metreleptin 🐶 Veterinary Use | 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 179.96 37.94 50 1034 30407 63457531
Blood glucose increased 112.52 37.94 45 1039 83711 63404227
Product dose omission issue 63.83 37.94 43 1041 234270 63253668
Blood triglycerides increased 57.78 37.94 17 1067 12471 63475467
Blood glucose decreased 49.13 37.94 17 1067 20935 63467003
Hypertriglyceridaemia 44.83 37.94 12 1072 6247 63481691
Pancreatitis 44.47 37.94 20 1064 49035 63438903
Hyperphagia 42.29 37.94 9 1075 1770 63486168
Pancreatitis acute 41.23 37.94 16 1068 27150 63460788

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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 123.43 41.12 35 795 37527 79706031
Blood glucose increased 61.91 41.12 28 802 114947 79628611
Pancreatitis 57.89 41.12 23 807 68552 79675006
Pancreatitis acute 50.23 41.12 19 811 49585 79693973
Insulin resistance 49.03 41.12 9 821 1370 79742188
Hypertriglyceridaemia 46.84 41.12 13 817 12727 79730831
Blood triglycerides increased 44.54 41.12 14 816 21026 79722532

FDA Adverse Event Reporting System (Pediatric)

None

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

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




🐶 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)

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

Pharmaceutical products:

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