metreleptin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

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 176.77 40.42 49 1206 36312 90590880
Blood glucose increased 119.51 40.42 46 1209 95200 90531992
Blood triglycerides increased 92.48 40.42 24 1231 13737 90613455
Insulin resistance 74.16 40.42 13 1242 1145 90626047
Product dose omission issue 65.76 40.42 44 1211 291643 90335549
Hypertriglyceridaemia 64.00 40.42 16 1239 7873 90619319
Hyperphagia 62.62 40.42 13 1242 2805 90624387
Neutralising antibodies positive 59.14 40.42 9 1246 327 90626865
Glycosylated haemoglobin increased 53.23 40.42 16 1239 15546 90611646
Blood glucose decreased 50.74 40.42 17 1238 23412 90603780
Pancreatitis acute 45.49 40.42 17 1238 32098 90595094

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 118.81 40.45 34 930 44823 110543512
Insulin resistance 81.75 40.45 14 950 1720 110586615
Blood triglycerides increased 71.68 40.45 20 944 23906 110564429
Blood glucose increased 66.04 40.45 29 935 132467 110455868
Neutralising antibodies positive 62.02 40.45 9 955 379 110587956
Hypertriglyceridaemia 60.00 40.45 16 948 16138 110572197
Pancreatitis acute 53.51 40.45 20 944 60254 110528081
Pancreatitis 51.55 40.45 22 942 93511 110494824
Hyperphagia 47.92 40.45 10 954 3521 110584814

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
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:50779 appetite enhancer
CHEBI has role CHEBI:50864 insulin-sensitizing drug
CHEBI has role CHEBI:74518 anti-obesity agent

Related Drugs by ATC class:

A16AA Amino acids and derivatives 6 drugs
ademetioninebetainecarglumic acidglutaminelevocarnitinemercaptamine

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
CHEBI:752900 CHEBI
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 10122-210 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 11.30 mg SUBCUTANEOUS BLA 30 sections