Bixlenvo

Bixlenvo is used to treat Human Immunodeficiency Virus-1 (HIV-1) in adults to replace their current HIV-1 medicines in those who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected resistance to the ingredients in Bixlenvo. Bixlenvo is taken once daily following a two-day initiation regimen with oral Sunlenca.

Bixlenvo combines two antiretrovirals that block HIV-1 at different points in its lifecycle. Bictegravir is an integrase strand transfer inhibitor (INSTI). It works by blocking HIV-1 integrase from inserting viral DNA into the host cell's genome, preventing formation of the provirus and stopping propagation of the virus. Lenacapavir is a capsid inhibitor. It binds at the interface between capsid protein subunits and disrupts several stages of the lifecycle: nuclear uptake of viral DNA, virus assembly and release, and formation of the capsid core. Bixlenvo is a complete regimen for adults with HIV-1 who are already virologically suppressed and are switching from their current antiretroviral regimen.

Bixlenvo received FDA approval on August 27, 2026, and is the first single-tablet regimen for virologically suppressed adults whose drug resistance or tolerability problems have kept them on complex, multi-pill HIV regimens.

Approval for Bixlenvo was based on Week 48 data from two randomized Phase 3 switch trials. ARTISTRY-1 (NCT05502341; N=557, open-label) enrolled adults switching from complex regimens of 2–11 pills daily; ARTISTRY-2 (NCT06333808; N=574, double-blind) enrolled adults switching from Biktarvy. In both, 1% of participants in every arm had HIV-1 RNA of 50 copies/mL or higher at Week 48. Treatment differences were −0.3% and 0.3%, respectively. Bixlenvo was generally well tolerated.

Take Bixlenvo exactly as your healthcare provider tells you to take it.

• Your treatment includes Bixlenvo tablets and, for the first 2 days only, another medicine called Sunlenca tablets.
• Take Bixlenvo and Sunlenca tablets by mouth, with or without food.
• Your dosing schedule will start as follows: On Day 1, take 1 Bixlenvo tablet and 2 Sunlenca tablets. On Day 2, take 1 Bixlenvo tablet and 2 Sunlenca tablets. It is very important that you take Bixlenvo with Sunlenca on these first 2 days. Contact your healthcare provider if you have questions.
• Your dosing schedule will then continue as follows: On Day 3 and each day after, take 1 Bixlenvo tablet each day.
• If you take antacids that contain aluminum or magnesium, take Bixlenvo at least 2 hours before or 6 hours after you take these antacids.
• If you take supplements or antacids that contain iron or calcium, take Bixlenvo with food at the same time that you take these supplements or antacids.
• If you are pregnant and take supplements or antacids that contain aluminum, magnesium, iron or calcium, talk to your healthcare provider about how to take Bixlenvo along with these supplements or antacids.
• If you miss a dose of Bixlenvo or Sunlenca on Day 1 or Day 2, take it as soon as possible. Do not take Day 1 and Day 2 doses of Sunlenca on the same day.
• If you miss a dose of Bixlenvo on Day 3 and each day after, take it as soon as possible. If more than 7 days have passed since your last dose of Bixlenvo, contact your healthcare provider as your healthcare provider will need to determine how to continue your HIV-1 treatment.
• If you take too much Bixlenvo, call your healthcare provider or go to the nearest hospital emergency room right away.
• When your Bixlenvo supply starts to run low, get more from your healthcare provider or pharmacy. This is very important because the amount of virus in your blood may increase if the medicine is stopped for even a short time. The virus may develop resistance to Bixlenvo and become harder to treat.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements, including St. John's wort. Some medicines may interact with Bixlenvo. Keep a list of your medicines and show it to your healthcare provider and pharmacist when you get a new medicine.

Do not take Bixlenvo with (contraindicated):

• Dofetilide. Bixlenvo can raise dofetilide levels, risking serious or life-threatening events.
• Strong CYP3A inducers. These lower bictegravir and lenacapavir levels, which can cause loss of therapeutic effect and development of resistance. These include: carbamazepine, phenytoin rifampin St. John's wort (Hypericum perforatum).

Not recommended:

• Other HIV-1 medicines. Bixlenvo is a complete regimen on its own.
• Moderate CYP3A inducers. Oxcarbazepine, phenobarbital, rifabutin, rifapentine.
• Combined P-gp, UGT1A1 and strong CYP3A inhibitors. May significantly increase levels of both components.
• Ergot derivatives. Dihydroergotamine, ergotamine, methylergonovine.
• Tadalafil for pulmonary arterial hypertension.
• Naloxegol. Avoid; if unavoidable, reduce the naloxegol dose and monitor for adverse reactions.

Use with caution or monitoring:

Timing rules for antacids and supplements:

Oral products containing polyvalent cations (magnesium, aluminium, calcium, iron) reduce bictegravir absorption, so timing matters. This also applies to sucralfate and buffered medicines.

• Antacids or laxatives containing aluminium or magnesium — take Bixlenvo at least 2 hours before, or 6 hours after.
• Calcium or iron supplements or antacids — take Bixlenvo together with food at the same time.
• If pregnant — take Bixlenvo at least 2 hours before or 6 hours after aluminium or magnesium antacids, regardless of food. For calcium or iron, take with food; if taken on an empty stomach, take Bixlenvo at least 2 hours before or 6 hours after.

This list is not all inclusive. Some interactions are based on studies of bictegravir or lenacapavir as individual agents rather than the combination. Consider potential drug interactions before and during Bixlenvo therapy, review concomitant medicines, and monitor for adverse reactions associated with them.

You can ask your healthcare provider or pharmacist for a list of medicines that interact with Bixlenvo. Do not start a new medicine without telling your healthcare provider. Your healthcare provider can tell you if it is safe to take Bixlenvo with other medicines.

Before taking Bixlenvo, tell your healthcare provider about all your medical conditions, including if you:

• have hepatitis B virus (HBV).
• are pregnant or plan to become pregnant. Tell your healthcare provider if you become pregnant during treatment with Bixlenvo. Pregnancy Exposure Registry: There is a pregnancy exposure registry for women who take Bixlenvo during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk with your healthcare provider about how you can take part in this registry.
• are breastfeeding or plan to breastfeed. Bixlenvo passes to your baby in your breastmilk. Talk with your healthcare provider about the following risks to your baby from breastfeeding during treatment with Bixlenvo: The HIV-1 virus may pass to your baby if your baby does not have HIV-1. The HIV-1 virus may become harder to treat if your baby has HIV-1. Your baby may get side effects from Bixlenvo.

It is not known if Bixlenvo is safe and effective in children.

Do not take Bixlenvo if you take dofetilide or certain other medicines called strong CYP3A inducers. Ask your healthcare provider if you are not sure. See "What other medicines will affect Bixlenvo?" below.

Common side effects

The most common side effects of Bixlenvo are headache, nausea, and diarrhea.

These are not all the possible side effects of Bixlenvo. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Store Bixlenvo tablets at room temperature between 68 °F and 77 °F (20 °C and 25 °C).

• Bixlenvo bottle contains a desiccant canister to help keep your medicine dry (protect it from moisture). Keep the desiccant canister in the bottle. Do not eat the desiccant canister.
• Keep Bixlenvo tablets in their original bottle.
• Keep the bottle tightly closed.
• Bixlenvo bottle has a child-resistant cap closure.

Keep Bixlenvo and all medicines out of the reach of children.

Active ingredients: bictegravir sodium and lenacapavir sodium

Inactive ingredients: copovidone, croscarmellose sodium, magnesium stearate, mannitol, microcrystalline cellulose, and poloxamer 407. The tablets are film-coated with a coating material containing iron oxide yellow, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

Bixlenvo is manufactured for and distributed by Gilead Sciences, Inc., Foster City, CA 94404.

For more information, call 1-800-445-3235 or go to www.BIXLENVO.com.