Lenacapavir

FDA label

Read the full label on DailyMed ↗

Renal No adjustment needed (mild–severe, CrCl ≥15 mL/min); not studied in ESRD (CrCl <15) → Undefined there

Hepatic No adjustment needed (mild–moderate, Child-Pugh A/B); not studied in severe (Child-Pugh C) → Undefined there

Injection window ±2 weeks. If delay >2 weeks anticipated: bridge with 300 mg PO once every 7 days (interim, up to 6 months); resume injections within 7 days of last oral dose.

Instructions

• Confirm HIV-1 negative status before initiation, before every injection, and as clinically appropriate
• Tablets: with or without food
• Injection: SC only, into abdomen (thigh alternative), by healthcare provider; NEVER intradermal (risk of necrosis/ulcer); two 1.5 mL injections per dose
• Missed Day 2 oral dose: take ASAP; do not take Day 1 and Day 2 oral doses on the same day
• >28 weeks since last injection without interim tablets: restart initiation from Day 1 if clinically appropriate
• Supplemental lenacapavir doses required when initiating strong or moderate CYP3A inducers (strong inducers only ≥2 days after lenacapavir start)

Contraindications

• Unknown or positive HIV-1 status

Cautions

• Use as part of comprehensive HIV prevention strategy (adherence, safer sex practices); not always effective
• Resistance risk if HIV-1 acquired before, during, or after use — test before each injection; start complete HIV regimen immediately if positive
• Long-acting tail: residual drug up to ≥12 months after last injection; consider alternative PrEP within 28 weeks of last injection if discontinuing; moderate CYP3A inhibition persists up to 9 months
• Serious injection site reactions (necrosis, ulcer) with improper intradermal administration — SC only

Adverse reactions

• Injection site reactions (69–83%; nodules ~63–64%, median duration ~10–12 months; pain, induration, erythema)
• Headache
• Nausea

Pregnancy Trial data (PURPOSE 1) identified no drug-associated risk of miscarriage or adverse maternal/fetal outcomes; birth-defect rate within background; pregnancy registry (APR 1-800-258-4263); consider continuing PrEP in pregnancy given increased HIV transmission risk during acute infection.

Lactation Present in human milk (milk:plasma ~0.63); very low infant levels; no infant adverse effects observed — weigh benefits of breastfeeding, need for PrEP, and HIV transmission risk.