General Information of Drug (ID: DMMSDOY)

Drug Name
Stiripentol
Synonyms Diacomit; ME-2080; Stiripentol (oral); Stiripentol (oral), Laboratoires Biocodex
Indication
Disease Entry ICD 11 Status REF
Dravet syndrome 8A61.11 Approved [1]
Epilepsy 8A60-8A68 Approved [2], [3]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 234.29
Topological Polar Surface Area (xlogp) 3.6
Rotatable Bond Count (rotbonds) 3
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 0.5-1 h [4]
Bioavailability
The bioavailability of drug is 3%-4% [4]
Elimination
About 73% of total administered dose is found in urine as metabolites, while further 13-24% of the total dose is recovered in faeces as unchanged substance [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 4.5 - 13 hours [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 213.4036 micromolar/kg/day [6]
Vd
The volume of distribution (Vd) of drug is 1.03 L/kg [7]
Chemical Identifiers
Formula
C14H18O3
IUPAC Name
(E)-1-(1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
Canonical SMILES
CC(C)(C)C(/C=C/C1=CC2=C(C=C1)OCO2)O
InChI
InChI=1S/C14H18O3/c1-14(2,3)13(15)7-5-10-4-6-11-12(8-10)17-9-16-11/h4-8,13,15H,9H2,1-3H3/b7-5+
InChIKey
IBLNKMRFIPWSOY-FNORWQNLSA-N
Cross-matching ID
PubChem CID
5311454
ChEBI ID
CHEBI:94435
CAS Number
49763-96-4
DrugBank ID
DB09118
TTD ID
D02XSA
INTEDE ID
DR1507
ACDINA ID
D01440

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
GABA(A) receptor gamma-3 (GABRG3) TTEX6LM GBRG3_HUMAN Modulator [3], [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [9]
Mephenytoin 4-hydroxylase (CYP2C19)
Main DME
DEGTFWK CP2CJ_HUMAN Substrate [10]
Cytochrome P450 1A2 (CYP1A2)
Main DME
DEJGDUW CP1A2_HUMAN Substrate [11]
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 Stiripentol (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased metabolism of Stiripentol caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [45]
Arn-509 DMT81LZ Major Increased metabolism of Stiripentol caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [46]
Oliceridine DM6MDCF Major Decreased metabolism of Stiripentol caused by Oliceridine mediated inhibition of CYP450 enzyme. Acute pain [MG31] [47]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Stiripentol caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [46]
HKI-272 DM6QOVN Major Decreased metabolism of Stiripentol caused by HKI-272 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [48]
LY2835219 DM93VBZ Moderate Decreased metabolism of Stiripentol caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [49]
Levonorgestrel DM1DP7T Moderate Decreased metabolism of Stiripentol caused by Levonorgestrel mediated inhibition of CYP450 enzyme. Contraceptive management [QA21] [50]
Lumacaftor DMCLWDJ Major Increased metabolism of Stiripentol caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [46]
MK-8228 DMOB58Q Moderate Decreased metabolism of Stiripentol caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [46]
OPC-34712 DMHG57U Major Decreased metabolism of Stiripentol caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [51]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Stiripentol caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [52]
Ripretinib DM958QB Moderate Decreased metabolism of Stiripentol caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [53]
MK-1439 DM215WE Minor Decreased metabolism of Stiripentol caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [54]
Levamlodipine DM92S6N Moderate Decreased metabolism of Stiripentol caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [55]
Lesinurad DMUR64T Moderate Increased metabolism of Stiripentol caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [46]
Eluxadoline DMYZ0P1 Moderate Decreased metabolism of Stiripentol caused by Eluxadoline mediated inhibition of CYP450 enzyme. Irritable bowel syndrome [DD91] [56]
Pemigatinib DM819JF Major Decreased metabolism of Stiripentol caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [46]
Brigatinib DM7W94S Major Decreased metabolism of Stiripentol caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [53]
PF-06463922 DMKM7EW Moderate Increased metabolism of Stiripentol caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [46]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Stiripentol caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [57]
Capmatinib DMYCXKL Moderate Decreased metabolism of Stiripentol caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [58]
GDC-0199 DMH0QKA Major Decreased metabolism of Stiripentol caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [53]
Acalabrutinib DM7GCVW Major Decreased metabolism of Stiripentol caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [59]
LGX818 DMNQXV8 Major Decreased metabolism of Stiripentol caused by LGX818 mediated inhibition of CYP450 enzyme. Melanoma [2C30] [60]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Stiripentol and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [61]
Rimegepant DMHOAUG Moderate Decreased metabolism of Stiripentol caused by Rimegepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [62]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Stiripentol and Lasmiditan. Migraine [8A80] [63]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Stiripentol caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [46]
Entrectinib DMMPTLH Major Decreased metabolism of Stiripentol caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [53]
S-297995 DM26IH8 Moderate Decreased metabolism of Stiripentol caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [46]
Istradefylline DM20VSK Moderate Decreased metabolism of Stiripentol caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [64]
Darolutamide DMV7YFT Minor Decreased metabolism of Stiripentol caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [65]
Upadacitinib DM32B5U Moderate Decreased metabolism of Stiripentol caused by Upadacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [66]
LDE225 DMM9F25 Major Decreased metabolism of Stiripentol caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [67]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Stiripentol caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [46]
Larotrectinib DM26CQR Moderate Decreased metabolism of Stiripentol caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [53]
LEE011 DMMX75K Moderate Decreased metabolism of Stiripentol caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [46]
Pitolisant DM8RFNJ Moderate Decreased metabolism of Stiripentol caused by Pitolisant mediated inhibition of CYP450 enzyme. Somnolence [MG42] [46]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Stiripentol caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [68]
Elagolix DMB2C0E Moderate Increased metabolism of Stiripentol caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [46]
Fluticasone DMGCSVF Moderate Decreased metabolism of Stiripentol caused by Fluticasone mediated inhibition of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [53]
⏷ Show the Full List of 41 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
Aspartame E00402 134601 Flavoring agent
Erythrosine sodium anhydrous E00324 27872 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Vanillin E00049 1183 Flavoring agent
Carmellose sodium E00625 Not Available Disintegrant
Dextrin E00359 62698 Binding agent; Diluent; Microencapsulating agent; Stiffening agent; Suspending agent; Viscosity-controlling agent
Dextrose anhydrous E00394 107526 Binding agent; Diluent; Flavoring agent; Tonicity agent
Gelatin E00630 Not Available Other agent
Hypromellose E00634 Not Available Coating agent
Magnesium stearate E00208 11177 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Sorbitan tristearate E00516 17800859 Dispersing agent; Emulsifying agent; Solubilizing agent; Surfactant; Suspending agent; Vaccine adjuvant
Hydroxyethyl cellulose E00700 Not Available Coating agent; Suspending agent; Binding agent; Viscosity-controlling agent
⏷ Show the Full List of 14 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Stiripentol 250 mg powder 250 mg Powder Oral
Stiripentol 500 mg powder 500 mg Powder Oral
Stiripentol 250 mg capsule 250 mg Capsule Oral
Stiripentol 500 mg capsule 500 mg Capsule Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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56 Product Information. Viberzi (eluxadoline). Actavis Pharma, Inc., Parsippany, NJ.
57 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
58 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
59 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
60 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
61 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
62 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
63 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
64 Product Information. Nourianz (istradefylline). Kyowa Kirin, Inc, Bedminster, NJ.
65 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
66 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
67 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
68 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.