Details of the Drug

General Information of Drug (ID: DMLVSYX)

Drug Name
Remimazolam
Synonyms
CNS-7054; CNS-7056; CNS-7056B; CNS-7056X; GW-351564X; GW-418259X; GW-457837A; GW-502056X; ONO-2745; Short-acting sedatives, Therasci; GABA A agonist (anesthesia, sedation) CeNeS/Ono; Sedatives (short acting), CeNeS/Ono; Sedatives (short acting), PAION/Ono; Sedatives (short-acting), TheraSci; Short-acting sedatives, Therasci/GSK; Sedatives (short-acting), TheraSci/GSK
Indication
Disease Entry ICD 11 Status REF
Procedural sedation JB0C.3 Approved [1]
Anaesthesia 9A78.6 Phase 3 [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 439.3
Logarithm of the Partition Coefficient (xlogp) 3.4
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 452 mcgh/L [3]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 189-6,960 mcg/L [3]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 20-30 min [3]
Clearance
The clearance of drug is 24-75 L/h [3]
Elimination
0.003% of drug is excreted from urine in the unchanged form, and >80% of drug is excreted from the urine as CNS7054 [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 37 - 53 minutes [3]
Metabolism
The drug is metabolized via the hepatic cytochrome P450 enzymes [3]
Vd
The volume of distribution (Vd) of drug is 0.76 - 0.98 L/kg [3]
Chemical Identifiers
Formula
C21H19BrN4O2
IUPAC Name
methyl 3-[(4S)-8-bromo-1-methyl-6-pyridin-2-yl-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
Canonical SMILES
CC1=CN=C2N1C3=C(C=C(C=C3)Br)C(=N[C@H]2CCC(=O)OC)C4=CC=CC=N4
InChI
InChI=1S/C21H19BrN4O2/c1-13-12-24-21-17(7-9-19(27)28-2)25-20(16-5-3-4-10-23-16)15-11-14(22)6-8-18(15)26(13)21/h3-6,8,10-12,17H,7,9H2,1-2H3/t17-/m0/s1
InChIKey
CYHWMBVXXDIZNZ-KRWDZBQOSA-N
Cross-matching ID
PubChem CID
9867812
CAS Number
308242-62-8
DrugBank ID
DB12404
TTD ID
D0L5KU
ACDINA ID
D01382
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

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 Agonist [1]
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
Hydrochloric acid E00015 313 Acidulant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Sodium hydroxide E00234 14798 Alkalizing agent
Dextran E00466 4125253 Lyophilization aid
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Remimazolam 20 mg For Injection 20 mg For Injection Intravenous
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 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: 8442).
3 FDA Approved Drug Products: Byfavo (remimazolam) for intravenous injection