Setmelanotide

Setmelanotide is a prescription medication indicated for long-term weight management in patients with obesity owing to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), leptin receptor (LEPR) deficiency, or Bardet-Biedl syndrome (BBS).

• Setmelanotide is available under the following different brand names: Imcivree

Common side effects of Setmelanotide include:

• injection site reactions
• skin hyperpigmentation
• nausea
• headache
• diarrhea
• abdominal pain
• back pain
• fatigue
• vomiting
• depression
• upper respiratory tract infection
• spontaneous penile erection

Serious side effects of Setmelanotide include:

• hives
• difficult breathing 
• swelling of the face, lips, tongue, or throat
• unexpected erections or erections that occur too often or that last longer than 4 hours
• increased sexual desire in women

Rare side effects of Setmelanotide include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, light-headedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Injection, solution

• 10 mg/mL (1-mL multidose vial)

Obesity

Adult dosage

• Starting dose: 2 mg SC once a day for 2 weeks
• 2 mg once a day not tolerated: Reduce to 1 mg SC once a day; if 1 mg once a day is tolerated and additional weight loss is desired, titrate to 2 mg once a day
• 2 mg once a day tolerated for 2 weeks: Increase to 3 mg SC once a day; if the 3 mg dose is not tolerated, decrease to 2 mg once a day

Pediatric dosage

• Children younger than 6 years: Safety and efficacy not established
• Children aged 6-11 years
• Starting dose: 1 mg SC once a day for 2 weeks
  • 1 mg once a day not tolerated: Reduce to 0.5 mg SC once a day; if 0.5 mg once a day tolerated for at least 1 week, titrate to 1 mg once a day
  • 1 mg once a day tolerated for 2 weeks: Increase to 2 mg SC once a day; if the 2 mg dose is tolerated, increase to 3 mg once a day
  • If a 2-mg dose is NOT tolerated, decrease to 1 mg once a day
• Children aged 12 years and older
  • Starting dose: 2 mg SC once a day for 2 weeks
  • 2 mg once a day not tolerated: Reduce to 1 mg SC once a day; if 1 mg once a day is tolerated and additional weight loss is desired, titrate to 2 mg once a day
  • 2 mg once a day tolerated and additional weight loss desired: Increase to 3 mg SC once a day; if not tolerated, maintain dose at 2 mg once a day

Dosage Considerations – Should be Given as Follows:

• See "Dosages"

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Setmelanotide has no noted severe interactions with any other drugs.
• Setmelanotide has no noted serious interactions with any other drugs.
• Setmelanotide has no noted moderate interactions with any other drugs.
• Setmelanotide has no noted minor interactions with any other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Setmelanotide?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Setmelanotide?”

Cautions

• Sexual adverse reactions reported; spontaneous penile erections in men and sexual adverse reactions in women occurred in clinical studies; advise patients who have an erection lasting more than 4 hours to seek emergency medical attention
• May cause generalized increased skin pigmentation and darkening of preexisting nevi owing to pharmacologic effects; reversible upon discontinuation; perform a full body skin examination before initiating and periodically during treatment
• Contains benzyl alcohol; not approved for use in neonates or infants; serious adverse reactions including fatal reactions and gasping syndrome reported in premature neonates and low-birth-weight infants who received drugs containing benzyl alcohol as a preservative
• Some drugs that target the central nervous system may cause depression or suicidal ideation; patients with a history of depression or suicidal ideation may be at an increased risk for recurrent episodes while taking this medication; monitor patients for new-onset or worsening of depression, suicidal thoughts, or behavior or any unusual changes in mood or behavior; consider discontinuing if the patient experiences suicidal thoughts or behaviors or if clinically significant or persistent depression symptoms occur and periodically during treatment to monitor preexisting and new skin pigmentary lesions
• Drug interaction overview
  • Setmelanotide has a low potential for pharmacokinetic drug-drug interactions related to CYP450 enzymes, transporters, and plasma protein binding

Pregnancy and Lactation

• Discontinue when pregnancy is recognized unless the benefits of therapy outweigh potential fetal risks
• Data are unavailable regarding use in pregnant women to inform a drug-associated risk for major birth defects and miscarriage or adverse maternal or fetal outcomes
• For the general US population, weight loss offers no potential benefit to pregnant women and may result in fetal harm
• Clinical considerations
• Maternal obesity increases the risk for congenital malformations, including neural tube defects, cardiac malformations, oral clefts, and limb reduction defects
• Additionally, weight loss during pregnancy may result in fetal harm, including increased risk for small for gestational age
• Appropriate weight gain based on prepregnancy weight is currently recommended for all pregnant women, including those who are already overweight or obese, owing to the obligatory weight gain that occurs in maternal tissues during pregnancy
• Lactation
  • Not recommended for use while breastfeeding
  • Data are unavailable regarding the presence in human milk, effects on breastfed infants, or effects on milk production
  • Setmelanotide is present in the milk of rats; when a drug is present in rat milk, it will likely be present in human milk
  • Additionally, setmelanotide contains the preservative benzyl alcohol; benzyl alcohol is rapidly metabolized by lactating women, and benzyl alcohol exposure in the breastfed infant is unlikely (benzyl alcohol toxicity in premature neonates and low-weight infants reported in neonatal intensive care unit)