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

Stem definition	Drug id	CAS RN
leptin derivatives	4826	186018-45-1

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
July 29, 2018	EMA	AEGERION PHARMACEUTICALS B.V.
Feb. 24, 2014	FDA	AMYLIN PHARMS LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Leptin receptor	Membrane receptor	P48357	LEPR_HUMAN	AGONIST				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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