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

Stem definitionDrug idCAS RN
peptides and glycopeptides 5416 920014-72-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • setmelanotide
  • setmelanotide hydrochloride
  • setmelanotide acetate
  • imcivree
  • RM-493
Setmelanotide is an 8 amino acid cyclic peptide analog of endogenous melanocortin peptide alpha-MSH (alpha-melanocyte stimulating hormone). It is a melanocortin 4 (MC4) receptor agonist, with 20-fold less activity at the melanocortin 3 (MC3) and melanocortin 1 (MC1) receptors.
  • Molecular weight: 1117.32
  • Formula: C49H68N18O9S2
  • CLOGP: -2.65
  • LIPINSKI: 3
  • HAC: 27
  • HDO: 15
  • TPSA: 444.16
  • ALOGS: -4.59
  • ROTB: 18

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 19, 2018 EMA Rhythm Pharmaceuticals Limited
Nov. 25, 2020 FDA RHYTHM PHARMACEUTICALS INC

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 A08AA12 ALIMENTARY TRACT AND METABOLISM
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
Centrally acting antiobesity products
FDA EPC N0000193940 Melanocortin 4 Receptor Agonist
FDA MoA N0000193941 Melanocortin 4 Receptor Agonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Obesity indication 414916001 DOID:9970
Pro-opiomelanocortin (POMC) deficiency indication 702949005
Leptin receptor (LEPR) deficiency indication 785722006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG/ML BASE (EQ 10MG/ML BASE) IMCIVREE RHYTHM N213793 Nov. 25, 2020 RX SOLUTION SUBCUTANEOUS Nov. 25, 2025 NEW CHEMICAL ENTITY
EQ 10MG/ML BASE (EQ 10MG/ML BASE) IMCIVREE RHYTHM N213793 Nov. 25, 2020 RX SOLUTION SUBCUTANEOUS Nov. 25, 2027 INDICATED FOR CHRONIC WEIGHT MANAGEMENT IN ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH OBESITY DUE TO PROOPIOMELANOCORTIN (POMC), PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 1 (PCSK1), OR LEPTIN RECEPTOR (LEPR) DEFICIENCY CONFIRMED BY GENETIC TESTING DEMONSTRATING VARIANTS IN POMC, PCSK1, OR LEPR GENES THAT ARE INTERPRETED AS PATHOGENIC, LIKELY PATHOGENIC, OR OF UNCERTAIN SIGNIFICANCE (VUS)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Melanocortin receptor 4 GPCR AGONIST Kd 8.68 DRUG LABEL DRUG LABEL
Melanocortin receptor 5 GPCR AGONIST Ki 6.37 IUPHAR
Melanocortin receptor 3 GPCR AGONIST Ki 8 IUPHAR
Melanocyte-stimulating hormone receptor GPCR AGONIST Ki 8.41 IUPHAR
Melanocortin receptor 4 GPCR AGONIST Ki 8.57 IUPHAR

External reference:

IDSource
D11927 KEGG_DRUG
N7T15V1FUY UNII
C4279595 UMLSCUI
CHEMBL3301624 ChEMBL_ID
11993702 PUBCHEM_CID
DB11700 DRUGBANK_ID
CHEMBL4594386 ChEMBL_ID
CHEMBL4650273 ChEMBL_ID
9272 IUPHAR_LIGAND_ID
2469247 RXNORM
39054 MMSL
d09689 MMSL
1137634006 SNOMEDCT_US
1137658005 SNOMEDCT_US
1137662004 SNOMEDCT_US
018576 NDDF
018577 NDDF
C579663 MESH_SUPPLEMENTAL_RECORD_UI
10011 INN_ID
2324799-41-7 SECONDARY_CAS_RN
1504602-49-6 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Imcivree HUMAN PRESCRIPTION DRUG LABEL 1 72829-010 SOLUTION 10 mg SUBCUTANEOUS NDA 26 sections
Imcivree HUMAN PRESCRIPTION DRUG LABEL 1 72829-010 SOLUTION 10 mg SUBCUTANEOUS NDA 26 sections