Setmelanotide
Also known as: BIM-22493, Imcivree, RM-493, RM‑493, Setmelanotide
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Summary
Setmelanotide is a synthetic cyclic peptide MC4R agonist indicated for chronic weight management in patients with obesity due to certain genetic deficiencies (e.g., POMC, PCSK1, LEPR).
Mechanism of Action
Selective agonist of the melanocortin‑4 receptor (MC4R) leading to reduced appetite and increased energy expenditure
Routes of Administration
Goals & Uses
- Weight management in PCSK1 deficiency obesityObesity TreatmentHigh
- Investigational use in other MC4R pathway deficienciesMetabolic / ObesityModerate
- Weight reduction in Bardet-Biedl syndromeMetabolic / ObesityHigh
- Weight management in POMC deficiency obesityObesity TreatmentHigh
- Hyperphagia reductionMetabolic / Appetite ControlHigh
- Weight reduction in POMC/PCSK1/LEPR deficiency obesityMetabolic / ObesityHigh
- Weight management in LEPR deficiency obesityObesity TreatmentHigh
Contraindications
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- Hypersensitivity to setmelanotide or excipientsAllergyHigh
- Hypersensitivity to setmelanotideAllergicHigh
- Use in obesity not caused by POMC/PCSK1/LEPR deficiency or BBSOff Label UseModerate
Adverse Effects
- Depression/suicidal ideationPsychiatricUncommon
- Injection site reactionsLocalCommon
- Sexual adverse reactionsSexual/ReproductiveUncommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Skin hyperpigmentationDermatologicCommon
- Spontaneous penile erectionsSexual/ReproductiveCommon
- HyperpigmentationDermatologicCommon
- DiarrheaGastrointestinalUncommonLoose or frequent stools
Drug Interactions
- Medications affecting glucose homeostasisLow
- Other melanocortin receptor agonistsModerate
- Serotonergic agents (e.g., SSRIs)Low
- OpioidsLow
Population Constraints
- PregnancyReproductive SafetyRelative
- Children under 6 yearsPediatricAbsolute
- Children under 2 yearsPediatricAbsolute
- Severe hepatic impairmentOrgan ImpairmentRelative
- Renal impairment (severe)RenalRelative
Regulatory Status
- European UnionApprovedApproved: Obesity due to POMC deficiency, Obesity due to PCSK1 deficiency, Obesity due to LEPR deficiencyEMA approval 2021.
- United StatesApprovedApproved: Obesity due to POMC deficiency, Obesity due to PCSK1 deficiency, Obesity due to LEPR deficiencyApproved 2020 as Imcivree.
- United KingdomApprovedApproved: Obesity due to POMC deficiency, Obesity due to PCSK1 deficiency, Obesity due to LEPR deficiencyApproved via MHRA 2021.
FDA‑approved (2020) as Imcivree; EMA‑approved (2021) for the same genetic obesity indications.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Setmelanotide?
Setmelanotide is a synthetic cyclic peptide MC4R agonist indicated for chronic weight management in patients with obesity due to certain genetic deficiencies (e.g., POMC, PCSK1, LEPR).
What is Setmelanotide used for?
Setmelanotide is educationally associated with: Weight management in PCSK1 deficiency obesity, Investigational use in other MC4R pathway deficiencies, Weight reduction in Bardet-Biedl syndrome, Weight management in POMC deficiency obesity, Hyperphagia reduction, Weight reduction in POMC/PCSK1/LEPR deficiency obesity, Weight management in LEPR deficiency obesity. Educational only — not medical advice.
How is Setmelanotide administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Setmelanotide?
Reported adverse effects include: Depression/suicidal ideation, Injection site reactions, Sexual adverse reactions, Nausea, Skin hyperpigmentation, Spontaneous penile erections, Hyperpigmentation, Diarrhea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Setmelanotide?
Recorded contraindications: Pregnancy, Hypersensitivity to setmelanotide or excipients, Hypersensitivity to setmelanotide, Use in obesity not caused by POMC/PCSK1/LEPR deficiency or BBS. Consult a qualified clinician before use.