Pharm

Lenacapavir

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Lenacapavir, Yeztugo, Sunlenca

  • Contraindications
  1. HIV positive status (or status unknown)
  2. Body Weight <35 kg
  • Mechanism
  1. Long-acting HIV capsid inhibitor
  • Medications
  1. Lenacapavir Oral Tablet (Sunlenca): 300 mg
  2. Lenacapavir SQ Injection (Yeztugo): 463.5 mg/1.5 mL in single dose vial
  • Dosing
  1. Precautions
    1. Injection must be administered by a healthcare professional (not the patient)
  2. Start
    1. Day 0: TWO Lenacapavir SQ Injections (927 mg and 3 ml total)
    2. Day 1: Lenacapavir 600 mg (two tablets) orally once
    3. Day 2: Lenacapavir 600 mg (two tablets) orally once
  3. Maintain
    1. TWO Lenacapavir SQ Injections (927 mg and 3 ml total) every 6 months
    2. Injections must be 26 weeks apart (+/- 14 days)
    3. Bridge with Lenacapavir 300 mg orally once weekly if SQ Injection delay >14 days
    4. If delayed injection >14 days, repeat the starting protocol (see above)
  • Adverse Effects
  1. Nausea
  2. Headache
  3. Local injection skin reactions
    1. Local redness or swelling
    2. Subcutaneous Nodules
  • Drug Interactions
  1. P-Glycoprotein (P-gp) Substrate (and moderate inhibitor)
  2. CYP3A Substrate (and moderate inhibitor)
    1. Avoid with strong CYP3A Inducers (e.g. Carbamazepine, Phenobarbital)
  • Safety
  1. Unknown safety in pregnancy and Lactation
    1. Balance risk versus benefit when using Lenacapavir in these populations
  2. Monitoring
    1. HIV Antigen/Antibody testing
      1. Baseline before starting PrEP
      2. Every 6 months (at time of SQ Injection)
        1. Consider every 3 months if frequent exposure risk
  1. As effective (>99%) as other PrEP options (FTC/TAF or TDF, Cabotegravir)
  2. Costs $28,000/year (may be covered by ACA, or with manufacturer cost assistance)
  • References
  1. (2025) Presc Lett 32(9): 53