Lenacapavir
HIV capsid inhibitors
HIV capsid inhibitors
A long-acting HIV capsid inhibitor, given as tablets and then as an injection every six months, for treatment and to prevent HIV infection.
Quick facts
- Group
- HIV capsid inhibitors
- Target
- HIV-1 capsid protein (p24)
- Used for
- HIV-1 infection
- Key effects
- Injection-site swelling · Nausea · Headache
- Monitor
- HIV viral load · Injection sites
- ATC
- J05AX31
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows lenacapavir (then called GS-6207) bound to an HIV-1 capsid hexamer.
Lenacapavir binds a pocket between neighbouring subunits of the HIV-1 capsid protein. The capsid protects the viral genome until it reaches the nucleus and must be assembled again in every new virion; lenacapavir disturbs these capsid functions, including assembly of new capsids. Because no other antiretroviral acts on the capsid, it remains active against virus resistant to the other classes.
- The capsid shields the HIV genome
- Lenacapavir binds between capsid subunits
- Capsid function and assembly are disturbed
- New infectious virus is not formed
Indications
- HIV-1 infection, with other antiretrovirals, including virus resistant to other classes HIV infection and AIDS →
- Pre-exposure prophylaxis to reduce the risk of acquiring HIV, together with safer sex HIV infection and AIDS →
Adverse effects
Common
- Injection-site swelling, pain, redness, itching or lumps (nodules)
- Nausea
- Headache
Contraindications
- Hypersensitivity to lenacapavir
- Medicines listed as not to be combined, such as St John's wort
Key interactions
- St John's wort
- Lowers lenacapavir levels; avoided
- Many other medicines
- Doses or monitoring may change; the effect lasts months after the last injection
- Grapefruit
- Discussed with the care team during treatment
What is monitored
- HIV viral load (treatment) or regular HIV tests (prophylaxis)
- Injection sites
- New signs of infection early in treatment
Administration and safety
- Subcutaneous injection into the abdomen or thigh by a health professional, every six months
- Oral tablets start therapy or bridge a missed injection
- Late injections risk low levels and resistance: appointments are tracked closely
Pregnancy and breastfeeding
Human data are limited; benefit and risk are weighed with the HIV team.
Nursing care
- Confirm a negative HIV test before starting prophylaxis
- Record the date of each injection and schedule the next one
- Check the injection site and explain that lumps can persist
- Teach to tell every prescriber when the last injection was given
Pharmacokinetics
- Absorption
- Oral tablets start therapy; the subcutaneous injection forms a depot that releases the drug slowly
- Elimination
- Interactions can persist for up to nine months after the last injection
- Half-life
- Very long, so the injection is repeated only every six months
Test yourself
Think of the answer, then tap the question to see it.
What is the target of lenacapavir?
The HIV-1 capsid protein (p24).
How often is lenacapavir injected?
Every six months, under the skin.
Which two uses does lenacapavir have?
Treatment of HIV, including resistant virus (with other drugs), and pre-exposure prophylaxis.
Connections
← Back to the class: HIV capsid inhibitors
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Lenacapavir: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Lenacapavir Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Crystal structure of the HIV capsid hexamer bound to the small molecule long-acting inhibitor, GS-6207 (RCSB Protein Data Bank, 2020).
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Representative model, for educational purposes only.