bremelanotide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5329 189691-06-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bremelanotide
  • bremelanotide acetate
  • vyleesi
  • PT-141
Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. The mechanism by which VYLEESI improves HSDD in women is unknown. The MC1R is expressed on melanocytes; binding at this receptor leads to melanin expression and increased pigmentation
  • Molecular weight: 1025.18
  • Formula: C50H68N14O10
  • CLOGP: 2.68
  • LIPINSKI: 3
  • HAC: 24
  • HDO: 13
  • TPSA: 378.97
  • ALOGS: -4.90
  • ROTB: 17

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 21, 2019 FDA AMAG PHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC G02CX05 GENITO URINARY SYSTEM AND SEX HORMONES
OTHER GYNECOLOGICALS
OTHER GYNECOLOGICALS
Other gynecologicals

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Lack or loss of sexual desire indication 270903007 DOID:13868
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of cardiovascular system contraindication 49601007 DOID:1287

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.28 acidic
pKa2 12.41 acidic
pKa3 12.76 acidic
pKa4 13.11 acidic
pKa5 13.39 acidic
pKa6 13.66 acidic
pKa7 8.36 Basic
pKa8 7.73 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) VYLEESI (AUTOINJECTOR) PALATIN TECHNOLOGIES N210557 June 21, 2019 RX SOLUTION SUBCUTANEOUS June 21, 2024 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Melanocortin receptor 4 GPCR AGONIST Kd 8 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Melanocyte-stimulating hormone receptor GPCR AGONIST DRUG LABEL
Melanocortin receptor 3 GPCR AGONIST DRUG LABEL
Melanocortin receptor 5 GPCR AGONIST DRUG LABEL
Adrenocorticotropic hormone receptor GPCR AGONIST DRUG LABEL

External reference:

IDSource
6Y24O4F92S UNII
1607799-13-2 SECONDARY_CAS_RN
4038620 VANDF
C1721339 UMLSCUI
CHEMBL2070241 ChEMBL_ID
CHEMBL4297533 ChEMBL_ID
DB11653 DRUGBANK_ID
D06569 KEGG_DRUG
8737 INN_ID
C476721 MESH_SUPPLEMENTAL_RECORD_UI
9941379 PUBCHEM_CID
10408 IUPHAR_LIGAND_ID
2176311 RXNORM
319387 MMSL
37138 MMSL
d09322 MMSL
018059 NDDF
018060 NDDF
427418003 SNOMEDCT_US
788500001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vyleesi HUMAN PRESCRIPTION DRUG LABEL 1 64011-701 INJECTION 1.75 mg SUBCUTANEOUS NDA 28 sections