HIV-1 infection

Active Ingredient: Lenacapavir

Indication for Lenacapavir

Population group: only adolescents (12 years - 18 years old) , adults (18 years old or older)
Therapeutic intent: Preventive action

Lenacapavir is indicated in combination with safer sex practices for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in adults and adolescents with increased HIV-1 acquisition risk, weighing at least 35 kg.

For this indication, competent medicine agencies globally authorize below treatments:

927 mg subcutaneously and 600 mg orally on Day 1, 600 mg orally on Day 2, and thereafter 927 mg subcutaneously every 6 months

For:

Dosage regimens

In case that patient weight is ≥ 35 kg

Subcutaneous, 927 milligrams lenacapavir, one dose, over the duration of 1 day. Afterwards, oral, 600 milligrams lenacapavir, one dose. Afterwards, subcutaneous, 927 milligrams lenacapavir, once every 6 months.

Detailed description

The dosing schedule in adults and adolescents weighing at least 35 kg consists of a required initiation dosing (subcutaneous injections and oral tablets) (Table 1), followed by once every 6-month continuation dosing (subcutaneous injections).

Initiation

On Day 1, the required dose is 927 mg of lenacapavir administered by subcutaneous injection and 600 mg taken orally. On Day 2, the required dose is 600 mg taken orally.

Table 1. Dosing schedule for lenacapavir initiation and continuation:

Time 
 Dose of lenacapavir: Initiationa
Day 1927 mg subcutaneous injection (2 x 1.5 mL injectionsb)
600 mg orally (2 x 300 mg tablets)
Day 2600 mg orally (2 x 300 mg tablets)
 Dose of lenacapavir: Continuation
Every 6 Months
(26 weeks)c
+/- 2 weeks
927 mg subcutaneous injection (2 x 1.5 mL injectionsb)

a The complete initiation dosing schedule, consisting of subcutaneous injections and oral tablets, is required; the efficacy of lenacapavir has only been established with this dosing schedule.
b Two injections, with the second injection at least 5 centimetres from the first injection.
c From the date of the last injection.

Missed initiation dose

If the Day 1 or Day 2 oral initiation dose (600 mg) is missed, it should be taken as soon as possible. Day 1 and Day 2 doses should not be taken on the same day.

Anticipated delayed injections

During continuation dosing, if the scheduled 6-month injection is anticipated to be delayed by more than 2 weeks, lenacapavir tablets may be used for oral bridging on an interim basis (for up to 6 months if needed), until injections resume. Oral bridging should be initiated within 26 to 28 weeks from the last injection. The dosing schedule is 300 mg (1 tablet) taken orally once every 7 days. Resume the continuation injection dosage within 7 days after the last oral dose (see Table 1).

Missed injections

During the continuation period, if more than 28 weeks have elapsed since the last injection and lenacapavir tablets have not been taken for oral bridging, restart the initiation dosing schedule from Day 1 (see Table 1).

Vomiting

If the individual vomits within 3 hours of taking an oral dose of lenacapavir, another oral dose should be taken. If the individual vomits more than 3 hours after taking an oral dose of lenacapavir there is no need to take another oral dose of lenacapavir, and the scheduled dosing regimen should continue.

Dosage considerations

Lenacapavir injections must only be administered subcutaneously into the abdomen or thigh (two injections, with the second injection at least 5 centimetres from the first injection) by a healthcare professional. Do NOT administer intradermally.

Following lenacapavir injection, a subcutaneous drug depot forms whereby lenacapavir is slowly released from the site of administration. In some individuals, this may lead to a nodule at the injection site.

Active ingredient

Lenacapavir

Lenacapavir is a multistage, selective inhibitor of HIV-1 capsid function that directly binds to the interface between capsid protein (CA) subunits. Lenacapavir inhibits HIV-1 replication by interfering with multiple, essential steps of the viral lifecycle, including capsid-mediated nuclear uptake of HIV-1 proviral DNA, virus assembly and release, and capsid core formation.

Read more about Lenacapavir

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