." Clin Genitourin Cancer 7 (2009): 34-8. [PMID: 19213666]
161 Hanci V, Aydin M, Yurtlu BS, et.al "Anesthesia induction with sevoflurane and propofol: evaluation of P-wave dispersion, QT and corrected QT intervals." Kaohsiung J Med Sci 26 (2010): 470-7. [PMID: 20837343]
162 Product Information. Lamprene (clofazimine). Novartis Pharmaceuticals, East Hanover, NJ.
163 Patel S, Robinson R, Burk M "Hypertensive crisis associated with St. John's Wort." Am J Med 112 (2002): 507-8. [PMID: 11959071]
164 Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
165 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
166 Product Information. VFEND (voriconazole). Pfizer U.S. Pharmaceuticals, New York, NY.
167 Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE.
168 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
169 Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475]
170 Product Information. Selzentry (maraviroc). Pfizer U.S. Pharmaceuticals Group, New York, NY.
171 Product Information. Isentress (raltegravir). Merck & Company Inc, West Point, PA.
172 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
173 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
174 Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
175 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
176 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
177 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
178 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
179 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
180 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
181 Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
182 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
183 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
184 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
185 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
186 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
187 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
188 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
189 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
190 Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]
191 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
192 Product Information. Beleodaq (belinostat). Spectrum Pharmaceuticals Inc, Irvine, CA.
193 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
194 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
195 Goto M, Sato M, Kitzazawa H, et.al "Papaverine-induced QT interval prolongation and ventricular fibrillation in a patient with a history of drug-induced QT prolongation." Intern Med 53 (2014): 1629-31. [PMID: 25088875]
196 Product Information. Farxiga (dapagliflozin). Bristol-Myers Squibb, Princeton, NJ.