setmelanotide

REMS

Chronic weight management in patients with syndromic or monogenic obesity due to pro-opiomelanocortin (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.
Chronic weight management in patients with syndromic or monogenic obesity due to Bardet-Biedl syndrome (BBS).

Action ⬆ ⬇

Stimulates melanocortin 4 (MC4) receptors in the CNS to reduce hunger and increase energy expenditure. Patients with obesity due to POMC, PCSK1, or LEPR deficiency or BBS have insufficient inactivation of the MC4 receptor, which normally regulates hunger, satiety, and energy expenditure.

Therapeutic effects:

Reduction in body weight and hunger.

Pharmacokinetics ⬆ ⬇

Absorption: Unknown.

Distribution: Distributed to extravascular tissues.

Metabolism/Excretion: Metabolized into small peptides by catabolic pathways. 39% excreted into urine as unchanged drug.

Half-Life: 11 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
SUBQ	unknown	8 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Serious hypersensitivity;
End-stage renal disease;
OB: Pregnancy (weight loss medications not recommended during pregnancy);
Lactation: Lactation.

Use Cautiously in:

Depression;
Severe renal impairment (patients ≥12 yr only);
Pedi: Children <2 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia, dry skin, rash, skin hyperpigmentation

EENT: upper respiratory tract infection

GI: abdominal pain, constipation, diarrhea, dry mouth, nausea, vomiting

GU: ↑sexual arousal, spontaneous erection

Local: injection site reactions

MS: arthralgia, muscle spasm

Neuro: depression, dizziness, fatigue, headache, insomnia, suicidal thoughts, vertigo

Misc: chills, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

None reported.

Route/Dosage ⬆ ⬇

SC (Adults and Children ≥12 yr): 2 mg once daily for 2 wk. If initial dose tolerated, ↑ to 3 mg once daily; if 3 mg once daily dose not tolerated, return to 2 mg once daily. If 2 mg once daily initial regimen not tolerated, ↓ to 1 mg once daily (if tolerated for ≥1 wk, ↑ to 2 mg once daily).
SC (Children 6–<12 yr): 1 mg once daily for 2 wk. If initial dose tolerated, ↑ to 2 mg once daily. If 2 mg once daily dose tolerated, ↑ to 3 mg once daily. If 2 mg once daily dose not tolerated, ↓ to 1 mg once daily. If 1 mg once daily initial regimen not tolerated, ↓ to 0.5 mg once daily (if tolerated for ≥1 wk, ↑ to 1 mg once daily).
SC (Children 2–<6 yr and ≥40 kg): 0.5 mg once daily for 2 wk. If initial dose tolerated, ↑ to 1 mg once daily for 2 wk; then ↑ to 1.5 mg once daily for 2 wk; then ↑ to 2 mg once daily. If 0.5 mg once daily initial regimen not tolerated, discontinue setmelanotide.
SC (Children 2–<6 yr and 30–<40 kg): 0.5 mg once daily for 2 wk. If initial dose tolerated, ↑ to 1 mg once daily for 2 wk; then ↑ to 1.5 mg once daily. If 0.5 mg once daily initial regimen not tolerated, discontinue setmelanotide.
SC (Children 2–<6 yr and 20–<30 kg): 0.5 mg once daily for 2 wk. If initial dose tolerated, ↑ to 1 mg once daily. If 0.5 mg once daily initial regimen not tolerated, discontinue setmelanotide.
SC (Children 2–<6 yr and 15–<20 kg): 0.5 mg once daily. If initial dose not tolerated, discontinue setmelanotide.

Renal Impairment

SC (Adults and Children ≥12 yr): CCr 15–29 mL/min/1.73 m²: 0.5 mg once daily for 2 wk. If initial dose tolerated, ↑ to 1 mg once daily. If 1 mg once daily dose tolerated for ≥1 wk, ↑ to 1.5 mg once daily. If 0.5 mg once daily initial regimen not tolerated, discontinue therapy.

Renal Impairment

SC (Children 6–<12 yr): CCr 15–29 mL/min/1.73 m²: 0.5 mg once daily for 2 wk. If initial dose tolerated, ↑ to 1 mg once daily. If 0.5 mg once daily initial regimen not tolerated, discontinue therapy.

Renal Impairment

SC (Children 2–<6 yr and ≥30 kg): CCr 15–29 mL/min/1.73 m²: 0.5 mg once daily for 2 wk. If initial dose tolerated, ↑ to 1 mg once daily. If 0.5 mg once daily initial regimen not tolerated, discontinue therapy.

Renal Impairment

SC (Children 2–<6 yr and 20–<30 kg): CCr 15–29 mL/min/1.73 m²: 0.5 mg once daily. If initial dose not tolerated, discontinue therapy.

Availability ⬆ ⬇

Solution for injection: 10 mg/mL

Assessment ⬆ ⬇

Monitor weight at baseline and response to therapy periodically. POMC, PCSK1, or LEPR deficiency: Evaluate weight loss after 12–16 wk of treatment. Bardet-Biedl syndrome: Evaluate weight loss after 1 yr of treatment.
Monitor for depression, suicidal ideation or behavior, or any unusual changes in mood or behavior. Consider discontinuation in patients who experience suicidal thoughts or behaviors or if clinically significant or persistent depression symptoms occur.
Monitor for signs and symptoms of hypersensitivity reactions (rash, urticaria, pruritus, flushing, dizziness, vomiting, abdominal pain) and angioedema (swelling of throat, lips, tongue, or face; dyspnea; wheezing; hoarseness). Discontinue immediately and provide supportive care.
Provide full body skin examination and monitor for ↑ skin pigmentation and darkening of pre-existing nevi; effect is reversible upon discontinuation.
Monitor for sexual adverse reactions, including spontaneous penile erections or priapism; medical attention may be necessary.
Pedi: Monitor the impact of weight loss on growth and maturation.

Lab Test Considerations:

Verify negative pregnancy test before starting therapy.
Monitor renal function at baseline.

Implementation ⬆ ⬇

SC: Administer at the beginning of the day. Remove from the refrigerator approximately 15 min prior to administration. Alternatively, warm prior to administration by rolling the vial gently between the palms of the hands for 60 sec. Solution should appear clear to slightly opalescent, colorless to slightly yellow. Do not use if particulate matter or discoloration is seen. After removal from refrigeration, unopened or opened vials may be kept at temperatures ranging from refrigerated to room temperature for up to 30 days. Use a 1-mL syringe with a 28- or 29-gauge needle to inject SUBQ into the abdomen, thigh, or arm, rotating to a different site each day.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of setmelanotide. Teach patient and/or caregiver proper technique and placement of injections. Advise patient to read Patient Information before starting therapy.
Advise patient and caregiver report symptoms of depression, suicidal ideation, or adverse behavioral or psychiatric reactions.
Instruct patient and caregiver that ↑ skin pigmentation and darkening of preexisting nevi may occur and to have full body skin examinations during treatment.
Advise men to report and seek treatment for spontaneous penile erection that lasts >4 hr.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆