General Information of Drug (ID: DMMRV29)

Drug Name
Telaprevir
Synonyms
402957-28-2; VX-950; Incivek; Telaprevir (VX-950); Incivo; MP-424; VX 950; Telavic; VX-950(Telaprevir); LY-570310; UNII-655M5O3W0U; VRT-111950; CHEMBL231813; CHEBI:68595; 655M5O3W0U; S-Telaprevir; (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-6-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)-octahydrocyclopenta[c]pyrrole-1-carboxamide
Indication
Disease Entry ICD 11 Status REF
Hepatitis C virus infection 1E51.1 Approved [1], [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 2 Molecular Weight (mw) 679.8
Topological Polar Surface Area (xlogp) 4.2
Rotatable Bond Count (rotbonds) 14
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 3-6 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Bioavailability
The bioavailability of drug is 25% [3]
Clearance
The total body clearance of drug is 32.4 L/h [5]
Elimination
Telaprevir is mainly eliminated in the feces (82%) with a smaller amount eliminated via expiration (9%) and very little in the urine (1%) [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 4.0 - 4.7 hours [6]
Metabolism
The drug is metabolized via the hydrolysis, oxidation, and reduction [6]
Vd
The volume of distribution (Vd) of drug is 252 L [5]
Chemical Identifiers
Formula
C36H53N7O6
IUPAC Name
(3S,3aS,6aR)-2-[(2S)-2-[[(2S)-2-cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamide
Canonical SMILES
CCC[C@@H](C(=O)C(=O)NC1CC1)NC(=O)[C@@H]2[C@H]3CCC[C@H]3CN2C(=O)[C@H](C(C)(C)C)NC(=O)[C@H](C4CCCCC4)NC(=O)C5=NC=CN=C5
InChI
InChI=1S/C36H53N7O6/c1-5-10-25(29(44)34(48)39-23-15-16-23)40-33(47)28-24-14-9-13-22(24)20-43(28)35(49)30(36(2,3)4)42-32(46)27(21-11-7-6-8-12-21)41-31(45)26-19-37-17-18-38-26/h17-19,21-25,27-28,30H,5-16,20H2,1-4H3,(H,39,48)(H,40,47)(H,41,45)(H,42,46)/t22-,24-,25-,27-,28-,30+/m0/s1
InChIKey
BBAWEDCPNXPBQM-GDEBMMAJSA-N
Cross-matching ID
PubChem CID
3010818
ChEBI ID
CHEBI:68595
CAS Number
402957-28-2
DrugBank ID
DB05521
TTD ID
D0X9CH
VARIDT ID
DR00702
INTEDE ID
DR1543
ACDINA ID
D00654

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Hepatitis C virus Serine protease NS3/4A (HCV NS3/4A) TTHC7JD POLG_HCV1 Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [8]
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 Telaprevir
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Simeprevir DMLUA9D Major Decreased metabolism of Telaprevir caused by Simeprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [27]
Daclatasvir DMSFK9V Major Decreased metabolism of Telaprevir caused by Daclatasvir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [28]
GS-9857 DMYU6P5 Moderate Decreased clearance of Telaprevir due to the transporter inhibition by GS-9857. Hepatitis virus infection [1E50-1E51] [29]
Coadministration of a Drug Treating the Disease Different from Telaprevir (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Decreased metabolism of Telaprevir caused by Ivosidenib mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [30]
Midostaurin DMI6E0R Major Decreased metabolism of Telaprevir caused by Midostaurin mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [31]
Gilteritinib DMWQ4MZ Major Decreased metabolism of Telaprevir caused by Gilteritinib mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [32]
Oliceridine DM6MDCF Major Decreased metabolism of Telaprevir caused by Oliceridine mediated inhibition of CYP450 enzyme. Acute pain [MG31] [33]
Ivabradine DM0L594 Major Decreased metabolism of Telaprevir caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [27]
Bedaquiline DM3906J Moderate Decreased metabolism of Telaprevir caused by Bedaquiline mediated inhibition of CYP450 enzyme. Antimicrobial drug resistance [MG50-MG52] [34]
Cariprazine DMJYDVK Major Decreased metabolism of Telaprevir caused by Cariprazine mediated inhibition of CYP450 enzyme. Bipolar disorder [6A60] [35]
Erdafitinib DMI782S Major Decreased metabolism of Telaprevir caused by Erdafitinib mediated inhibition of CYP450 enzyme. Bladder cancer [2C94] [36]
Pexidartinib DMS2J0Z Major Decreased metabolism of Telaprevir caused by Pexidartinib mediated inhibition of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [37]
Talazoparib DM1KS78 Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [38]
HKI-272 DM6QOVN Major Decreased metabolism of Telaprevir caused by HKI-272 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [39]
LY2835219 DM93VBZ Major Decreased metabolism of Telaprevir caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [40]
Palbociclib DMD7L94 Major Decreased metabolism of Telaprevir caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [41]
Cabazitaxel DMPAZHC Moderate Decreased metabolism of Telaprevir caused by Cabazitaxel mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [27]
Bosutinib DMTI8YE Major Decreased metabolism of Telaprevir caused by Bosutinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [27]
Trastuzumab Emtansine DMU1LXS Moderate Decreased metabolism of Telaprevir caused by Trastuzumab Emtansine mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [27]
Macitentan DMP79A1 Major Decreased metabolism of Telaprevir caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [42]
PF-04449913 DMSB068 Major Decreased metabolism of Telaprevir caused by PF-04449913 mediated inhibition of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [43]
Vilanterol DMF5EK1 Moderate Decreased metabolism of Telaprevir caused by Vilanterol mediated inhibition of CYP450 enzyme. Chronic obstructive pulmonary disease [CA22] [44]
Revefenacin DMMP5SI Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Revefenacin. Chronic obstructive pulmonary disease [CA22] [45]
Levomilnacipran DMV26S8 Major Decreased metabolism of Telaprevir caused by Levomilnacipran mediated inhibition of CYP450 enzyme. Chronic pain [MG30] [46]
Fidaxomicin DMFP6MV Minor Decreased clearance of Telaprevir due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [27]
Regorafenib DMHSY1I Moderate Decreased metabolism of Telaprevir caused by Regorafenib mediated inhibition of CYP450 enzyme. Colorectal cancer [2B91] [27]
Intedanib DMSTA36 Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Intedanib. Colorectal cancer [2B91] [47]
Levonorgestrel DM1DP7T Major Increased metabolism of Telaprevir caused by Levonorgestrel mediated induction of CYP450 enzyme. Contraceptive management [QA21] [48]
Osilodrostat DMIJC9X Major Decreased metabolism of Telaprevir caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [49]
Ivacaftor DMZC1HS Major Decreased metabolism of Telaprevir caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [27]
Rivaroxaban DMQMBZ1 Major Decreased metabolism of Telaprevir caused by Rivaroxaban mediated inhibition of CYP450 enzyme. Deep vein thrombosis [BD71] [27]
Vilazodone DM4LECQ Major Decreased metabolism of Telaprevir caused by Vilazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [50]
OPC-34712 DMHG57U Major Decreased metabolism of Telaprevir caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [51]
Polatuzumab vedotin DMF6Y0L Major Decreased metabolism of Telaprevir caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [52]
Ingrezza DMVPLNC Major Additive CNS depression effects by the combination of Telaprevir and Ingrezza. Dystonic disorder [8A02] [53]
Oestradiol valerate and dienogest DMZK0FQ Major Increased metabolism of Telaprevir caused by Oestradiol valerate and dienogest mediated induction of CYP450 enzyme. Endometriosis [GA10] [48]
Cenobamate DMGOVHA Moderate Increased metabolism of Telaprevir caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [54]
Stiripentol DMMSDOY Moderate Decreased metabolism of Telaprevir caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [28]
Lacosamide DMVM6QR Moderate Decreased metabolism of Telaprevir caused by Lacosamide mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [27]
Rufinamide DMWE60C Moderate Increased metabolism of Telaprevir caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [54]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Telaprevir caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [54]
Cannabidiol DM0659E Minor Decreased metabolism of Telaprevir caused by Cannabidiol mediated inhibition of CYP450 enzyme. Epileptic encephalopathy [8A62] [28]
Bay 80-6946 DMLOS5R Major Decreased clearance of Telaprevir due to the transporter inhibition by Bay 80-6946. Follicular lymphoma [2A80] [55]
Tazemetostat DMWP1BH Major Decreased metabolism of Telaprevir caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [56]
Mirabegron DMS1GYT Minor Decreased metabolism of Telaprevir caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [57]
Ripretinib DM958QB Major Decreased metabolism of Telaprevir caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [27]
Avapritinib DMK2GZX Major Decreased metabolism of Telaprevir caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [28]
Brentuximab vedotin DMWLC57 Moderate Decreased metabolism of Telaprevir caused by Brentuximab vedotin mediated inhibition of CYP450 enzyme. Hodgkin lymphoma [2B30] [28]
MK-1439 DM215WE Minor Decreased metabolism of Telaprevir caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [58]
Fostemsavir DM50ILT Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [59]
Dolutegravir DMCZGRE Minor Decreased metabolism of Telaprevir caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [60]
Etravirine DMGV8QU Moderate Decreased metabolism of Telaprevir caused by Etravirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [61]
BMS-201038 DMQTAGO Major Decreased metabolism of Telaprevir caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [27]
Aliskiren DM1BV7W Moderate Decreased metabolism of Telaprevir caused by Aliskiren mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [38]
Levamlodipine DM92S6N Moderate Decreased metabolism of Telaprevir caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [54]
Tolvaptan DMIWFRL Major Decreased metabolism of Telaprevir caused by Tolvaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [27]
TP-434 DM5A31S Minor Decreased metabolism of Telaprevir caused by TP-434 mediated inhibition of CYP450 enzyme. Infectious gastroenteritis/colitis [1A40] [62]
Suvorexant DM0E6S3 Major Decreased metabolism of Telaprevir caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [27]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Telaprevir caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [63]
ITI-007 DMUQ1DO Major Decreased metabolism of Telaprevir caused by ITI-007 mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [64]
Eluxadoline DMYZ0P1 Moderate Decreased metabolism of Telaprevir caused by Eluxadoline mediated inhibition of CYP450 enzyme. Irritable bowel syndrome [DD91] [65]
Naloxegol DML0B41 Major Decreased metabolism of Telaprevir caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [27]
Pemigatinib DM819JF Major Decreased metabolism of Telaprevir caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [66]
Crizotinib DM4F29C Major Decreased metabolism of Telaprevir caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [27]
Brigatinib DM7W94S Major Decreased metabolism of Telaprevir caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [67]
Lurbinectedin DMEFRTZ Major Decreased metabolism of Telaprevir caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [68]
PF-06463922 DMKM7EW Major Decreased metabolism of Telaprevir caused by PF-06463922 mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [69]
Osimertinib DMRJLAT Major Decreased metabolism of Telaprevir caused by Osimertinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [70]
Pralsetinib DMWU0I2 Major Decreased metabolism of Telaprevir caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [71]
Capmatinib DMYCXKL Major Decreased metabolism of Telaprevir caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [72]
Selpercatinib DMZR15V Major Decreased metabolism of Telaprevir caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [73]
Artemether DM48QOT Major Decreased metabolism of Telaprevir caused by Artemether mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [27]
Idelalisib DM602WT Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Idelalisib. Mature B-cell leukaemia [2A82] [74]
GDC-0199 DMH0QKA Major Decreased metabolism of Telaprevir caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [75]
IPI-145 DMWA24P Major Decreased metabolism of Telaprevir caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [76]
Acalabrutinib DM7GCVW Major Decreased metabolism of Telaprevir caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [77]
Ibrutinib DMHZCPO Major Decreased metabolism of Telaprevir caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [27]
Ponatinib DMYGJQO Major Decreased metabolism of Telaprevir caused by Ponatinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [27]
Arry-162 DM1P6FR Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Arry-162. Melanoma [2C30] [27]
Vemurafenib DM62UG5 Moderate Decreased metabolism of Telaprevir caused by Vemurafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [78]
Selumetinib DMC7W6R Major Decreased metabolism of Telaprevir caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [79]
LGX818 DMNQXV8 Major Decreased metabolism of Telaprevir caused by LGX818 mediated inhibition of CYP450 enzyme. Melanoma [2C30] [80]
Dabrafenib DMX6OE3 Moderate Decreased metabolism of Telaprevir caused by Dabrafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [27]
Ubrogepant DM749I3 Major Decreased metabolism of Telaprevir caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [81]
Rimegepant DMHOAUG Moderate Decreased metabolism of Telaprevir caused by Rimegepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [82]
Panobinostat DM58WKG Major Decreased metabolism of Telaprevir caused by Panobinostat mediated inhibition of CYP450 enzyme. Multiple myeloma [2A83] [83]
Siponimod DM2R86O Major Decreased metabolism of Telaprevir caused by Siponimod mediated inhibition of CYP450 enzyme. Multiple sclerosis [8A40] [27]
Deflazacort DMV0RNS Major Decreased metabolism of Telaprevir caused by Deflazacort mediated inhibition of CYP450 enzyme. Muscular dystrophy [8C70] [28]
Romidepsin DMT5GNL Moderate Decreased metabolism of Telaprevir caused by Romidepsin mediated inhibition of CYP450 enzyme. Mycosis fungoides [2B01] [84]
Fedratinib DM4ZBK6 Major Decreased metabolism of Telaprevir caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [28]
Ruxolitinib DM7Q98D Major Decreased metabolism of Telaprevir caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [85]
Vorapaxar DMA16BR Major Decreased metabolism of Telaprevir caused by Vorapaxar mediated inhibition of CYP450 enzyme. Myocardial infarction [BA41-BA43] [27]
Netupitant DMEKAYI Minor Decreased metabolism of Telaprevir caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [86]
E-2007 DMJDYNQ Minor Decreased metabolism of Telaprevir caused by E-2007 mediated inhibition of CYP450 enzyme. Neuropathy [8C0Z] [28]
Entrectinib DMMPTLH Major Decreased metabolism of Telaprevir caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [28]
S-297995 DM26IH8 Moderate Decreased metabolism of Telaprevir caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [28]
Olaparib DM8QB1D Major Decreased metabolism of Telaprevir caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [27]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Telaprevir caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [87]
Istradefylline DM20VSK Major Decreased metabolism of Telaprevir caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [88]
Abametapir DM2RX0I Moderate Decreased metabolism of Telaprevir caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [89]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Telaprevir caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [90]
ABIRATERONE DM8V75C Minor Decreased metabolism of Telaprevir caused by ABIRATERONE mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [91]
Enzalutamide DMGL19D Moderate Decreased metabolism of Telaprevir caused by Enzalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [92]
Darolutamide DMV7YFT Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [93]
Silodosin DMJSBT6 Major Decreased metabolism of Telaprevir caused by Silodosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [27]
Ambrisentan DMD1QXW Minor Decreased metabolism of Telaprevir caused by Ambrisentan mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [94]
Riociguat DMXBLMP Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Riociguat. Pulmonary hypertension [BB01] [27]
Axitinib DMGVH6N Major Decreased metabolism of Telaprevir caused by Axitinib mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [27]
Temsirolimus DMS104F Major Increased metabolism of Telaprevir caused by Temsirolimus mediated induction of CYP450 enzyme. Renal cell carcinoma [2C90] [27]
Upadacitinib DM32B5U Major Decreased metabolism of Telaprevir caused by Upadacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [95]
Tofacitinib DMBS370 Major Decreased metabolism of Telaprevir caused by Tofacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [27]
Avanafil DM75CXN Major Decreased metabolism of Telaprevir caused by Avanafil mediated inhibition of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [27]
Voxelotor DMCS6M5 Major Decreased metabolism of Telaprevir caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [96]
LDE225 DMM9F25 Major Decreased metabolism of Telaprevir caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [97]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Telaprevir caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [28]
Larotrectinib DM26CQR Major Decreased metabolism of Telaprevir caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [27]
Armodafinil DMGB035 Minor Decreased metabolism of Telaprevir caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [27]
LEE011 DMMX75K Major Decreased metabolism of Telaprevir caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [28]
Pomalidomide DMTGBAX Moderate Decreased metabolism of Telaprevir caused by Pomalidomide mediated inhibition of CYP450 enzyme. Systemic sclerosis [4A42] [27]
Fostamatinib DM6AUHV Major Decreased metabolism of Telaprevir caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [98]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [87]
As-1670542 DMV05SW Moderate Decreased metabolism of Telaprevir caused by As-1670542 mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [28]
Apixaban DM89JLN Major Decreased clearance of Telaprevir due to the transporter inhibition by Apixaban. Thrombosis [DB61-GB90] [27]
Brilinta DMBR01X Major Decreased metabolism of Telaprevir caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [27]
Cabozantinib DMIYDT4 Major Decreased metabolism of Telaprevir caused by Cabozantinib mediated inhibition of CYP450 enzyme. Thyroid cancer [2D10] [27]
Saxagliptin DMGXENV Moderate Decreased metabolism of Telaprevir caused by Saxagliptin mediated inhibition of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [28]
Elagolix DMB2C0E Major Decreased metabolism of Telaprevir caused by Elagolix mediated inhibition of CYP450 enzyme. Uterine fibroid [2E86] [99]
Fluticasone DMGCSVF Major Decreased metabolism of Telaprevir caused by Fluticasone mediated inhibition of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [100]
Betrixaban DM2C4RF Moderate Decreased clearance of Telaprevir due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [101]
⏷ Show the Full List of 126 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
Allura red AC dye E00338 33258 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sodium stearyl fumarate E00545 23665634 lubricant
Carmellose sodium E00625 Not Available Disintegrant
Polyethylene glycol 3350 E00652 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
⏷ Show the Full List of 10 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Telaprevir 375 mg tablet 375 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: 7871).
2 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
3 Myhre E, Rugstad HE, Hansen T: Clinical pharmacokinetics of methyldopa. Clin Pharmacokinet. 1982 May-Jun;7(3):221-33. doi: 10.2165/00003088-198207030-00003.
4 BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
5 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
6 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
7 Drug interactions and protease inhibitors used in the treatment of hepatitis C: how to manage? Eur J Clin Pharmacol. 2014 Jul;70(7):775-89.
8 Managing drug-drug interactions with boceprevir and telaprevir. Clin Liver Dis (Hoboken). 2012 Apr 26;1(2):36-40.
9 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.
10 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
11 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.
12 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
13 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.
14 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.
15 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
16 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.
17 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.
18 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
19 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
20 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.
21 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
22 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
23 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
24 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.
25 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
26 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
27 Cerner Multum, Inc. "Australian Product Information.".
28 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
29 Product Information. Vosevi (sofosbuvir/velpatasvir/voxilaprevir). Gilead Sciences, Foster City, CA.
30 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
31 Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y "Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers." Cancer Chemother Pharmacol 72 (2013): 1223-34. [PMID: 24085261]
32 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
33 Gunston GD, Mehta U "Potentially serious drug interactions with grapefruit juice." S Afr Med J 90 (2000): 41. [PMID: 10721388]
34 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
35 Product Information. Vraylar (cariprazine). Actavis Pharma, Inc., Parsippany, NJ.
36 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
37 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
38 Canadian Pharmacists Association.
39 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]
40 Product Information. Verzenio (abemaciclib). Lilly, Eli and Company, Indianapolis, IN.
41 Product Information. Ibrance (palbociclib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
42 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
43 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
44 Product Information. Breo Ellipta (fluticasone-vilanterol). GlaxoSmithKline, Research Triangle Park, NC.
45 Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
46 Product Information. Fetzima (levomilnacipran). Forest Pharmaceuticals, St. Louis, MO.
47 Product Information. Ofev (nintedanib). Boehringer Ingelheim, Ridgefield, CT.
48 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
49 Product Information. Isturisa (osilodrostat). Recordati Rare Diseases Inc, Lebanon, NJ.
50 Product Information. Viibryd (vilazodone). Trovis Pharmaceuticals LLC, New Haven, CT.
51 Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
52 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
53 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
54 Product Information. Incivek (telaprevir). Vertex Pharmaceuticals, Cambridge, MA.
55 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
56 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
57 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
58 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
59 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
60 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
61 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
62 Product Information. Xerava (eravacycline). Tetraphase Pharmaceuticals, Inc, Watertown, MA.
63 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
64 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
65 Product Information. Viberzi (eluxadoline). Actavis Pharma, Inc., Parsippany, NJ.
66 Product Information. Pemazyre (pemigatinib). Incyte Corporation, Wilmington, DE.
67 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
68 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
69 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
70 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
71 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
72 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
73 Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN.
74 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
75 Product Information. Venclexta (venetoclax). AbbVie US LLC, North Chicago, IL.
76 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
77 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
78 Product Information. Zelboraf (vemurafenib). Genentech, South San Francisco, CA.
79 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
80 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
81 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
82 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
83 Hamberg P, Woo MM, Chen LC, et al. "Effect of ketoconazole-mediated CYP3A4 inhibition on clinical pharmacokinetics of panobinostat (LBH589), an orally active histone deacetylase inhibitor." Cancer Chemother Pharmacol 68 (2011): 805-13. [PMID: 21706316]
84 Product Information. Istodax (romidepsin). Gloucester Pharmaceuticals, Cambridge, MA.
85 Product Information. Jakafi (ruxolitinib). Incyte Corporation, Wilmington, DE.
86 Product Information. Akynzeo (netupitant-palonosetron). Eisai Inc, Woodcliff Lake, NJ.
87 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
88 Product Information. Nourianz (istradefylline). Kyowa Kirin, Inc, Bedminster, NJ.
89 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
90 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
91 Product Information. Zytiga (abiraterone). Centocor Inc, Malvern, PA.
92 Product Information. Xtandi (enzalutamide). Astellas Pharma US, Inc, Deerfield, IL.
93 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
94 Product Information. Letairis (ambrisentan). Gilead Sciences, Foster City, CA.
95 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
96 Bailey DG, Arnold JMO, Spence JD "Grapefruit juice and drugs - how significant is the interaction." Clin Pharmacokinet 26 (1994): 91-8. [PMID: 8162660]
97 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
98 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
99 Product Information. Orilissa (elagolix). AbbVie US LLC, North Chicago, IL.
100 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]
101 Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA.