Details of the Drug

General Information of Drug (ID: DMIWFRL)

Drug Name
Tolvaptan
Synonyms
Samsca; OPC 41061; Benzazepine derivative, 32; OPC-41061; Samsca (TN); N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide; (-)-4'-((7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl)-o-tolu-m-toluidide; 7-Chloro-5-hydroxy-1-(2-methyl-4-(2-methylbenzoylamino)benzoyl)2,3,4,5-tetrahydro-1H-1-benzazepine
Indication
Disease Entry ICD 11 Status REF
Hyponatraemia 5C72 Approved [1], [2]
Heart failure BD10-BD13 Phase 3 [1], [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 448.9
Topological Polar Surface Area (xlogp) 4.8
Rotatable Bond Count (rotbonds) 3
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Clearance
The clearance of drug is 4 mL/min/kg [4]
Elimination
0% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 12 hours [5]
Metabolism
The drug is metabolized via the CYP3A4 enzyme in the liver [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.9092 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.01% [5]
Vd
The volume of distribution (Vd) of drug is 3 L/kg [4]
Water Solubility
The ability of drug to dissolve in water is measured as 0.0005 mg/mL [3]
Chemical Identifiers
Formula
C26H25ClN2O3
IUPAC Name
N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
Canonical SMILES
CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C
InChI
InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)
InChIKey
GYHCTFXIZSNGJT-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
216237
ChEBI ID
CHEBI:32246
CAS Number
150683-30-0
DrugBank ID
DB06212
TTD ID
D03KZM
VARIDT ID
DR00059
INTEDE ID
DR1617
ACDINA ID
D00688

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Vasopressin V2 receptor (V2R) TTK8R02 V2R_HUMAN Antagonist [8], [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [10]
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 Disease Different from Tolvaptan (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Tolvaptan and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [37]
Sarecycline DMLZNIQ Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Sarecycline . Acne vulgaris [ED80] [38]
Metreleptin DM1NOEK Moderate Increased metabolism of Tolvaptan caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [39]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Tolvaptan caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [39]
Midostaurin DMI6E0R Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [38]
Arn-509 DMT81LZ Major Increased metabolism of Tolvaptan caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [39]
Gilteritinib DMWQ4MZ Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Gilteritinib. Acute myeloid leukaemia [2A60] [39]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Tolvaptan and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [40]
ABT-492 DMJFD2I Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by ABT-492. Bacterial infection [1A00-1C4Z] [37]
Troleandomycin DMUZNIG Major Decreased metabolism of Tolvaptan caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [37]
Erdafitinib DMI782S Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [38]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Tolvaptan and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [41]
Talazoparib DM1KS78 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [42]
Tucatinib DMBESUA Major Decreased metabolism of Tolvaptan caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [37]
Alpelisib DMEXMYK Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Alpelisib. Breast cancer [2C60-2C6Y] [38]
Bosutinib DMTI8YE Moderate Decreased metabolism of Tolvaptan caused by Bosutinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [39]
PF-04449913 DMSB068 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by PF-04449913. Chronic myelomonocytic leukaemia [2A40] [38]
Fidaxomicin DMFP6MV Minor Decreased clearance of Tolvaptan due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [37]
Ulipristal DMBNI20 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Ulipristal. Contraceptive management [QA21] [38]
Lumacaftor DMCLWDJ Major Increased metabolism of Tolvaptan caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [39]
Ivacaftor DMZC1HS Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [38]
MK-8228 DMOB58Q Moderate Decreased metabolism of Tolvaptan caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [38]
Rivaroxaban DMQMBZ1 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Rivaroxaban. Deep vein thrombosis [BD71] [43]
Empagliflozin DMRF9YK Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Empagliflozin. Diabetes mellitus [5A10] [37]
Stiripentol DMMSDOY Moderate Decreased metabolism of Tolvaptan caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [38]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Tolvaptan and Cannabidiol. Epileptic encephalopathy [8A62] [39]
Ripretinib DM958QB Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Ripretinib. Gastrointestinal stromal tumour [2B5B] [37]
Boceprevir DMBSHMF Major Decreased metabolism of Tolvaptan caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [37]
Daclatasvir DMSFK9V Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Daclatasvir. Hepatitis virus infection [1E50-1E51] [38]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Tolvaptan and Brentuximab vedotin. Hodgkin lymphoma [2B30] [44]
Cobicistat DM6L4H2 Major Decreased metabolism of Tolvaptan caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Tolvaptan and Teriflunomide. Hyper-lipoproteinaemia [5C80] [45]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Tolvaptan and BMS-201038. Hyper-lipoproteinaemia [5C80] [46]
Aliskiren DM1BV7W Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [45]
TAK-491 DMCF6SX Moderate Increased risk of hyperkalemia by the combination of Tolvaptan and TAK-491. Hypertension [BA00-BA04] [38]
Berotralstat DMWA2DZ Major Decreased clearance of Tolvaptan due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [47]
Suvorexant DM0E6S3 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Suvorexant. Insomnia [7A00-7A0Z] [38]
Naloxegol DML0B41 Minor Decreased clearance of Tolvaptan due to the transporter inhibition by Naloxegol. Large intestine motility disorder [DB32] [48]
Crizotinib DM4F29C Moderate Decreased metabolism of Tolvaptan caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [38]
Brigatinib DM7W94S Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Brigatinib. Lung cancer [2C25] [38]
PF-06463922 DMKM7EW Moderate Increased metabolism of Tolvaptan caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [39]
Pralsetinib DMWU0I2 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Pralsetinib. Lung cancer [2C25] [37]
Capmatinib DMYCXKL Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [38]
Selpercatinib DMZR15V Moderate Decreased metabolism of Tolvaptan caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [39]
Artesunate DMR27C8 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Artesunate. Malaria [1F40-1F45] [37]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Tolvaptan and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [49]
Idelalisib DM602WT Major Decreased metabolism of Tolvaptan caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [37]
GDC-0199 DMH0QKA Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [38]
IPI-145 DMWA24P Moderate Decreased metabolism of Tolvaptan caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [38]
Ibrutinib DMHZCPO Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Ibrutinib. Mature B-cell lymphoma [2A85] [39]
Ponatinib DMYGJQO Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Ponatinib. Mature B-cell lymphoma [2A85] [38]
Arry-162 DM1P6FR Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Arry-162. Melanoma [2C30] [37]
Vemurafenib DM62UG5 Moderate Increased metabolism of Tolvaptan caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [39]
LGX818 DMNQXV8 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by LGX818. Melanoma [2C30] [38]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Tolvaptan caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [39]
Ubrogepant DM749I3 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Ubrogepant. Migraine [8A80] [50]
Rimegepant DMHOAUG Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Rimegepant. Migraine [8A80] [51]
Lasmiditan DMXLVDT Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Lasmiditan. Migraine [8A80] [38]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Tolvaptan caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [38]
Rolapitant DM8XP26 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [38]
Netupitant DMEKAYI Moderate Decreased metabolism of Tolvaptan caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [38]
S-297995 DM26IH8 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by S-297995. Opioid use disorder [6C43] [37]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Tolvaptan caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [52]
MK-4827 DMLYGH4 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by MK-4827. Ovarian cancer [2C73] [37]
Istradefylline DM20VSK Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Istradefylline. Parkinsonism [8A00] [38]
Abametapir DM2RX0I Moderate Decreased metabolism of Tolvaptan caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [53]
Lefamulin DME6G97 Moderate Decreased metabolism of Tolvaptan caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [54]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Tolvaptan caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [37]
Enzalutamide DMGL19D Major Increased metabolism of Tolvaptan caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [39]
Relugolix DMK7IWL Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Relugolix. Prostate cancer [2C82] [37]
Darolutamide DMV7YFT Minor Decreased metabolism of Tolvaptan caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [55]
Selexipag DMAHSU0 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Selexipag. Pulmonary hypertension [BB01] [37]
Riociguat DMXBLMP Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Riociguat. Pulmonary hypertension [BB01] [37]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Tolvaptan caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [38]
Sodium chloride DMM3950 Moderate Increased risk of hypernatremia by the combination of Tolvaptan and Sodium chloride. Skin sensation disturbance [ME65] [39]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Tolvaptan caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [39]
Larotrectinib DM26CQR Moderate Decreased metabolism of Tolvaptan caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [37]
Armodafinil DMGB035 Moderate Increased metabolism of Tolvaptan caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [39]
LEE011 DMMX75K Moderate Decreased metabolism of Tolvaptan caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [38]
Fostamatinib DM6AUHV Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [38]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [52]
Apixaban DM89JLN Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Apixaban. Thrombosis [DB61-GB90] [39]
Brilinta DMBR01X Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Brilinta. Thrombosis [DB61-GB90] [38]
Cabozantinib DMIYDT4 Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Cabozantinib. Thyroid cancer [2D10] [38]
Elagolix DMB2C0E Moderate Increased metabolism of Tolvaptan caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [39]
Betrixaban DM2C4RF Moderate Decreased clearance of Tolvaptan due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [56]
⏷ Show the Full List of 86 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
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Tolvaptan 15 mg tablet 15 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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