Lenacapavir

Dosage Forms

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Tablet

300 mg

Injection

463.5 mg per 1.5 mL (309 mg/mL)

The complete injectable dose is 927 mg, administered as two 1.5 mL subcutaneous injections.

Uses

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HIV-1 pre-exposure prophylaxis (PrEP)
Reduction of the risk of sexually acquired HIV-1 infection
HIV prevention as part of a comprehensive combination prevention approach

Dose and Duration

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HIV-1 pre-exposure prophylaxis (PrEP)

By subcutaneous injection and oral administration

Adults and adolescents weighing at least 35 kg: Initiation on Day 1 consists of 927 mg by subcutaneous injection (two 1.5 mL injections) plus 600 mg orally (two 300 mg tablets). On Day 2, take 600 mg orally (two 300 mg tablets).

Continuation: 927 mg by subcutaneous injection every 6 months (26 weeks), with the scheduled injection administered within approximately ±2 weeks of the due date.

HIV-1 testing must be performed before initiation and before each subsequent injection, with additional testing when clinically appropriate.

If a scheduled injection is expected to be delayed by more than 2 weeks, oral lenacapavir 300 mg once every 7 days may be used temporarily until injections can resume.

Side Effects

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Injection-site reactions, pain, nodule, induration and erythema
Headache
Nausea
Diarrhoea

Contra-indications

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Known HIV-1 infection or unknown HIV-1 status
Positive HIV-1 test
Known hypersensitivity to lenacapavir or any component of the formulation
Concomitant use of certain strong CYP3A inducers may reduce lenacapavir concentrations and compromise its effectiveness

Pregnancy

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Pregnancy is not an absolute contraindication to HIV PrEP. Use if benefits outweigh the risks or based on the local guidelines.
Available pregnancy data for long-acting lenacapavir are limited; consult current product information and local HIV/PrEP guidelines.

Breast-feeding

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Use during breastfeeding should be considered according to current HIV PrEP guidelines and available safety data.
Consult current prescribing information and local guidance before use.

⚠️ Caution

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Confirm HIV-negative status before starting lenacapavir and before each subsequent injection.
Do not administer lenacapavir for PrEP to a person with HIV-1 infection or unknown HIV-1 status.
Carefully assess individuals with symptoms or signs suggestive of acute HIV-1 infection.
Adherence to the 6-month injection schedule is important because prolonged subtherapeutic drug concentrations may increase the risk of HIV infection and development of resistance.
Residual lenacapavir concentrations may remain in the body for 12 months or longer after discontinuation.
Review concomitant medicines for clinically important drug interactions, particularly CYP3A inducers.
Incorrect administration into the skin rather than the subcutaneous tissue can cause serious injection-site reactions.
Lenacapavir does not protect against other sexually transmitted infections; additional prevention measures may be required.

Efficacy

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Long-acting lenacapavir has demonstrated very high efficacy in preventing sexually acquired HIV-1 infection in clinical trials.
In PURPOSE 1, no HIV infections occurred among participants receiving twice-yearly lenacapavir during the primary analysis period.
WHO recommends twice-yearly injectable lenacapavir as an additional HIV prevention choice as part of combination HIV prevention.

Administration

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Administered by subcutaneous injection.
Two 1.5 mL injections are required to provide the 927 mg dose.
Administered every 6 months (26 weeks) after completion of the initial loading regimen.
Administration should be performed by a trained healthcare professional.

Important Information

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Lenacapavir is a capsid inhibitor, not an integrase inhibitor.
HIV testing is required before initiation and before subsequent injections.
The first dose requires both injections and oral tablets; the subsequent regimen consists of injections every 6 months.
Maintaining scheduled injections is important to maintain protective drug concentrations.