Setmelanotide

Class: Anorexigenic Agents, Miscellaneous
Chemical Name: (4R,7S,10S,13R,16S,19R,22R)-22-[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-13-benzyl-10-[3-(diaminomethylideneamino)propyl]-16-(1H-imidazol-5-ylmethyl)-7-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexazacyclotricosane-4-carboxamide
Molecular Formula: C₄₉H₆₈N₁₈O₉S₂
CAS Number: 920014-72-8
Brands: Imcivree

Medically reviewed by Drugs.com on Jan 11, 2021. Written by ASHP.

Introduction

Setmelanotide acetate, a melanocortin 4 (MC4) receptor agonist, is an anorexigenic agent.

Uses for Setmelanotide

Setmelanotide acetate has the following uses:

Setmelanotide acetate is 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).

Setmelanotide acetate has the following limitations of use:

Not indicated for obesity due to suspected POMC, PCSK1, or LEPR deficiency with POMC, PCSK1, or LEPR variants classified as benign or likely benign.

Not indicated for other types of obesity not related to POMC, PCSK1, or LEPR deficiency, including obesity associated with other genetic syndromes and general (polygenic) obesity.

Setmelanotide Dosage and Administration

General

Setmelanotide acetate is available in the following dosage form(s) and strength(s):

Injection: 10 mg/mL solution for subcutaneous use in a 1-mL multiple-dose vial.

Dosage

It isessentialthat the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

• Select patients for setmelanotide acetate treatment who have genetically confirmed or suspected deficiency of POMC, PCSK1, or LEPR.

• Treat patients with variants in POMC, PCSK1, or LEPR genes that are interpreted as pathogenic, likely pathogenic, or of uncertain significance in the clinical context of the patient.

• Periodically assess response to setmelanotide acetate. In pediatric patients, evaluate the impact of weight loss on growth and maturation.

• Evaluate weight loss after 12–16 weeks of treatment. If a patient has not lost at least 5% of baseline body weight or 5% of baseline BMI for those with continued growth potential, discontinue setmelanotide acetate since it is unlikely such patients will achieve and sustain clinically meaningful weight loss with continued treatment.

• See the Full Prescribing Information for administration instructions.

Pediatric Patients

Dosage and Administration in Pediatric Patients 6 to less than 12 Years of Age

• Starting dosage is 1 mg (0.1 mL) injected subcutaneously once daily ...