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], [3]

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

439.3

Topological Polar Surface Area (xlogp)

3.4

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 452 mcgh/L [4]
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 189-6,960 mcg/L [4]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 20-30 min [4]
Clearance: The clearance of drug is 24-75 L/h [4]
Elimination: 0.003% of drug is excreted from urine in the unchanged form, and >80% of drug is excreted from the urine as CNS7054 [4]
Half-life: The concentration or amount of drug in body reduced by one-half in 37 - 53 minutes [4]
Metabolism: The drug is metabolized via the hepatic cytochrome P450 enzymes [4]
Vd: The volume of distribution (Vd) of drug is 0.76 - 0.98 L/kg [4]

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

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]

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Molecular Interaction Atlas (MIA)

MIA Detail

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
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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	ClinicalTrials.gov (NCT02523859) Study Evaluating the Efficacy and Safety of Remimazolam in General Anesthesia in Adult Patients Undergoing Cardiac Surgery.
4	FDA Approved Drug Products: Byfavo (remimazolam) for intravenous injection
5	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. (Target id: 415).
6	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8	Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
9	Prodynorphin gene deletion increased anxiety-like behaviours, impaired the anxiolytic effect of bromazepam and altered GABAA receptor subunits gene expression in the amygdala. J Psychopharmacol. 2011Jan;25(1):87-96.