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

Stem definitionDrug idCAS RN
leptin derivatives 4826 186018-45-1

Description:

MoleculeDescription

Synonyms:

  • metreleptin
  • myalept
  • r-metHuLeptin
  • methionyl human leptin
Metreleptin is a recombinant human leptin analog that exerts its function by binding to and activating the human leptin receptor (ObR), which belongs to the Class I cytokine family of receptors that signals through the JAK/STAT transduction pathway. Native leptin is a hormone predominantly secreted by adipose tissue that informs the central nervous system of the status of energy stores in the body. In patients with generalized lipodystrophy, leptin deficiency, resulting from the loss of adipose tissue, contributes to excess caloric intake, which exacerbates the metabolic abnormalities.
  • Molecular weight: 16155.67
  • Formula: C714H1167N191O221S6
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 6610.67
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 29, 2018 EMA AEGERION PHARMACEUTICALS B.V.
Feb. 24, 2014 FDA AMYLIN PHARMS LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Therapy cessation 174.83 43.15 50 963 26579 46658470
Blood glucose increased 108.72 43.15 45 968 71968 46613081
Product dose omission issue 80.23 43.15 48 965 168472 46516577
Blood triglycerides increased 50.56 43.15 16 997 11767 46673282
Blood glucose decreased 46.87 43.15 17 996 18875 46666174

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC A16AA07 ALIMENTARY TRACT AND METABOLISM
OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
Amino acids and derivatives
FDA Chemical/Ingredient N0000170333 Leptin
FDA Chemical/Ingredient N0000175452 Analogs/Derivatives
FDA EPC N0000190854 Leptin Analog

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acquired partial lipodystrophy indication 75659004
Acquired generalized lipodystrophy indication 86907008
Congenital generalized lipodystrophy indication 284449005

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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Leptin receptor Membrane receptor AGONIST DRUG LABEL DRUG LABEL

External reference:

IDSource
4033286 VUID
N0000190647 NUI
4033286 VANDF
C0961965 UMLSCUI
CHEMBL2107857 ChEMBL_ID
DB09046 DRUGBANK_ID
C415771 MESH_SUPPLEMENTAL_RECORD_UI
7333 IUPHAR_LIGAND_ID
7808 INN_ID
TL60C27RLH UNII
1491625 RXNORM
213104 MMSL
30187 MMSL
d08243 MMSL
015482 NDDF
703361000 SNOMEDCT_US
715594006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Myalept HUMAN PRESCRIPTION DRUG LABEL 1 76431-210 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 11.30 mg SUBCUTANEOUS BLA 30 sections