General Information of Drug (ID: DM7HXWT)

Drug Name
Nilotinib
Synonyms
NIL; Nilotinibum; Tasigna (Novartis); Nilotinib (INN/USAN); Nilotinib, AMN107, Tasigna; Tasigna, AMN-107, Nilotinib; L-1-yl)-3-(trifluoromethyl)phenyl]benzamide; Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-(9CI); 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazo; 4-Methyl-N-(3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-pyridin-3-ylpyrimidin-2-yl)amino)benzamide; 4-Methyl-N-[3-(4-methylimidazol-1-yl)-5-trifluoromethylphenyl]-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino]benzamide; 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide; Nilotinib (BCR-ABL inhibitor 2nd gen)
Indication
Disease Entry ICD 11 Status REF
Chronic myelogenous leukaemia 2A20.0 Approved [1]
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 529.5
Logarithm of the Partition Coefficient (xlogp) 4.9
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 9
ADMET Property
Absorption
The drug is orally available []
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [2]
Elimination
4% of drug is excreted from urine in the unchanged form [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 15 hours [3]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 21.58252 micromolar/kg/day [4]
Chemical Identifiers
Formula
C28H22F3N7O
IUPAC Name
4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
Canonical SMILES
CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
InChI
InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37)
InChIKey
HHZIURLSWUIHRB-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
644241
ChEBI ID
CHEBI:52172
CAS Number
641571-10-0
DrugBank ID
DB04868
TTD ID
D00STL
VARIDT ID
DR00013
INTEDE ID
DR1155
ACDINA ID
D00468
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Fusion protein Bcr-Abl (Bcr-Abl) TTS7G69 BCR_HUMAN-ABL1_HUMAN Modulator [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [6]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [7]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [7]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [9]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [10]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Acetyl-CoA carboxylase 1 (ACACA) OT5CQPZY ACACA_HUMAN Post-Translational Modifications [11]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Protein Interaction/Cellular Processes [12]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [13]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Drug Response [14]
Breakpoint cluster region protein (BCR) OTCN76C1 BCR_HUMAN Post-Translational Modifications [15]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Drug Response [16]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [11]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Gene/Protein Processing [11]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Protein Interaction/Cellular Processes [13]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Protein Interaction/Cellular Processes [17]
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 Nilotinib
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Nilotinib caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [18]
Ruxolitinib DM7Q98D Minor Decreased metabolism of Nilotinib caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [19]
Coadministration of a Drug Treating the Disease Different from Nilotinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Nilotinib and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [20]
Sarecycline DMLZNIQ Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Sarecycline . Acne vulgaris [ED80] [18]
Metreleptin DM1NOEK Moderate Increased metabolism of Nilotinib caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [18]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Nilotinib and Ivosidenib. Acute myeloid leukaemia [2A60] [21]
Midostaurin DMI6E0R Major Increased risk of prolong QT interval by the combination of Nilotinib and Midostaurin. Acute myeloid leukaemia [2A60] [21]
Arn-509 DMT81LZ Major Increased metabolism of Nilotinib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [18]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Nilotinib and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [21]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Nilotinib and Levalbuterol. Asthma [CA23] [22]
Retigabine DMGNYIH Major Increased risk of prolong QT interval by the combination of Nilotinib and Retigabine. Behcet disease [4A62] [21]
Cariprazine DMJYDVK Moderate Decreased metabolism of Nilotinib caused by Cariprazine mediated inhibition of CYP450 enzyme. Bipolar disorder [6A60] [23]
Erdafitinib DMI782S Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [24]
Pexidartinib DMS2J0Z Major Decreased metabolism of Nilotinib caused by Pexidartinib mediated inhibition of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [25]
Eribulin DM1DX4Q Major Increased risk of prolong QT interval by the combination of Nilotinib and Eribulin. Breast cancer [2C60-2C6Y] [21]
Talazoparib DM1KS78 Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [26]
LY2835219 DM93VBZ Moderate Decreased metabolism of Nilotinib caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [27]
Tucatinib DMBESUA Major Decreased metabolism of Nilotinib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [20]
Palbociclib DMD7L94 Moderate Decreased metabolism of Nilotinib caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [18]
Alpelisib DMEXMYK Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Alpelisib. Breast cancer [2C60-2C6Y] [18]
Cabazitaxel DMPAZHC Moderate Decreased metabolism of Nilotinib caused by Cabazitaxel mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [28]
Bosutinib DMTI8YE Moderate Decreased metabolism of Nilotinib caused by Bosutinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [18]
Macitentan DMP79A1 Moderate Decreased metabolism of Nilotinib caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [29]
PF-04449913 DMSB068 Major Increased risk of prolong QT interval by the combination of Nilotinib and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [21]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Nilotinib and Olodaterol. Chronic obstructive pulmonary disease [CA22] [30]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Nilotinib and Vilanterol. Chronic obstructive pulmonary disease [CA22] [22]
Fidaxomicin DMFP6MV Minor Decreased clearance of Nilotinib due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [20]
Intedanib DMSTA36 Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Intedanib. Colorectal cancer [2B91] [31]
Ulipristal DMBNI20 Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Ulipristal. Contraceptive management [QA21] [18]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Nilotinib and Pasireotide. Cushing syndrome [5A70] [21]
Osilodrostat DMIJC9X Major Increased risk of prolong QT interval by the combination of Nilotinib and Osilodrostat. Cushing syndrome [5A70] [21]
Lumacaftor DMCLWDJ Major Increased metabolism of Nilotinib caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [32]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Nilotinib caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [18]
MK-8228 DMOB58Q Moderate Decreased metabolism of Nilotinib caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [18]
Rivaroxaban DMQMBZ1 Moderate Decreased metabolism of Nilotinib caused by Rivaroxaban mediated inhibition of CYP450 enzyme. Deep vein thrombosis [BD71] [33]
Desvenlafaxine DMHD4PE Moderate Decreased metabolism of Nilotinib caused by Desvenlafaxine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [18]
OPC-34712 DMHG57U Major Decreased metabolism of Nilotinib caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [34]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Nilotinib caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [35]
SODIUM CITRATE DMHPD2Y Moderate Decreased absorption of Nilotinib due to altered gastric pH caused by SODIUM CITRATE. Discovery agent [N.A.] [20]
Ospemifene DMC4GEI Moderate Decreased metabolism of Nilotinib caused by Ospemifene mediated inhibition of CYP450 enzyme. Dyspareunia [GA12] [36]
Deutetrabenazine DMUPFLI Major Increased risk of prolong QT interval by the combination of Nilotinib and Deutetrabenazine. Dystonic disorder [8A02] [21]
Ingrezza DMVPLNC Major Increased risk of prolong QT interval by the combination of Nilotinib and Ingrezza. Dystonic disorder [8A02] [21]
Cenobamate DM8KLU9 Moderate Increased metabolism of Nilotinib caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Rufinamide DMWE60C Moderate Increased metabolism of Nilotinib caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Nilotinib caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Nilotinib and Cannabidiol. Epileptic encephalopathy [8A62] [19]
Bay 80-6946 DMLOS5R Moderate Decreased metabolism of Nilotinib caused by Bay 80-6946 mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [37]
Tazemetostat DMWP1BH Moderate Increased metabolism of Nilotinib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [18]
Mirabegron DMS1GYT Minor Decreased metabolism of Nilotinib caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [38]
Dexlansoprazole DM1DBV5 Moderate Increased risk of hypomagnesemia by the combination of Nilotinib and Dexlansoprazole. Gastro-oesophageal reflux disease [DA22] [18]
Ripretinib DM958QB Moderate Decreased metabolism of Nilotinib caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [20]
Avapritinib DMK2GZX Moderate Decreased metabolism of Nilotinib caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [19]
Boceprevir DMBSHMF Major Decreased metabolism of Nilotinib caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [18]
Telaprevir DMMRV29 Major Decreased metabolism of Nilotinib caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [20]
Daclatasvir DMSFK9V Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Daclatasvir. Hepatitis virus infection [1E50-1E51] [18]
GS-5885 DMSL3DX Moderate Decreased clearance of Nilotinib due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [39]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Nilotinib and Brentuximab vedotin. Hodgkin lymphoma [2B30] [40]
MK-1439 DM215WE Minor Decreased metabolism of Nilotinib caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [41]
Fostemsavir DM50ILT Major Increased risk of prolong QT interval by the combination of Nilotinib and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [21]
Cobicistat DM6L4H2 Major Decreased metabolism of Nilotinib caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [20]
Dolutegravir DMCZGRE Minor Decreased metabolism of Nilotinib caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [42]
Etravirine DMGV8QU Moderate Decreased metabolism of Nilotinib caused by Etravirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [43]
Rilpivirine DMJ0QOW Major Increased risk of prolong QT interval by the combination of Nilotinib and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [21]
Raltegravir DMYURI6 Minor Decreased metabolism of Nilotinib caused by Raltegravir mediated inhibition of UGT. Human immunodeficiency virus disease [1C60-1C62] [44]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Nilotinib and Mipomersen. Hyper-lipoproteinaemia [5C80] [45]
Teriflunomide DMQ2FKJ Major Additive immunosuppressive effects by the combination of Nilotinib and Teriflunomide. Hyper-lipoproteinaemia [5C80] [46]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Nilotinib and BMS-201038. Hyper-lipoproteinaemia [5C80] [47]
Sodium zirconium cyclosilicate DMCSLZ4 Moderate Decreased absorption of Nilotinib due to altered gastric pH caused by Sodium zirconium cyclosilicate. Hyperkalaemia [5C76] [19]
Aliskiren DM1BV7W Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [21]
Levamlodipine DM92S6N Moderate Decreased metabolism of Nilotinib caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [18]
Tolvaptan DMIWFRL Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [48]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Nilotinib caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [18]
Suvorexant DM0E6S3 Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Suvorexant. Insomnia [7A00-7A0Z] [18]
ITI-007 DMUQ1DO Moderate Decreased metabolism of Nilotinib caused by ITI-007 mediated inhibition of UGT. Insomnia [7A00-7A0Z] [49]
Polyethylene glycol DM4I1JP Major Increased risk of ventricular arrhythmias by the combination of Nilotinib and Polyethylene glycol. Irritable bowel syndrome [DD91] [50]
Naloxegol DML0B41 Minor Decreased metabolism of Nilotinib caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [51]
Pemigatinib DM819JF Moderate Decreased metabolism of Nilotinib caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [19]
Denosumab DMNI0KO Moderate Additive myelosuppressive effects by the combination of Nilotinib and Denosumab. Low bone mass disorder [FB83] [52]
Brigatinib DM7W94S Moderate Decreased metabolism of Nilotinib caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [20]
PF-06463922 DMKM7EW Moderate Increased metabolism of Nilotinib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [18]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Nilotinib and Osimertinib. Lung cancer [2C25] [21]
Capmatinib DMYCXKL Moderate Decreased metabolism of Nilotinib caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [18]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Nilotinib and Lumefantrine. Malaria [1F40-1F45] [20]
Artesunate DMR27C8 Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Artesunate. Malaria [1F40-1F45] [18]
Inotuzumab ozogamicin DMAC130 Major Increased risk of prolong QT interval by the combination of Nilotinib and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [21]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Nilotinib and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [53]
Idelalisib DM602WT Major Decreased metabolism of Nilotinib caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [20]
GDC-0199 DMH0QKA Major Decreased metabolism of Nilotinib caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [20]
Acalabrutinib DM7GCVW Moderate Decreased metabolism of Nilotinib caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [54]
Ibrutinib DMHZCPO Moderate Decreased metabolism of Nilotinib caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [55]
Ponatinib DMYGJQO Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Ponatinib. Mature B-cell lymphoma [2A85] [18]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Nilotinib and Vemurafenib. Melanoma [2C30] [21]
LGX818 DMNQXV8 Major Increased risk of prolong QT interval by the combination of Nilotinib and LGX818. Melanoma [2C30] [21]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Nilotinib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [18]
Lasmiditan DMXLVDT Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Lasmiditan. Migraine [8A80] [56]
Flibanserin DM70DTN Moderate Decreased metabolism of Nilotinib caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [57]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Nilotinib and Tecfidera. Multiple sclerosis [8A40] [58]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Nilotinib and Siponimod. Multiple sclerosis [8A40] [20]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Nilotinib and Fingolimod. Multiple sclerosis [8A40] [59]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Nilotinib and Ocrelizumab. Multiple sclerosis [8A40] [60]
Ozanimod DMT6AM2 Major Increased risk of prolong QT interval by the combination of Nilotinib and Ozanimod. Multiple sclerosis [8A40] [21]
Romidepsin DMT5GNL Major Increased risk of prolong QT interval by the combination of Nilotinib and Romidepsin. Mycosis fungoides [2B01] [21]
Rolapitant DM8XP26 Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [20]
S-297995 DM26IH8 Moderate Decreased metabolism of Nilotinib caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [19]
Rucaparib DM9PVX8 Major Increased risk of prolong QT interval by the combination of Nilotinib and Rucaparib. Ovarian cancer [2C73] [21]
Triclabendazole DMPWGBR Major Increased risk of prolong QT interval by the combination of Nilotinib and Triclabendazole. Parasitic worm infestation [1F90] [21]
Istradefylline DM20VSK Moderate Decreased metabolism of Nilotinib caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [18]
Pimavanserin DMR7IVC Major Increased risk of prolong QT interval by the combination of Nilotinib and Pimavanserin. Parkinsonism [8A00] [21]
Abametapir DM2RX0I Moderate Decreased metabolism of Nilotinib caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [61]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Nilotinib and Macimorelin. Pituitary gland disorder [5A60-5A61] [62]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Nilotinib and Lefamulin. Pneumonia [CA40] [63]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Nilotinib caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [20]
Degarelix DM3O8QY Major Increased risk of prolong QT interval by the combination of Nilotinib and Degarelix. Prostate cancer [2C82] [21]
ABIRATERONE DM8V75C Major Increased risk of prolong QT interval by the combination of Nilotinib and ABIRATERONE. Prostate cancer [2C82] [21]
Enzalutamide DMGL19D Major Increased metabolism of Nilotinib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [18]
Relugolix DMK7IWL Major Increased risk of prolong QT interval by the combination of Nilotinib and Relugolix. Prostate cancer [2C82] [64]
Darolutamide DMV7YFT Minor Decreased metabolism of Nilotinib caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [65]
Silodosin DMJSBT6 Moderate Decreased metabolism of Nilotinib caused by Silodosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [66]
Selexipag DMAHSU0 Moderate Decreased metabolism of Nilotinib caused by Selexipag mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [67]
Ambrisentan DMD1QXW Moderate Decreased metabolism of Nilotinib caused by Ambrisentan mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [18]
Riociguat DMXBLMP Moderate Decreased metabolism of Nilotinib caused by Riociguat mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [20]
Axitinib DMGVH6N Moderate Decreased metabolism of Nilotinib caused by Axitinib mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [19]
Temsirolimus DMS104F Moderate Decreased metabolism of Nilotinib caused by Temsirolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [18]
Canakinumab DM8HLO5 Moderate Additive immunosuppressive effects by the combination of Nilotinib and Canakinumab. Rheumatoid arthritis [FA20] [68]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Nilotinib and Rilonacept. Rheumatoid arthritis [FA20] [68]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Nilotinib and Golimumab. Rheumatoid arthritis [FA20] [69]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Nilotinib and Iloperidone. Schizophrenia [6A20] [21]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Nilotinib and Amisulpride. Schizophrenia [6A20] [21]
Asenapine DMSQZE2 Major Increased risk of prolong QT interval by the combination of Nilotinib and Asenapine. Schizophrenia [6A20] [21]
LDE225 DMM9F25 Moderate Decreased metabolism of Nilotinib caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [70]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Nilotinib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [19]
Larotrectinib DM26CQR Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Larotrectinib. Solid tumour/cancer [2A00-2F9Z] [20]
PDX-101 DM6OC53 Moderate Decreased metabolism of Nilotinib caused by PDX-101 mediated inhibition of UGT. Solid tumour/cancer [2A00-2F9Z] [71]
Trabectedin DMG3Y89 Moderate Decreased metabolism of Nilotinib caused by Trabectedin mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [19]
Armodafinil DMGB035 Minor Decreased metabolism of Nilotinib caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [20]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Nilotinib and LEE011. Solid tumour/cancer [2A00-2F9Z] [21]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Nilotinib and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [21]
Pitolisant DM8RFNJ Major Increased risk of prolong QT interval by the combination of Nilotinib and Pitolisant. Somnolence [MG42] [21]
Telavancin DM58VQX Major Increased risk of prolong QT interval by the combination of Nilotinib and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [21]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Nilotinib caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [72]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [18]
Apixaban DM89JLN Moderate Decreased metabolism of Nilotinib caused by Apixaban mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [19]
Brilinta DMBR01X Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Brilinta. Thrombosis [DB61-GB90] [18]
Lenvatinib DMB1IU4 Major Increased risk of prolong QT interval by the combination of Nilotinib and Lenvatinib. Thyroid cancer [2D10] [21]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Nilotinib and Cabozantinib. Thyroid cancer [2D10] [21]
Elagolix DMB2C0E Moderate Increased metabolism of Nilotinib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [18]
Betrixaban DM2C4RF Moderate Decreased clearance of Nilotinib due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [18]
⏷ Show the Full List of 145 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
Crospovidone E00626 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferric oxide black E00522 16211978 Colorant
Gelatin E00630 Not Available Other agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Poloxamer 188 E00645 Not Available Emulsifying agent; Solubilizing agent; Surfactant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Colcothar yellow E00436 518696 Colorant
Haematite red E00236 14833 Colorant
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
⏷ Show the Full List of 13 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Nilotinib Hydrochloride Monohydrate eq 50mg base capsule eq 50mg base Capsule Oral
Nilotinib Hydrochloride Monohydrate eq 150mg base capsule eq 150mg base Capsule Oral
Nilotinib Hydrochloride Monohydrate eq 200mg base capsule eq 200mg base Capsule Oral
Nilotinib 150 mg capsule 150 mg Oral Capsule Oral
Nilotinib 200 mg capsule 200 mg Oral Capsule 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: 5697).
2 BDDCS applied to over 900 drugs
3 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4 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
5 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
6 Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64.
7 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
8 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
9 Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib. Blood. 2011 Feb 24;117(8):e75-87.
10 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
11 Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes. Toxicol Appl Pharmacol. 2013 Oct 1;272(1):245-55.
12 Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes. Toxicol Lett. 2018 Jul;291:138-148. doi: 10.1016/j.toxlet.2018.04.010. Epub 2018 Apr 12.
13 Nilotinib reduced the viability of human ovarian cancer cells via mitochondria-dependent apoptosis, independent of JNK activation. Toxicol In Vitro. 2016 Mar;31:1-11. doi: 10.1016/j.tiv.2015.11.002. Epub 2015 Nov 6.
14 Reversal of ABCB1 mediated efflux by imatinib and nilotinib in cells expressing various transporter levels. Chem Biol Interact. 2017 Aug 1;273:171-179. doi: 10.1016/j.cbi.2017.06.012. Epub 2017 Jun 13.
15 AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028.
16 Resistance to daunorubicin, imatinib, or nilotinib depends on expression levels of ABCB1 and ABCG2 in human leukemia cells. Chem Biol Interact. 2014 Aug 5;219:203-10. doi: 10.1016/j.cbi.2014.06.009. Epub 2014 Jun 19.
17 p53 Gene (NY-CO-13) Levels in Patients with Chronic Myeloid Leukemia: The Role of Imatinib and Nilotinib. Diseases. 2018 Jan 25;6(1):13. doi: 10.3390/diseases6010013.
18 Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
19 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
20 Cerner Multum, Inc. "Australian Product Information.".
21 Canadian Pharmacists Association.
22 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
23 Product Information. Vraylar (cariprazine). Actavis Pharma, Inc., Parsippany, NJ.
24 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
25 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
26 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
27 Product Information. Verzenio (abemaciclib). Lilly, Eli and Company, Indianapolis, IN.
28 Product Information. Jevtana (cabazitaxel). sanofi-aventis , Bridgewater, NJ.
29 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
30 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
31 Product Information. Ofev (nintedanib). Boehringer Ingelheim, Ridgefield, CT.
32 Patel S, Robinson R, Burk M "Hypertensive crisis associated with St. John's Wort." Am J Med 112 (2002): 507-8. [PMID: 11959071]
33 Product Information. Xarelto (rivaroxaban). Bayer Inc, Toronto, IA.
34 Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
35 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
36 Product Information. Osphena (ospemifene). Shionogi USA Inc, Florham Park, NJ.
37 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
38 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
39 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
40 Product Information. VFEND (voriconazole). Pfizer U.S. Pharmaceuticals, New York, NY.
41 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
42 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
43 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
44 Product Information. Isentress (raltegravir). Merck & Company Inc, West Point, PA.
45 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
46 Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
47 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
48 Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
49 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
50 Hill AG, Parry BR "Hypokalaemia following bowel cleansing with sodium phosphate." N Z Med J 109 (1996): 347. [PMID: 8862361]
51 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
52 Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
53 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]
54 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
55 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
56 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
57 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
58 Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
59 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
60 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
61 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
62 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
63 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
64 Product Information. Orgovyx (relugolix). Myovant Sciences, Inc., Brisbane, CA.
65 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
66 Product Information. Rapaflo (silodosin). Watson Pharmaceuticals, Corona, CA.
67 Product Information. Uptravi (selexipag). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
68 Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
69 Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
70 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
71 Product Information. Beleodaq (belinostat). Spectrum Pharmaceuticals Inc, Irvine, CA.
72 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.