Short answer: Setmelanotide has a half-life of about 11 hours. Levels peak median 8 hours after a dose. People vary, so treat these as estimates.
Setmelanotide is a peptide that switches on the MC4R receptor, part of the brain pathway that controls hunger. It is sold as Imcivree, a once-daily injection under the skin for rare forms of obesity caused by damage to that pathway. The label says it is not expected to work for general obesity.
Also known as: Imcivree.
Imcivree is a 10 mg/mL solution in a 1 mL multiple-dose vial, drawn up with a 1 mL syringe and a 28- or 29-gauge needle.
The Imcivree label approves setmelanotide to reduce excess weight and keep it off long term in people 4 and older with acquired hypothalamic obesity, and in people 2 and older with obesity due to Bardet-Biedl syndrome or to POMC, PCSK1 or LEPR deficiency confirmed by genetic testing. Label dosing: once a day at the start of the day, without regard to meals, into the belly, thigh or arm, using a different site each day. For acquired hypothalamic obesity it starts at 0.5 mg and rises every 2 weeks to 3 mg. For Bardet-Biedl syndrome or the gene deficiencies it starts at 2 mg at ages 12 and up or 1 mg at ages 6 to 11, with a 3 mg maintenance dose; under age 6 the dose depends on weight.
The label has no boxed warning. It warns about spontaneous erections (one lasting more than 4 hours needs emergency care), depression and suicidal thoughts, serious allergic reactions, and skin darkening with darker or new moles (a full skin exam is done before starting and from time to time). In acquired hypothalamic obesity it also warns about adrenal insufficiency and sodium imbalance. In that trial, skin darkening affected 58% vs 10% on placebo, nausea 55% vs 25% and vomiting 38% vs 19%. See Imcivree side effects, Imcivree dosing schedule, missed Imcivree dose and how to store Imcivree.
The Imcivree label says setmelanotide peaks at a median of 8 hours after an injection under the skin and has an effective elimination half-life of about 11 hours. Steady state is reached within 2 days of daily dosing, with about 30% build-up. About 39% of a 3 mg dose leaves unchanged in the urine over 24 hours.
Numbers shown are taken from the source above. Half-life varies from person to person.
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