II. Indications

III. Contraindications

  1. HIV positive status (or status unknown)
  2. Body Weight <35 kg

IV. Mechanism

  1. Long-acting HIV capsid inhibitor

V. Medications

  1. Lenacapavir Oral Tablet (Sunlenca): 300 mg
  2. Lenacapavir SQ Injection (Yeztugo): 463.5 mg/1.5 mL in single dose vial

VI. 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)

VII. Adverse Effects

  1. Nausea
  2. Headache
  3. Local injection skin reactions
    1. Local redness or swelling
    2. Subcutaneous Nodules

VIII. 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)

IX. 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

X. Efficacy: HIV Preexposure Prophylaxis (PrEP)

  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)

XII. References

  1. (2025) Presc Lett 32(9): 53

Images: Related links to external sites (from Bing)