Formulary
Setmelanotide: Indications, Dosing, Side Effects and Interactions
Setmelanotide is a centrally-acting selective melanocortin-4 receptor agonist that regulates hunger, satiety, and energy expenditure, thereby promoting weight...
MedNext Academy | 4 min read
Setmelanotide: Indications, Dosing, Side Effects and Interactions
Setmelanotide is a centrally-acting selective melanocortin-4 receptor agonist that regulates hunger, satiety, and energy expenditure, thereby promoting weight...
Drug action
Setmelanotide is a centrally-acting selective melanocortin-4 receptor agonist that regulates hunger, satiety, and energy expenditure, thereby promoting weight loss.
Indications and dose
**Obesity with underlying genetic aetiology [pro-opiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor (LEPR) deficiency] (under expert supervision)**
- **Adult** (By Subcutaneous Injection): 1 mg once daily for 2 weeks, to be administered in the morning, then increased if tolerated to 2 mg once daily, to be administered in the morning; increased if necessary to 2.5 mg once daily, to be administered in the morning, then increased if necessary up to 3 mg once daily, to be administered in the morning.
**Obesity with underlying genetic aetiology [Bardet-Biedl syndrome (BBS)] (under expert supervision)**
- **Adult** (By Subcutaneous Injection): 2 mg once daily for 2 weeks, to be administered in the morning, if not tolerated, reduce dose to 1 mg once daily; then if tolerated, increase dose to 2 mg once daily, then increased if tolerated to 3 mg once daily, to be administered in the morning.
**Obesity with underlying genetic aetiology [pro-opiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor (LEPR) deficiency] (under expert supervision) for setmelanotide**
- **Child 6-11 years** (By subcutaneous injection): 0.5 mg once daily for 2 weeks, to be administered in the morning, then increased if tolerated to 1 mg once daily for 2 weeks, to be administered in the morning; increased if tolerated to 2 mg once daily, to be administered in the morning, then increased if necessary up to 2.5 mg once daily, to be administered in the morning.
- **Child 12-17 years** (By subcutaneous injection): 1 mg once daily for 2 weeks, to be administered in the morning, then increased if tolerated to 2 mg once daily, to be administered in the morning; increased if necessary to 2.5 mg once daily, to be administered in the morning, then increased if necessary up to 3 mg once daily, to be administered in the morning.
**Obesity with underlying genetic aetiology [Bardet-Biedl syndrome (BBS)] (under expert supervision) for setmelanotide**
- **Child 6-15 years** (By subcutaneous injection): 1 mg once daily for 1 week, to be administered in the morning, if not tolerated, reduce dose to 0.5 mg once daily; then if tolerated, increase dose to 1 mg once daily, then increased if tolerated to 2 mg once daily for 1 week, to be administered in the morning, then increased if tolerated to 3 mg once daily, to be administered in the morning.
- **Child 16-17 years** (By subcutaneous injection): 2 mg once daily for 2 weeks, to be administered in the morning, if not tolerated, reduce dose to 1 mg once daily; then if tolerated, increase dose to 2 mg once daily, then increased if tolerated to 3 mg once daily, to be administered in the morning.
Cautions
Contains benzyl alcohol as an excipient (risk of allergic reactions, and of metabolic acidosis due to accumulation over time)
Side effects
Common or very common Alopecia; asthenia; constipation; depression; diarrhoea; dizziness; dry mouth; gastrointestinal discomfort; headaches; hot flush; hyperhidrosis; muscle complaints; nausea; neoplasms; pain; sexual dysfunction; skin reactions; sleep disorders; vertigo; vomiting Uncommon Altered smell sensation; anxiety; arthralgia; chest pain; chills; cough; drowsiness; eye naevus; gastrointestinal disorders; genital abnormalities; genital disorder female; hair colour changes; hyperaesthesia; jaundice ocular; mood altered; nail discolouration; nail disorder; oral disorders; rhinorrhoea; scleral discolouration; taste altered; temperature sensation altered; yawning Frequency not known Hyperpigmentation disorders; tongue discolouration
Interactions
**Other interactions (1):**
- In vitro studies showed that setmelanotide has low potential for pharmacokinetic interactions related to cytochrome P450 (CYP) transporters and plasma protein binding.
Pregnancy
No evidence of teratogenicity in animal studies, but lack of information in pregnant women. M Avoid initiation during pregnancy-weight loss during pregnancy may cause fetal harm. M If pregnancy occurs during treatment in a patient who is still losing weight, consider reducing dose or discontinuing treatment. M If pregnancy occurs during treatment in a patient who has reached a stable weight, consider continuing treatment. M Monitoring in pregnancy Monitor weight against recommended weight gain if treatment is continued during pregnancy. M
Breast feeding
Avoid-present in milk in animal studies. M
Hepatic impairment
Avoid (no information available). M
Renal impairment
Avoid in end-stage renal disease (no information available). M Dose adjustments Start with reduced dose in severe impairment (risk of increased exposure-consult product literature). M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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