remimazolam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 5400 308242-62-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • remimazolam
  • remimazolam besylate
  • byfavo
  • CNS 7056
  • CNS 7056B
  • ONO-2745BS
  • ONO-2745
  • anerem
  • aptimyda
Remimazolam is a benzodiazepine and it binds to brain benzodiazepine sites (gamma amino butyric acid type A [GABAA] receptors), while its carboxylic acid metabolite (CNS7054) has a 300 times lower affinity for the receptor. Remimazolam, like other benzodiazepines, did not show clear selectivity between subtypes of the GABAA receptor.
  • Molecular weight: 439.31
  • Formula: C21H19BrN4O2
  • CLOGP: 2.81
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 69.37
  • ALOGS: -4.31
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 8.30 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
March 26, 2021 EMA PAION Netherlands B.V.
July 2, 2020 FDA ACACIA
Jan. 23, 2020 PMDA Anerem

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05CD14 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Sedation indication 72641008
Non-allergic hypersensitivity to dextran contraindication 609536007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 10472365 July 10, 2027 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 10961250 July 10, 2027 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 10052334 Nov. 7, 2031 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 10195210 Nov. 7, 2031 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 10342800 Nov. 7, 2031 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 10722522 Nov. 7, 2031 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 9737547 Nov. 7, 2031 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 9827251 Nov. 7, 2031 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS 9561236 April 30, 2033 USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 20MG BASE/VIAL BYFAVO ACACIA N212295 Oct. 6, 2020 RX POWDER INTRAVENOUS Oct. 6, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
GABA-A receptor; benzodiazepine binding site Ion channel MODULATOR Ki 7.53 SCIENTIFIC LITERATURE DRUG LABEL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel MODULATOR EC50 6.04 SCIENTIFIC LITERATURE
GABA-A receptor; alpha-1/beta-2/gamma-2 Ion channel MODULATOR EC50 6.44 SCIENTIFIC LITERATURE
GABA A receptor alpha-2/beta-2/gamma-2 Ion channel MODULATOR EC50 6.18 SCIENTIFIC LITERATURE
GABA A receptor alpha-5/beta-2/gamma-2 Ion channel MODULATOR EC50 5.86 SCIENTIFIC LITERATURE

External reference:

IDSource
D11788 KEGG_DRUG
7V4A8U16MB UNII
1001415-66-2 SECONDARY_CAS_RN
C3179470 UMLSCUI
CHEMBL4297526 ChEMBL_ID
9867812 PUBCHEM_CID
DB12404 DRUGBANK_ID
CHEMBL4594301 ChEMBL_ID
8442 IUPHAR_LIGAND_ID
018433 NDDF
018438 NDDF
926369003 SNOMEDCT_US
926383001 SNOMEDCT_US
926385008 SNOMEDCT_US
4039938 VANDF
2383941 RXNORM
336210 MMSL
38618 MMSL
d09651 MMSL
C522201 MESH_SUPPLEMENTAL_RECORD_UI
9232 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BYFAVO HUMAN PRESCRIPTION DRUG LABEL 1 71390-011 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2.50 mg INTRAVENOUS NDA 35 sections
BYFAVO HUMAN PRESCRIPTION DRUG LABEL 1 71390-011 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2.50 mg INTRAVENOUS NDA 35 sections