Details of the Drug

General Information of Drug (ID: DMIMF8J)

Drug Name
Risdiplam
Synonyms
UNII-76RS4S2ET1; 76RS4S2ET1; 1825352-65-5; Risdiplam [INN]; SCHEMBL17260852; EX-A2074; RG-7916; HY-109101; RO7034067; CS-0039501; 4H-Pyrido(1,2-a)pyrimidin-4-one, 7-(4,7-diazaspiro(2.5)oct-7-yl)-2-(2,8-dimethylimidazo(1,2-b)pyridazin-6-yl)-; 2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)-7-(4,7-diazaspiro[2.5]octan-7-yl)-4H-pyrido[1,2-a]pyrimidin-4-one
Indication
Disease Entry ICD 11 Status REF
Spinal muscular atrophy 8B61 Approved [1]
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 401.5
Logarithm of the Partition Coefficient (xlogp) 0.5
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 6
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1-4 h [2]
Elimination
Following the oral administration of 18mg risdiplam, approximately 53% of the dose was excreted in the feces and 28% was excreted in the urine [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 50 hours [2]
Metabolism
The drug is metabolized via the flavin monooxygenases 1 and 3 (FMO1 and FMO3), with some involvement of CYP1A1, CYP2J2, CYP3A4, and CYP3A7 [2]
Vd
The volume of distribution (Vd) of drug is 6.3 L/kg [3]
Chemical Identifiers
Formula
C22H23N7O
IUPAC Name
7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one
Canonical SMILES
CC1=CC(=NN2C1=NC(=C2)C)C3=CC(=O)N4C=C(C=CC4=N3)N5CCNC6(C5)CC6
InChI
InChI=1S/C22H23N7O/c1-14-9-18(26-29-11-15(2)24-21(14)29)17-10-20(30)28-12-16(3-4-19(28)25-17)27-8-7-23-22(13-27)5-6-22/h3-4,9-12,23H,5-8,13H2,1-2H3
InChIKey
ASKZRYGFUPSJPN-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
118513932
CAS Number
1825352-65-5
DrugBank ID
DB15305
TTD ID
D0N5MH
INTEDE ID
DR1823
ACDINA ID
D01397
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Isomalt E00383 88735 Binding agent; Coating agent; Diluent; Flavoring agent; Suspending agent
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium benzoate E00432 517055 Antimicrobial preservative; lubricant
Sucralose E00370 71485 Flavoring agent
Ascorbic acid E00579 54670067 Acidulant; Antioxidant
Edetate disodium E00186 8759 Complexing agent
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Tartaric acid E00029 875 Acidulant; Complexing agent; Flavoring agent
⏷ Show the Full List of 8 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Risdiplam 0.75 mg/ml powder 0.75 mg/ml Powder Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
2 FDA Approved Drug Products: Evrysdi (risdiplam) powder for oral solution
3 Ramdas S, Servais L: New treatments in spinal muscular atrophy: an overview of currently available data. Expert Opin Pharmacother. 2020 Feb;21(3):307-315. doi: 10.1080/14656566.2019.1704732.
4 A phase 1 healthy male volunteer single escalating dose study of the pharmacokinetics and pharmacodynamics of risdiplam (RG7916, RO7034067), a SMN2 splicing modifier. Br J Clin Pharmacol. 2019 Jan;85(1):181-193.