General Information of Drug (ID: DMG814N)

Drug Name
Saquinavir
Synonyms
Fortovase; Invirase; ROC; SQV; Saguinavir; Ro 318959; Fortovase (TN); Fortovase(TM); Invirase (TN); Ro 31-8959; Invirase(TM)(monomesylate); Ro-31-8959; Saquinavir (JAN/USP/INN); QNC-ASN-HPH-DIQ-NTB; CIS-N-TERT-BUTYL-DECAHYDRO-2-[2(R)-HYDROXY-4-PHENYL-3(S)-[[N-2-QUINOLYLCARBONYL-L-ASPARAGINYL]AMINO]BUTYL]-(4AS)-ISOQUINOLINE-3(S)-CARBOXAMIDE; (2S)-N-[(2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinoline-2-carbonylamino)butanediamide; (2s)-N-[(2s,3r)-4-[(2s,3s,4as,8as)-3-(Tert-Butylcarbamoyl)-3,4,4a,5,6,7,8,8a-Octahydro-1h-Isoquinolin-2-Yl]-3-Hydroxy-1-Phenyl-Butan-2-Yl]-2-(Quinolin-2-Ylcarbonylamino)butanediamide
Indication
Disease Entry ICD 11 Status REF
Human immunodeficiency virus infection 1C62 Approved [1], [2]
Therapeutic Class
Anti-HIV Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 2 Molecular Weight (mw) 670.8
Topological Polar Surface Area (xlogp) 4.2
Rotatable Bond Count (rotbonds) 13
Hydrogen Bond Donor Count (hbonddonor) 5
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 39026 mcgh/L [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Bioavailability
The bioavailability of drug is 4% [3]
Clearance
The sytemic clearance of drug is 1.14 L/h/kg [3]
Elimination
Following the administration of radiolabeled saquinavir (both orally and intravenously), approximately 81-88% of radioactivity is recovered in the feces within 5 days of dosing while only 1-3% is recovered in the urine [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 13 hours [5]
Metabolism
The drug is metabolized via the liver [3]
Unbound Fraction
The unbound fraction of drug in plasma is 0.028% [5]
Vd
The volume of distribution (Vd) of drug is 700 L [3]
Water Solubility
The ability of drug to dissolve in water is measured as 0.08 mg/mL [4]
Chemical Identifiers
Formula
C38H50N6O5
IUPAC Name
(2S)-N-[(2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinoline-2-carbonylamino)butanediamide
Canonical SMILES
CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@H]([C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)N)NC(=O)C4=NC5=CC=CC=C5C=C4)O
InChI
InChI=1S/C38H50N6O5/c1-38(2,3)43-37(49)32-20-26-14-7-8-15-27(26)22-44(32)23-33(45)30(19-24-11-5-4-6-12-24)41-36(48)31(21-34(39)46)42-35(47)29-18-17-25-13-9-10-16-28(25)40-29/h4-6,9-13,16-18,26-27,30-33,45H,7-8,14-15,19-23H2,1-3H3,(H2,39,46)(H,41,48)(H,42,47)(H,43,49)/t26-,27+,30-,31-,32-,33+/m0/s1
InChIKey
QWAXKHKRTORLEM-UGJKXSETSA-N
Cross-matching ID
PubChem CID
441243
ChEBI ID
CHEBI:63621
CAS Number
127779-20-8
DrugBank ID
DB01232
TTD ID
D0WI3T
VARIDT ID
DR00309
INTEDE ID
DR1462
ACDINA ID
D00615

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Human immunodeficiency virus Protease (HIV PR) TT5FNQT POL_HV1B1 Inhibitor [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [7]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [8]
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [9]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [10]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [11]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [12]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [13]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [14]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [15]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [15]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Saquinavir
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
MK-1439 DM215WE Minor Decreased metabolism of Saquinavir caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [108]
Fostemsavir DM50ILT Major Increased risk of prolong QT interval by the combination of Saquinavir and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [109]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Saquinavir caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [110]
Dolutegravir DMCZGRE Minor Decreased metabolism of Saquinavir caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [111]
Lopinavir DMITQS0 Major Increased risk of prolong QT interval by the combination of Saquinavir and Lopinavir. Human immunodeficiency virus disease [1C60-1C62] [109]
Rilpivirine DMJ0QOW Major Increased risk of prolong QT interval by the combination of Saquinavir and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [109]
⏷ Show the Full List of 6 DDI Information of This Drug
Coadministration of a Drug Treating the Disease Different from Saquinavir (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Saquinavir and Ivosidenib. Acute myeloid leukaemia [2A60] [109]
Midostaurin DMI6E0R Major Increased risk of prolong QT interval by the combination of Saquinavir and Midostaurin. Acute myeloid leukaemia [2A60] [109]
Arn-509 DMT81LZ Major Increased risk of prolong QT interval by the combination of Saquinavir and Arn-509. Acute myeloid leukaemia [2A60] [109]
Oliceridine DM6MDCF Major Increased risk of prolong QT interval by the combination of Saquinavir and Oliceridine. Acute pain [MG31] [109]
Ivabradine DM0L594 Major Decreased metabolism of Saquinavir caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [110]
Bepridil DM0RKS4 Major Decreased metabolism of Saquinavir caused by Bepridil mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [112]
Dronedarone DMA8FS5 Major Decreased metabolism of Saquinavir caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [110]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Saquinavir and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [113]
Posaconazole DMUL5EW Major Increased risk of prolong QT interval by the combination of Saquinavir and Posaconazole. Aspergillosis [1F20] [109]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Saquinavir and Levalbuterol. Asthma [CA23] [114]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Saquinavir and Pirbuterol. Asthma [CA23] [115]
Lisdexamfetamine DM6W8V5 Major Increased risk of prolong QT interval by the combination of Saquinavir and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [109]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Saquinavir caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [116]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Saquinavir caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [112]
Retigabine DMGNYIH Major Increased risk of prolong QT interval by the combination of Saquinavir and Retigabine. Behcet disease [4A62] [109]
Cariprazine DMJYDVK Major Decreased metabolism of Saquinavir caused by Cariprazine mediated inhibition of CYP450 enzyme. Bipolar disorder [6A60] [117]
Erdafitinib DMI782S Major Decreased metabolism of Saquinavir caused by Erdafitinib mediated inhibition of CYP450 enzyme. Bladder cancer [2C94] [118]
Pexidartinib DMS2J0Z Major Decreased metabolism of Saquinavir caused by Pexidartinib mediated inhibition of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [119]
Eribulin DM1DX4Q Major Increased risk of prolong QT interval by the combination of Saquinavir and Eribulin. Breast cancer [2C60-2C6Y] [109]
Talazoparib DM1KS78 Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [120]
Ixabepilone DM2OZ3G Moderate Decreased metabolism of Saquinavir caused by Ixabepilone mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [121]
Lapatinib DM3BH1Y Major Increased risk of prolong QT interval by the combination of Saquinavir and Lapatinib. Breast cancer [2C60-2C6Y] [109]
HKI-272 DM6QOVN Major Decreased metabolism of Saquinavir caused by HKI-272 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [122]
LY2835219 DM93VBZ Major Decreased metabolism of Saquinavir caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [123]
Esterified estrogens DM9KZDO Moderate Decreased metabolism of Saquinavir caused by Esterified estrogens mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [112]
Tucatinib DMBESUA Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Tucatinib. Breast cancer [2C60-2C6Y] [124]
Palbociclib DMD7L94 Major Decreased metabolism of Saquinavir caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [125]
Quinestrol DMJ6H1Z Moderate Decreased metabolism of Saquinavir caused by Quinestrol mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [112]
Cabazitaxel DMPAZHC Moderate Decreased metabolism of Saquinavir caused by Cabazitaxel mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [110]
Bosutinib DMTI8YE Major Decreased metabolism of Saquinavir caused by Bosutinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [110]
Trastuzumab Emtansine DMU1LXS Moderate Decreased metabolism of Saquinavir caused by Trastuzumab Emtansine mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [110]
Macitentan DMP79A1 Major Decreased metabolism of Saquinavir caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [126]
PF-04449913 DMSB068 Major Increased risk of prolong QT interval by the combination of Saquinavir and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [109]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Saquinavir and Olodaterol. Chronic obstructive pulmonary disease [CA22] [115]
Vilanterol DMF5EK1 Moderate Decreased metabolism of Saquinavir caused by Vilanterol mediated inhibition of CYP450 enzyme. Chronic obstructive pulmonary disease [CA22] [127]
Revefenacin DMMP5SI Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Revefenacin. Chronic obstructive pulmonary disease [CA22] [128]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Saquinavir and Indacaterol. Chronic obstructive pulmonary disease [CA22] [115]
Arformoterol DMYM974 Moderate Increased risk of prolong QT interval by the combination of Saquinavir and Arformoterol. Chronic obstructive pulmonary disease [CA22] [115]
Levomilnacipran DMV26S8 Major Decreased metabolism of Saquinavir caused by Levomilnacipran mediated inhibition of CYP450 enzyme. Chronic pain [MG30] [129]
Fidaxomicin DMFP6MV Minor Decreased clearance of Saquinavir due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [130]
Regorafenib DMHSY1I Moderate Decreased metabolism of Saquinavir caused by Regorafenib mediated inhibition of CYP450 enzyme. Colorectal cancer [2B91] [110]
Intedanib DMSTA36 Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Intedanib. Colorectal cancer [2B91] [131]
Drospirenone DM1A9W3 Major Decreased metabolism of Saquinavir caused by Drospirenone mediated inhibition of CYP450 enzyme. Contraceptive management [QA21] [110]
Levonorgestrel DM1DP7T Moderate Decreased metabolism of Saquinavir caused by Levonorgestrel mediated inhibition of CYP450 enzyme. Contraceptive management [QA21] [112]
Ulipristal DMBNI20 Minor Decreased metabolism of Saquinavir caused by Ulipristal mediated inhibition of CYP450 enzyme. Contraceptive management [QA21] [120]
Sevoflurane DMC9O43 Major Increased risk of prolong QT interval by the combination of Saquinavir and Sevoflurane. Corneal disease [9A76-9A78] [109]
Probucol DMVZQ2M Major Increased risk of prolong QT interval by the combination of Saquinavir and Probucol. Coronary atherosclerosis [BA80] [109]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Saquinavir and Pasireotide. Cushing syndrome [5A70] [109]
Osilodrostat DMIJC9X Major Increased risk of prolong QT interval by the combination of Saquinavir and Osilodrostat. Cushing syndrome [5A70] [109]
Ivacaftor DMZC1HS Major Decreased metabolism of Saquinavir caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [110]
Rivaroxaban DMQMBZ1 Major Decreased metabolism of Saquinavir caused by Rivaroxaban mediated inhibition of CYP450 enzyme. Deep vein thrombosis [BD71] [110]
Vilazodone DM4LECQ Major Decreased metabolism of Saquinavir caused by Vilazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [132]
OPC-34712 DMHG57U Major Decreased metabolism of Saquinavir caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [133]
Clomipramine DMINRKW Major Increased risk of prolong QT interval by the combination of Saquinavir and Clomipramine. Depression [6A70-6A7Z] [109]
Polatuzumab vedotin DMF6Y0L Major Decreased metabolism of Saquinavir caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [134]
[3H]estrone-3-sulphate DMGPF0N Moderate Decreased metabolism of Saquinavir caused by [3H]estrone-3-sulphate mediated inhibition of CYP450 enzyme. Discovery agent [N.A.] [110]
Tetrabenazine DMYWQ0O Major Increased risk of prolong QT interval by the combination of Saquinavir and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [109]
Ospemifene DMC4GEI Moderate Decreased metabolism of Saquinavir caused by Ospemifene mediated inhibition of CYP450 enzyme. Dyspareunia [GA12] [135]
Deutetrabenazine DMUPFLI Major Increased risk of prolong QT interval by the combination of Saquinavir and Deutetrabenazine. Dystonic disorder [8A02] [109]
Ingrezza DMVPLNC Major Increased risk of prolong QT interval by the combination of Saquinavir and Ingrezza. Dystonic disorder [8A02] [109]
Cenobamate DMGOVHA Moderate Increased metabolism of Saquinavir caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [136]
Stiripentol DMMSDOY Moderate Decreased metabolism of Saquinavir caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [120]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Saquinavir caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [136]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Saquinavir caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [136]
Cannabidiol DM0659E Minor Decreased metabolism of Saquinavir caused by Cannabidiol mediated inhibition of CYP450 enzyme. Epileptic encephalopathy [8A62] [120]
Bay 80-6946 DMLOS5R Major Decreased clearance of Saquinavir due to the transporter inhibition by Bay 80-6946. Follicular lymphoma [2A80] [137]
Tazemetostat DMWP1BH Major Decreased metabolism of Saquinavir caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [138]
Solifenacin DMG592Q Major Increased risk of prolong QT interval by the combination of Saquinavir and Solifenacin. Functional bladder disorder [GC50] [109]
Mirabegron DMS1GYT Minor Decreased metabolism of Saquinavir caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [139]
Ripretinib DM958QB Major Decreased metabolism of Saquinavir caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [110]
Sunitinib DMCBJSR Major Increased risk of prolong QT interval by the combination of Saquinavir and Sunitinib. Gastrointestinal stromal tumour [2B5B] [109]
Avapritinib DMK2GZX Major Decreased metabolism of Saquinavir caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [120]
Colchicine DM2POTE Major Decreased metabolism of Saquinavir caused by Colchicine mediated inhibition of CYP450 enzyme. Gout [FA25] [140]
Simeprevir DMLUA9D Major Decreased metabolism of Saquinavir caused by Simeprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [110]
Daclatasvir DMSFK9V Major Decreased metabolism of Saquinavir caused by Daclatasvir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [120]
Brentuximab vedotin DMWLC57 Moderate Decreased metabolism of Saquinavir caused by Brentuximab vedotin mediated inhibition of CYP450 enzyme. Hodgkin lymphoma [2B30] [120]
BMS-201038 DMQTAGO Major Decreased metabolism of Saquinavir caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [110]
Sodium zirconium cyclosilicate DMCSLZ4 Moderate Decreased absorption of Saquinavir due to altered gastric pH caused by Sodium zirconium cyclosilicate. Hyperkalaemia [5C76] [120]
Aliskiren DM1BV7W Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [141]
Levamlodipine DM92S6N Moderate Decreased metabolism of Saquinavir caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [141]
Tolvaptan DMIWFRL Major Decreased metabolism of Saquinavir caused by Tolvaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [110]
Retapamulin DM9JXB7 Minor Decreased metabolism of Saquinavir caused by Retapamulin mediated inhibition of CYP450 enzyme. Impetigo [1B72] [142]
Lesinurad DMUR64T Moderate Increased metabolism of Saquinavir caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [136]
Berotralstat DMWA2DZ Major Decreased clearance of Saquinavir due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [143]
Suvorexant DM0E6S3 Major Decreased metabolism of Saquinavir caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [110]
Amobarbital DM0GQ8N Moderate Increased metabolism of Saquinavir caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [136]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Saquinavir caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [144]
ITI-007 DMUQ1DO Major Decreased metabolism of Saquinavir caused by ITI-007 mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [145]
Polyethylene glycol DM4I1JP Major Increased risk of ventricular arrhythmias by the combination of Saquinavir and Polyethylene glycol. Irritable bowel syndrome [DD91] [146]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Saquinavir and Phenolphthalein. Irritable bowel syndrome [DD91] [141]
Eluxadoline DMYZ0P1 Major Decreased clearance of Saquinavir due to the transporter inhibition by Eluxadoline. Irritable bowel syndrome [DD91] [120]
Naloxegol DML0B41 Major Decreased metabolism of Saquinavir caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [110]
Pemigatinib DM819JF Major Decreased metabolism of Saquinavir caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [120]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Saquinavir and Crizotinib. Lung cancer [2C25] [109]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Saquinavir and Ceritinib. Lung cancer [2C25] [109]
Lurbinectedin DMEFRTZ Major Decreased metabolism of Saquinavir caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [147]
PF-06463922 DMKM7EW Major Decreased metabolism of Saquinavir caused by PF-06463922 mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [148]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Saquinavir and Osimertinib. Lung cancer [2C25] [109]
Pralsetinib DMWU0I2 Major Decreased clearance of Saquinavir due to the transporter inhibition by Pralsetinib. Lung cancer [2C25] [149]
Capmatinib DMYCXKL Major Decreased metabolism of Saquinavir caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [150]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Saquinavir and Selpercatinib. Lung cancer [2C25] [109]
Artemether DM48QOT Major Decreased metabolism of Saquinavir caused by Artemether mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [110]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Saquinavir and Hydroxychloroquine. Malaria [1F40-1F45] [109]
Idelalisib DM602WT Moderate Decreased metabolism of Saquinavir caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [151]
GDC-0199 DMH0QKA Major Decreased metabolism of Saquinavir caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [152]
IPI-145 DMWA24P Major Decreased metabolism of Saquinavir caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [153]
Acalabrutinib DM7GCVW Major Decreased metabolism of Saquinavir caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [154]
Ibrutinib DMHZCPO Major Decreased metabolism of Saquinavir caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [110]
Ponatinib DMYGJQO Major Decreased metabolism of Saquinavir caused by Ponatinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [110]
Arry-162 DM1P6FR Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Arry-162. Melanoma [2C30] [110]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Saquinavir and Vemurafenib. Melanoma [2C30] [109]
Selumetinib DMC7W6R Major Decreased metabolism of Saquinavir caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [155]
LGX818 DMNQXV8 Major Increased risk of prolong QT interval by the combination of Saquinavir and LGX818. Melanoma [2C30] [109]
Dabrafenib DMX6OE3 Moderate Decreased metabolism of Saquinavir caused by Dabrafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [110]
Rimegepant DMHOAUG Moderate Decreased metabolism of Saquinavir caused by Rimegepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [156]
Lasmiditan DMXLVDT Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Lasmiditan. Migraine [8A80] [157]
Exjade DMHPRWG Moderate Decreased metabolism of Saquinavir caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [158]
Flibanserin DM70DTN Major Decreased metabolism of Saquinavir caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [159]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Saquinavir and Panobinostat. Multiple myeloma [2A83] [109]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Saquinavir and Siponimod. Multiple sclerosis [8A40] [110]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Saquinavir and Fingolimod. Multiple sclerosis [8A40] [141]
Ozanimod DMT6AM2 Major Increased risk of prolong QT interval by the combination of Saquinavir and Ozanimod. Multiple sclerosis [8A40] [109]
Deflazacort DMV0RNS Major Decreased metabolism of Saquinavir caused by Deflazacort mediated inhibition of CYP450 enzyme. Muscular dystrophy [8C70] [120]
Romidepsin DMT5GNL Major Increased risk of prolong QT interval by the combination of Saquinavir and Romidepsin. Mycosis fungoides [2B01] [109]
Fedratinib DM4ZBK6 Major Decreased metabolism of Saquinavir caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [120]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Saquinavir and Nilotinib. Myeloproliferative neoplasm [2A20] [109]
Ruxolitinib DM7Q98D Major Decreased metabolism of Saquinavir caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [160]
Dasatinib DMJV2EK Major Increased risk of prolong QT interval by the combination of Saquinavir and Dasatinib. Myeloproliferative neoplasm [2A20] [109]
Vorapaxar DMA16BR Major Decreased metabolism of Saquinavir caused by Vorapaxar mediated inhibition of CYP450 enzyme. Myocardial infarction [BA41-BA43] [110]
E-2007 DMJDYNQ Minor Decreased metabolism of Saquinavir caused by E-2007 mediated inhibition of CYP450 enzyme. Neuropathy [8C0Z] [120]
Entrectinib DMMPTLH Major Increased risk of prolong QT interval by the combination of Saquinavir and Entrectinib. Non-small cell lung cancer [2C25] [109]
Lofexidine DM1WXA6 Major Increased risk of prolong QT interval by the combination of Saquinavir and Lofexidine. Opioid use disorder [6C43] [109]
S-297995 DM26IH8 Moderate Decreased metabolism of Saquinavir caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [120]
Olaparib DM8QB1D Major Decreased metabolism of Saquinavir caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [110]
Rucaparib DM9PVX8 Major Increased risk of prolong QT interval by the combination of Saquinavir and Rucaparib. Ovarian cancer [2C73] [109]
MK-4827 DMLYGH4 Moderate Decreased clearance of Saquinavir due to the transporter inhibition by MK-4827. Ovarian cancer [2C73] [161]
Triclabendazole DMPWGBR Major Increased risk of prolong QT interval by the combination of Saquinavir and Triclabendazole. Parasitic worm infestation [1F90] [109]
Istradefylline DM20VSK Major Decreased metabolism of Saquinavir caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [162]
Pimavanserin DMR7IVC Major Increased risk of prolong QT interval by the combination of Saquinavir and Pimavanserin. Parkinsonism [8A00] [109]
Abametapir DM2RX0I Moderate Decreased metabolism of Saquinavir caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [163]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Saquinavir and Macimorelin. Pituitary gland disorder [5A60-5A61] [164]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Saquinavir and Lefamulin. Pneumonia [CA40] [109]
Ergonovine DM0VEC1 Major Decreased metabolism of Saquinavir caused by Ergonovine mediated inhibition of CYP450 enzyme. Postpartum haemorrhage [JA43] [165]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Saquinavir caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [166]
Degarelix DM3O8QY Major Increased risk of prolong QT interval by the combination of Saquinavir and Degarelix. Prostate cancer [2C82] [109]
ABIRATERONE DM8V75C Major Increased risk of prolong QT interval by the combination of Saquinavir and ABIRATERONE. Prostate cancer [2C82] [109]
Enzalutamide DMGL19D Major Increased risk of prolong QT interval by the combination of Saquinavir and Enzalutamide. Prostate cancer [2C82] [109]
Relugolix DMK7IWL Major Increased risk of prolong QT interval by the combination of Saquinavir and Relugolix. Prostate cancer [2C82] [109]
Darolutamide DMV7YFT Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [167]
Silodosin DMJSBT6 Major Decreased metabolism of Saquinavir caused by Silodosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [110]
Levomepromazine DMIKFEL Major Increased risk of prolong QT interval by the combination of Saquinavir and Levomepromazine. Psychotic disorder [6A20-6A25] [109]
Ambrisentan DMD1QXW Minor Decreased metabolism of Saquinavir caused by Ambrisentan mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [168]
Riociguat DMXBLMP Major Decreased clearance of Saquinavir due to the transporter inhibition by Riociguat. Pulmonary hypertension [BB01] [110]
Everolimus DM8X2EH Major Decreased metabolism of Saquinavir caused by Everolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [110]
Axitinib DMGVH6N Major Decreased metabolism of Saquinavir caused by Axitinib mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [110]
Temsirolimus DMS104F Major Increased metabolism of Saquinavir caused by Temsirolimus mediated induction of CYP450 enzyme. Renal cell carcinoma [2C90] [110]
Ciclesonide DM2NA4K Moderate Decreased metabolism of Saquinavir caused by Ciclesonide mediated inhibition of CYP450 enzyme. Respiratory system disease [CB40-CB7Z] [169]
Upadacitinib DM32B5U Major Decreased metabolism of Saquinavir caused by Upadacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [170]
Tofacitinib DMBS370 Major Decreased metabolism of Saquinavir caused by Tofacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [110]
Dexamethasone DMMWZET Moderate Decreased metabolism of Saquinavir caused by Dexamethasone mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [110]
Aripiprazole DM3NUMH Moderate Decreased metabolism of Saquinavir caused by Aripiprazole mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [171]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Saquinavir and Iloperidone. Schizophrenia [6A20] [109]
Paliperidone DM7NPJS Major Increased risk of prolong QT interval by the combination of Saquinavir and Paliperidone. Schizophrenia [6A20] [109]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Saquinavir and Amisulpride. Schizophrenia [6A20] [109]
Asenapine DMSQZE2 Major Increased risk of prolong QT interval by the combination of Saquinavir and Asenapine. Schizophrenia [6A20] [109]
Avanafil DM75CXN Major Decreased metabolism of Saquinavir caused by Avanafil mediated inhibition of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [110]
Voxelotor DMCS6M5 Major Decreased metabolism of Saquinavir caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [172]
LDE225 DMM9F25 Major Decreased metabolism of Saquinavir caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [173]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Saquinavir caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [120]
Larotrectinib DM26CQR Major Decreased metabolism of Saquinavir caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [110]
Docetaxel DMDI269 Major Decreased metabolism of Saquinavir caused by Docetaxel mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [174]
Trabectedin DMG3Y89 Major Decreased metabolism of Saquinavir caused by Trabectedin mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [110]
Armodafinil DMGB035 Moderate Decreased metabolism of Saquinavir caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [175]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Saquinavir and LEE011. Solid tumour/cancer [2A00-2F9Z] [109]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Saquinavir and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [109]
Triptorelin DMTK4LS Major Increased risk of prolong QT interval by the combination of Saquinavir and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [109]
Pitolisant DM8RFNJ Major Increased risk of prolong QT interval by the combination of Saquinavir and Pitolisant. Somnolence [MG42] [109]
Telavancin DM58VQX Major Increased risk of prolong QT interval by the combination of Saquinavir and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [109]
Pomalidomide DMTGBAX Moderate Decreased metabolism of Saquinavir caused by Pomalidomide mediated inhibition of CYP450 enzyme. Systemic sclerosis [4A42] [110]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Saquinavir due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [176]
As-1670542 DMV05SW Moderate Decreased metabolism of Saquinavir caused by As-1670542 mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [120]
Apixaban DM89JLN Major Decreased metabolism of Saquinavir caused by Apixaban mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [110]
Brilinta DMBR01X Major Decreased metabolism of Saquinavir caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [110]
Lenvatinib DMB1IU4 Major Increased risk of prolong QT interval by the combination of Saquinavir and Lenvatinib. Thyroid cancer [2D10] [109]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Saquinavir and Cabozantinib. Thyroid cancer [2D10] [109]
Saxagliptin DMGXENV Moderate Decreased metabolism of Saquinavir caused by Saxagliptin mediated inhibition of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [120]
Elagolix DMB2C0E Major Decreased metabolism of Saquinavir caused by Elagolix mediated inhibition of CYP450 enzyme. Uterine fibroid [2E86] [177]
Trimeprazine DMEMV9D Major Increased risk of prolong QT interval by the combination of Saquinavir and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [110]
Fluticasone DMGCSVF Major Decreased metabolism of Saquinavir caused by Fluticasone mediated inhibition of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [178]
⏷ Show the Full List of 189 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
FD&C blue no. 2 E00446 2723854 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferric oxide black E00522 16211978 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Gelatin E00630 Not Available Other agent
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Water E00035 962 Solvent
Colcothar yellow E00436 518696 Colorant
Haematite red E00236 14833 Colorant
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 20 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Saquinavir 200 mg capsule 200 mg Oral Capsule Oral
Saquinavir Mesylate eq 200mg base capsule eq 200mg base Capsule Oral
Saquinavir Mesylate eq 500mg base tablet eq 500mg base Tablet Oral
Saquinavir 500 mg tablet 500 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: 4813).
2 Approved antiretroviral drugs. Antiretroviral Drugs. Company report of AVERT. 2009.
3 FDA Approved Drug Products: Invirase (saquinavir mesylate) oral tablets
4 BDDCS applied to over 900 drugs
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 PL-100, a novel HIV-1 protease inhibitor displaying a high genetic barrier to resistance: an in vitro selection study. J Med Virol. 2008 Dec;80(12):2053-63.
7 Evidence for two interacting ligand binding sites in human multidrug resistance protein 2 (ATP binding cassette C2). J Biol Chem. 2003 Jun 27;278(26):23538-44.
8 Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004 Jan 12;1(1):49-56.
9 Direct evidence that saquinavir is transported by multidrug resistance-associated protein (MRP1) and canalicular multispecific organic anion transporter (MRP2). Antimicrob Agents Chemother. 2002 Nov;46(11):3456-62.
10 Nicotine and cotinine increases the brain penetration of saquinavir in rat. J Neurochem. 2010 Dec;115(6):1495-507.
11 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
12 Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26.
13 Effect of saquinavir-ritonavir on cytochrome P450 3A4 activity in healthy volunteers using midazolam as a probe. Pharmacotherapy. 2009 Oct;29(10):1175-81.
14 Inhibition of desipramine hydroxylation (Cytochrome P450-2D6) in vitro by quinidine and by viral protease inhibitors: relation to drug interactions in vivo. J Pharm Sci. 1998 Oct;87(10):1184-9.
15 Differential inhibition of cytochrome P450 3A4, 3A5 and 3A7 by five human immunodeficiency virus (HIV) protease inhibitors in vitro. Basic Clin Pharmacol Toxicol. 2006 Jan;98(1):79-85.
16 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.
17 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
18 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.
19 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
20 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.
21 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.
22 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
23 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.
24 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.
25 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
26 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
27 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
28 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
29 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
30 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
31 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
32 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
33 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.
34 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.
35 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.
36 Drug Interactions Flockhart Table
37 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.
38 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
39 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
40 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
41 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
42 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.
43 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
44 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
45 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.
46 The role of bioreductive activation of doxorubicin in cytotoxic activity against leukaemia HL60-sensitive cell line and its multidrug-resistant sublines. Br J Cancer. 2005 Jul 11;93(1):89-97.
47 Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32.
48 Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
49 Hammerhead ribozyme against gamma-glutamylcysteine synthetase sensitizes human colonic cancer cells to cisplatin by down-regulating both the glutathione synthesis and the expression of multidrug resistance proteins. Cancer Gene Ther. 2001 Oct;8(10):803-14.
50 Multidrug resistance-associated protein-1 functional activity in Calu-3 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1199-205.
51 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
52 ATP-Dependent efflux of CPT-11 and SN-38 by the multidrug resistance protein (MRP) and its inhibition by PAK-104P. Mol Pharmacol. 1999 May;55(5):921-8.
53 Structural determinants of substrate specificity differences between human multidrug resistance protein (MRP) 1 (ABCC1) and MRP3 (ABCC3). Drug Metab Dispos. 2008 Dec;36(12):2571-81.
54 Evaluation of transport of common antiepileptic drugs by human multidrug resistance-associated proteins (MRP1, 2 and 5) that are overexpressed in pharmacoresistant epilepsy. Neuropharmacology. 2010 Jun;58(7):1019-32.
55 Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83.
56 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.
57 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
58 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
59 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.
60 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
61 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.
62 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.
63 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.
64 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.
65 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
66 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
67 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.
68 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
69 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
70 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
71 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.
72 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
73 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
74 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.
75 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
76 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
77 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
78 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.
79 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
80 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
81 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
82 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
83 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.
84 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.
85 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.
86 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
87 FDA Drug Development and Drug Interactions
88 Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. J Pharmacol Exp Ther. 2006 Aug;318(2):521-9.
89 Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3. Pflugers Arch. 2001 Nov;443(2):188-95.
90 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
91 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
92 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
93 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
94 Uptake of enalapril and expression of organic anion transporting polypeptide 1 in zonal, isolated rat hepatocytes. Drug Metab Dispos. 2000 Jul;28(7):801-6.
95 Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82.
96 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.
97 Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol. J Pharm Sci. 2009 Jul;98(7):2529-39.
98 Quantification of HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors in peripheral blood mononuclear cell lysate using liq... J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Feb 15;877(5-6):575-80.
99 Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. Int J Antimicrob Agents. 2009 Apr;33(4):307-20.
100 Hollow-fiber unit evaluation of a new human immunodeficiency virus type 1 protease inhibitor, BMS-232632, for determination of the linked pharmacod... J Infect Dis. 2001 Apr 1;183(7):1126-9.
101 Darunavir: a review of its use in the management of HIV infection in adults. Drugs. 2009;69(4):477-503.
102 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
103 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
104 Fosamprenavir/ritonavir in advanced HIV disease (TRIAD): a randomized study of high-dose, dual-boosted or standard dose fosamprenavir/ritonavir in ... J Antimicrob Chemother. 2009 Aug;64(2):398-410.
105 2011 Pipeline of Boehringer Ingelheim Pharma.
106 2011 Pipeline of Bristol-Myers Squibb.
107 2011 Pipeline of InterMune.
108 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
109 Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475]
110 Cerner Multum, Inc. "Australian Product Information.".
111 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
112 Product Information. Fortovase (saquinavir) Roche Laboratories, Nutley, NJ.
113 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
114 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
115 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
116 Product Information. Synercid (dalfopristin-quinupristin) Rhone-Poulenc Rorer, Collegeville, PA.
117 Product Information. Vraylar (cariprazine). Actavis Pharma, Inc., Parsippany, NJ.
118 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
119 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
120 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
121 Product Information. Ixempra (ixabepilone). Bristol-Myers Squibb, Princeton, NJ.
122 Abbas R, Hug BA, Leister C, Burns J, Sonnichsen D "Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects." Br J Clin Pharmacol 71 (2011): 522-7. [PMID: 21395644]
123 Product Information. Verzenio (abemaciclib). Lilly, Eli and Company, Indianapolis, IN.
124 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
125 Product Information. Ibrance (palbociclib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
126 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
127 Product Information. Breo Ellipta (fluticasone-vilanterol). GlaxoSmithKline, Research Triangle Park, NC.
128 Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
129 Product Information. Fetzima (levomilnacipran). Forest Pharmaceuticals, St. Louis, MO.
130 Product Information. Dificid (fidaxomicin). Optimer Pharmaceuticals, San Diego, CA.
131 Product Information. Ofev (nintedanib). Boehringer Ingelheim, Ridgefield, CT.
132 Product Information. Viibryd (vilazodone). Trovis Pharmaceuticals LLC, New Haven, CT.
133 Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
134 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
135 Product Information. Osphena (ospemifene). Shionogi USA Inc, Florham Park, NJ.
136 Acosta EP, Henry K, Baken L, Page LM, Fletcher CV "Indinavir concentrations and antiviral effect." Pharmacotherapy 19 (1999): 708-12. [PMID: 10391416]
137 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
138 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
139 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
140 Akdag I, Ersoy A, Kahvecioglu S, Gullulu M, Dilek K "Acute colchicine intoxication during clarithromycin administration in patients with chronic renal failure." J Nephrol 19 (2006): 515-7. [PMID: 17048210]
141 Canadian Pharmacists Association.
142 Product Information. Altabax (retapamulin topical). GlaxoSmithKline, Research Triangle Park, NC.
143 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
144 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
145 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
146 Hill AG, Parry BR "Hypokalaemia following bowel cleansing with sodium phosphate." N Z Med J 109 (1996): 347. [PMID: 8862361]
147 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
148 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
149 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
150 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
151 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
152 Product Information. Venclexta (venetoclax). AbbVie US LLC, North Chicago, IL.
153 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
154 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
155 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
156 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
157 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
158 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
159 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
160 Product Information. Jakafi (ruxolitinib). Incyte Corporation, Wilmington, DE.
161 Product Information. Zejula (niraparib). Tesaro Inc., Waltham, MA.
162 Product Information. Nourianz (istradefylline). Kyowa Kirin, Inc, Bedminster, NJ.
163 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
164 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
165 Baldwin ZK, Ceraldi CC "Ergotism associated with HIV antiviral protease inhibitor therapy." J Vasc Surg 37 (2003): 676-8. [PMID: 12618710]
166 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
167 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
168 Product Information. Letairis (ambrisentan). Gilead Sciences, Foster City, CA.
169 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
170 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
171 Product Information. Abilify (aripiprazole). Bristol-Myers Squibb, Princeton, NJ.
172 Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.
173 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
174 Aronson JK, Grahame-Smith DG "Clinical pharmacology: adverse drug interactions." Br Med J 282 (1981): 288-91. [PMID: 6779990]
175 Barry M, Gibbons S, Back D, Mulcahy F "Protease inhibitors in patients with HIV disease. Clinically important pharmacokinetic considerations." Clin Pharmacokinet 32 (1997): 194-209. [PMID: 9084959]
176 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
177 Product Information. Orilissa (elagolix). AbbVie US LLC, North Chicago, IL.
178 Arrington-Sanders R, Hutton N, Siberry GK "Ritonavir-fluticasone interaction causing Cushing syndrome in HIV-infected children and adolescents." Pediatr Infect Dis J 25 (2006): 1044-1048. [PMID: 17072128]