Details of the Drug

General Information of Drug (ID: DMT5GNL)

Drug Name
Romidepsin
Synonyms
Chromadax; Istodax; Antibiotic FR 901228; FK 228; FK228; FR 901228; FR901228; HDInhib_000006; Chromadax (TN); FK-228; FK-901228; FR-901228; Istodax (TN); Romidepsin (USAN); Cyclo((2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl), cyclic (35)-disulfide; L-Valine, N-((3S,4E)-3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-D-valyl-D-cysteinyl-(2Z)-2-amino-2-butenoxyl-, (4-1)-lactone, cyclic (1-2)-disulfide; (1S,4S,7Z,10S,16E,21R)-7-Ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo(8.7.6)tricos-16-ene-3,6,9,19,22-pentone; (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone; (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
Indication
Disease Entry ICD 11 Status REF
Cutaneous T-cell lymphoma 2B01 Approved [1], [2]
Peripheral T-cell lymphoma 2A90.C Phase 3 [3]
Renal cell carcinoma 2C90 Phase 3 [1], [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 540.7
Topological Polar Surface Area (xlogp) 2.2
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Clearance
The clearance of drug is 8.4 L/h [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 3 hours [6]
Metabolism
The drug is metabolized via the hepatic [7]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.64 micromolar/kg/day [8]
Unbound Fraction
The unbound fraction of drug in plasma is 0.07% [6]
Vd
The volume of distribution (Vd) of drug is 44.5 L [5]
Chemical Identifiers
Formula
C24H36N4O6S2
IUPAC Name
(1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
Canonical SMILES
C/C=C\\1/C(=O)N[C@H](C(=O)O[C@H]\\2CC(=O)N[C@@H](C(=O)N[C@H](CSSCC/C=C2)C(=O)N1)C(C)C)C(C)C
InChI
InChI=1S/C24H36N4O6S2/c1-6-16-21(30)28-20(14(4)5)24(33)34-15-9-7-8-10-35-36-12-17(22(31)25-16)26-23(32)19(13(2)3)27-18(29)11-15/h6-7,9,13-15,17,19-20H,8,10-12H2,1-5H3,(H,25,31)(H,26,32)(H,27,29)(H,28,30)/b9-7+,16-6-/t15-,17-,19-,20+/m1/s1
InChIKey
OHRURASPPZQGQM-GCCNXGTGSA-N
Cross-matching ID
PubChem CID
5352062
ChEBI ID
CHEBI:61080
CAS Number
128517-07-7
DrugBank ID
DB06176
TTD ID
D0L7LC
VARIDT ID
DR00233
INTEDE ID
DR1438
ACDINA ID
D01401

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histone deacetylase 1 (HDAC1) TT6R7JZ HDAC1_HUMAN Inhibitor [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [9]
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]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [11]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Substrate [12]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Cutaneous T-cell lymphoma
ICD Disease Classification 2B01
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histone deacetylase 1 (HDAC1) DTT HDAC1 6.27E-01 0.11 0.33
P-glycoprotein 1 (ABCB1) DTP P-GP 2.30E-01 3.06E-01 7.43E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 5.85E-01 1.81E-01 6.68E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 2.05E-01 -1.49E-01 -3.36E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 8.58E-01 -3.73E-03 -1.00E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.76E-01 -4.64E-01 -9.16E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Romidepsin (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sarecycline DMLZNIQ Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Sarecycline . Acne vulgaris [ED80] [64]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Romidepsin and Ivosidenib. Acute myeloid leukaemia [2A60] [65]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Midostaurin. Acute myeloid leukaemia [2A60] [66]
Arn-509 DMT81LZ Moderate Increased metabolism of Romidepsin caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [64]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Gilteritinib. Acute myeloid leukaemia [2A60] [67]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Oliceridine. Acute pain [MG31] [68]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Romidepsin and Ivabradine. Angina pectoris [BA40] [69]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Romidepsin and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [70]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Levalbuterol. Asthma [CA23] [71]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Romidepsin caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [64]
Erdafitinib DMI782S Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [72]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Romidepsin caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [73]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Eribulin. Breast cancer [2C60-2C6Y] [66]
Tucatinib DMBESUA Moderate Decreased metabolism of Romidepsin caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [64]
Alpelisib DMEXMYK Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Alpelisib. Breast cancer [2C60-2C6Y] [64]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [74]
Olodaterol DM62B78 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Olodaterol. Chronic obstructive pulmonary disease [CA22] [75]
Vilanterol DMF5EK1 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Vilanterol. Chronic obstructive pulmonary disease [CA22] [71]
Regorafenib DMHSY1I Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Regorafenib. Colorectal cancer [2B91] [64]
Ulipristal DMBNI20 Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Ulipristal. Contraceptive management [QA21] [64]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Romidepsin and Pasireotide. Cushing syndrome [5A70] [66]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Osilodrostat. Cushing syndrome [5A70] [65]
Lumacaftor DMCLWDJ Moderate Increased metabolism of Romidepsin caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [76]
Ivacaftor DMZC1HS Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [64]
Deutetrabenazine DMUPFLI Moderate Additive CNS depression effects by the combination of Romidepsin and Deutetrabenazine. Dystonic disorder [8A02] [77]
Ingrezza DMVPLNC Moderate Additive CNS depression effects by the combination of Romidepsin and Ingrezza. Dystonic disorder [8A02] [78]
Stiripentol DMMSDOY Moderate Decreased metabolism of Romidepsin caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [79]
Boceprevir DMBSHMF Moderate Decreased metabolism of Romidepsin caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [64]
Daclatasvir DMSFK9V Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Daclatasvir. Hepatitis virus infection [1E50-1E51] [64]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [80]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Romidepsin caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [64]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [66]
Teriflunomide DMQ2FKJ Major Additive myelosuppressive effects by the combination of Romidepsin and Teriflunomide. Hyper-lipoproteinaemia [5C80] [81]
BMS-201038 DMQTAGO Moderate Decreased clearance of Romidepsin due to the transporter inhibition by BMS-201038. Hyper-lipoproteinaemia [5C80] [64]
Tolvaptan DMIWFRL Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [64]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Romidepsin and Polyethylene glycol. Irritable bowel syndrome [DD91] [69]
Denosumab DMNI0KO Moderate Additive myelosuppressive effects by the combination of Romidepsin and Denosumab. Low bone mass disorder [FB83] [82]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Romidepsin and Crizotinib. Lung cancer [2C25] [83]
Brigatinib DM7W94S Moderate Increased metabolism of Romidepsin caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [84]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Romidepsin and Ceritinib. Lung cancer [2C25] [66]
PF-06463922 DMKM7EW Moderate Increased metabolism of Romidepsin caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [85]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Romidepsin and Osimertinib. Lung cancer [2C25] [86]
Capmatinib DMYCXKL Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [64]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Romidepsin and Selpercatinib. Lung cancer [2C25] [87]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Romidepsin and Lumefantrine. Malaria [1F40-1F45] [88]
IPI-145 DMWA24P Moderate Decreased metabolism of Romidepsin caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [89]
Ponatinib DMYGJQO Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Ponatinib. Mature B-cell lymphoma [2A85] [64]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Romidepsin and Vemurafenib. Melanoma [2C30] [66]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and LGX818. Melanoma [2C30] [90]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Romidepsin caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [69]
Lasmiditan DMXLVDT Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Lasmiditan. Migraine [8A80] [91]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Romidepsin and Panobinostat. Multiple myeloma [2A83] [92]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Romidepsin and Tecfidera. Multiple sclerosis [8A40] [93]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Romidepsin and Siponimod. Multiple sclerosis [8A40] [88]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Romidepsin and Fingolimod. Multiple sclerosis [8A40] [94]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Romidepsin and Ocrelizumab. Multiple sclerosis [8A40] [95]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Romidepsin and Ozanimod. Multiple sclerosis [8A40] [69]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Romidepsin caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [69]
Rolapitant DM8XP26 Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [64]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Entrectinib. Non-small cell lung cancer [2C25] [69]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Rucaparib. Ovarian cancer [2C73] [66]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Triclabendazole. Parasitic worm infestation [1F90] [68]
Istradefylline DM20VSK Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Istradefylline. Parkinsonism [8A00] [64]
Abametapir DM2RX0I Moderate Decreased metabolism of Romidepsin caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [96]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Romidepsin and Macimorelin. Pituitary gland disorder [5A60-5A61] [97]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Romidepsin and Lefamulin. Pneumonia [CA40] [65]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Romidepsin caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [64]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Degarelix. Prostate cancer [2C82] [69]
Enzalutamide DMGL19D Moderate Increased metabolism of Romidepsin caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [64]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Relugolix. Prostate cancer [2C82] [69]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Romidepsin and Rilonacept. Rheumatoid arthritis [FA20] [98]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Romidepsin and Golimumab. Rheumatoid arthritis [FA20] [99]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Romidepsin and Amisulpride. Schizophrenia [6A20] [100]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Asenapine. Schizophrenia [6A20] [66]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Romidepsin when combined with Anthrax vaccine. Sepsis [1G40-1G41] [101]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Romidepsin caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [69]
Larotrectinib DM26CQR Moderate Decreased metabolism of Romidepsin caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [88]
LEE011 DMMX75K Major Decreased metabolism of Romidepsin caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [66]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [69]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Pitolisant. Somnolence [MG42] [66]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [66]
Fostamatinib DM6AUHV Moderate Decreased clearance of Romidepsin due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [102]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Romidepsin and Lenvatinib. Thyroid cancer [2D10] [66]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Romidepsin and Cabozantinib. Thyroid cancer [2D10] [69]
⏷ Show the Full List of 84 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
DL-alpha-tocopherol E00052 2116 Antioxidant
Ethanol E00023 702 Antimicrobial preservative; Penetration agent; Solvent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Romidepsin 10mg/2ml solution 10mg/2ml Solution Intravenous
Romidepsin 27.5mg/5.5ml solution 27.5mg/5.5ml Solution Intravenous
Romidepsin 10mg/vial powder 10mg/vial Powder Intravenous
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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