Pharm

Lorcaserin

search

Lorcaserin, Belviq, Belviq XR

  • Background
  1. Released in U.S. in 2013
  2. Removed from market February 2020 in U.S. due to cancer risk
    1. https://www.fda.gov/drugs/drug-safety-and-availability/fda-requests-withdrawal-weight-loss-drug-belviq-belviq-xr-lorcaserin-market
  • Efficacy
  1. Weight loss is 7 pounds more than Placebo in one year
  2. Weight loss of at least 5% in up to 47% of patients at one year
  • Mechanism
  1. Serotonin 2C (5HT-2C) agonist that increases satiety
  2. Active at pro-opiomelanocortin (POMC) Neurons of the Hypothalamus
  3. POMC is cleaved into a-Melanocyte stimulating hormone (MSH)
  4. MSH binds Hypothalamus melanocortin 4 receptors, resulting in decreased food intake
  5. Thomsen (2008) J Pharmacol Exp Ther 325(2): 577-87 [PubMed]
  • Dosing
  1. Lorcaserin (Belviq) 10 mg orally twice daily
  2. Belviq XR preparation available for once daily use in 2017
  3. Stop medication if 5% weight loss is not achieved at 12 weeks
  • Adverse Effects
  1. Cancer Risk
    1. https://www.fda.gov/drugs/drug-safety-and-availability/safety-clinical-trial-shows-possible-increased-risk-cancer-weight-loss-medicine-belviq-belviq-xr
  2. No associated valvulopathy
    1. Lorcaserin has 100 fold greater neurologic 5HT-2C affinity over cardiac valve 5HT-2B affinity
  3. Well tolerated
  4. More specific, and does not appear to carry same valvular heart disease risks as with fenfluramine
  5. Constipation
  6. Cough
  7. Dry Mouth
  8. Fatigue
  9. Nausea
  10. Hypoglycemia
  • Drug Interactions
  1. Serotonergic medications (e.g. SSRI, Dextromethorphan)
    1. Serotonin Syndrome risk