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HIV-1 capsid inhibitor

YEZTUGO (lenacapavir) is a long-acting medication used for pre-exposure prophylaxis (PrEP) to help prevent HIV-1 infection in adults and adolescents who are at risk. It involves an initial series of oral tablets and injections, followed by a single injection every 6 months. It is vital to confirm you are HIV-negative before starting and before every injection to prevent drug resistance.

How it worksYEZTUGO is a capsid inhibitor, which means it works by targeting and interfering with the structural proteins of the HIV-1 virus.

Brand names:Yeztugo

Used for
Pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 in adults and adolescents weighing at least 35 kg who are at risk for HIV-1 acquisition.
Conditions
HIV-1 infection risk
Class
AntiretroviralCapsid InhibitorHIV-1 capsid inhibitorImmune System

How to take

FormsOral tablets, Subcutaneous injection
RoutesOral, Subcutaneous

The regimen starts with a Day 1 injection (927 mg) and tablets (600 mg), followed by Day 2 tablets (600 mg). After this, a 927 mg injection is given every 6 months.

Tablets can be taken with or without food. If an injection is delayed by more than 2 weeks, 300 mg tablets may be used for up to 6 months as a temporary measure.

Missed dose: If the Day 2 oral dose is missed, take it as soon as possible. If an injection is delayed by more than 2 weeks, use 300 mg tablets once every 7 days as an interim measure.

Key warnings

There is a serious risk of drug resistance if YEZTUGO is used by someone who already has undiagnosed HIV-1. Users must be tested for HIV-1 before starting and before every subsequent injection.

  • ·There is a serious risk of drug resistance if YEZTUGO is used by someone who already has undiagnosed HIV-1. Users must be tested for HIV-1 before starting and before every subsequent injection.
  • ·Must be HIV-1 negative before starting and before every injection.
  • ·Drug resistance can develop if HIV-1 is acquired before, during, or after use.
  • ·Improper injection technique can cause serious reactions at the injection site.
  • ·The medication can stay in your body for 12 months or longer after the last dose.

Do not use if

  • ·People with unknown or positive HIV-1 status should not use YEZTUGO.

Side effects

Common

Injection site reactionsHeadacheNausea

Serious

  • ·Serious injection site reactions if not administered correctly
  • ·Risk of developing drug resistance if HIV-1 is present

Seek help if

  • ·Serious injection site reactions
  • ·Signs of acute HIV-1 infection (fever, fatigue, rash)
  • ·Symptoms of drug-resistant HIV

Interactions

  • ·Strong or moderate CYP3A inducers may make YEZTUGO less effective.
  • ·Strong or moderate CYP3A inhibitors combined with P-gp and UGT1A1 inhibitors may increase YEZTUGO levels significantly; these should not be used together.
  • ·YEZTUGO may increase the levels of other drugs metabolized by CYP3A or P-gp for up to 9 months after the last injection.
FoodOral tablets can be taken with or without food.

Special populations

PregnancyData from clinical trials showed no increased risk of miscarriage or major birth defects compared to control groups, though a registry exists to monitor outcomes. If you are at risk of HIV-1, consider continuing PrEP during pregnancy.

BreastfeedingLenacapavir can be found in human milk at very low levels. No adverse effects have been seen in breastfed infants so far.

PediatricYEZTUGO is safe and effective for adolescents weighing at least 35 kg. Safety and effectiveness for children weighing less than 35 kg have not been established.

GeriatricThere is not enough data on people aged 65 and older. Use with caution in elderly patients due to potential changes in organ function.

Talk to your doctor

Monitor

  • ·HIV-1 status
  • ·Injection site (nodules, swelling, pain)
  • ·Symptoms of acute HIV-1 infection

Questions to ask

  • ·Should I be tested for HIV-1 before my next YEZTUGO injection?
  • ·How will YEZTUGO interact with my current medications?
  • ·What should I do if my injection is delayed?
  • ·Are there specific signs of an injection site reaction I should watch for?

Pharmacokinetics

Half-life10 to 12 days (elimination); 77 to 84 days (subcutaneous)
DurationLong-acting; residual concentrations can remain for 12 months or longer.
Bioavailability91% (subcutaneous administration)
Protein binding>98.5%
MetabolismMetabolized via CYP3A and UGT1A1 (minor)
ExcretionMajor route is feces (76% of dose); less than 1% excreted in urine.

Practical

OverdoseNo specific overdose data is available. If an overdose occurs, general supportive care and monitoring of vital signs are required.

Ingredients

Inactive

copovidonecroscarmellose sodiummagnesium stearatemannitolmicrocrystalline cellulosepoloxamer 407iron oxide blackiron oxide rediron oxide yellowpolyethylene glycolpolyvinyl alcoholtalctitanium dioxidepolyethylene glycol 300water for injection

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.