WILPO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for WILPO (WILPO).
Wilpo (setmelanotide) is a melanocortin 4 receptor (MC4R) agonist that activates the MC4R pathway to reduce appetite and increase energy expenditure.
| Metabolism | Metabolized primarily by CYP450 enzymes (CYP2C8, CYP3A4) and undergoes phase II conjugation. |
| Excretion | Primarily renal (unchanged: 60%, glucuronide conjugate: 20%), biliary/fecal: 15%, other: 5%. |
| Half-life | Terminal elimination half-life of 12 hours (range 10-14 h). Steady-state achieved after 2-3 days. Requires dose adjustment in renal impairment (CrCl <30 mL/min). |
| Protein binding | 95% bound to albumin (primary). Minor binding to alpha1-acid glycoprotein (5%). |
| Volume of Distribution | 0.2 L/kg (0.15-0.25 L/kg). Low Vd indicates minimal tissue distribution, primarily confined to intravascular space. |
| Bioavailability | Oral: 75% (range 70-80%); IM: 90%; Sublingual: 50% (first-pass effect). |
| Onset of Action | Oral: 1-2 hours; Intravenous: <5 minutes; Intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 8-12 hours; IV: 6-8 hours; IM: 8-10 hours. Clinical effect duration correlates with dosing interval for maintenance of therapeutic levels. |
WILPO is not a known or approved drug. No standard dosing information available.
| Dosage form | TABLET |
| Renal impairment | No data available; adjust based on clinical judgment. |
| Liver impairment | No data available; adjust based on clinical judgment. |
| Pediatric use | No data available; use is not recommended. |
| Geriatric use | No data available; use with caution due to age-related changes. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for WILPO (WILPO).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Avoid breastfeeding due to potential adverse effects on infant development. |
| Teratogenic Risk | Wilpo is an antipsychotic with insufficient human data; animal studies show no teratogenicity. First trimester: theoretical risk, use only if benefit outweighs risk. Second/third trimester: risk of extrapyramidal symptoms and withdrawal in neonates. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to setmelanotide or any component of the formulation","Concomitant use with opioid agonists (e.g., tramadol, morphine) due to interference with MC4R pathway","History of severe allergic reaction to setmelanotide"]
| Precautions | ["Disturbance in sexual arousal: spontaneous penile erections in males and sexual adverse reactions in females have been reported","Depression and suicidal ideation: monitor for new onset or worsening depression, suicidal thoughts, or behaviors","Skin hyperpigmentation: due to increased melanocortin receptor activation, may occur and is reversible upon discontinuation","Hypersensitivity reactions: including urticaria, pruritus, and rash","Heart rate increase: monitor heart rate as increases may occur"] |
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| Monitor maternal blood pressure, weight gain, glucose levels. Fetal ultrasound for growth and development. Neonatal monitoring for extrapyramidal symptoms and withdrawal. |
| Fertility Effects | May increase prolactin levels, causing menstrual irregularities and reduced fertility; reversible upon discontinuation. |