Apretude Injection

Apretude (cabotegravir) is a long-acting injectable pre-exposure prophylaxis (PrEP) medication used to reduce the risk of HIV-1 infection in adults and adolescents weighing at least 35 kg (77 lb). Unlike daily oral PrEP pills, Apretude is administered as an injection once every two months, making it a convenient alternative for those who find daily medication difficult to maintain. It was the first long-acting injectable PrEP approved by the FDA, receiving approval on January 21, 2022.

• HIV-1 is the virus that causes acquired immune deficiency syndrome (AIDS).
• Oral cabotegravir may be administered initially to assess tolerability to cabotegravir before administering Apretude.
• It is not known if Apretude is safe and effective in children <12 years or < 35 kg (77 lb).

Pre-exposure prophylaxis (PrEP) refers to medication taken by HIV-negative individuals to significantly reduce their risk of contracting HIV. When used correctly, PrEP has been shown to reduce the risk of sexually acquired HIV by up to 99%. Apretude is currently the only long-acting injectable PrEP option approved by the FDA.

Apretude is available online through telehealth for a $25 provider fee. The cost of the medicine depends on your health insurance, and there may be additional lab testing or administration fees. Click here to see if you are eligible for this service.

Clinical trials report Apretude is 99% effective in preventing HIV-1 transmission when used correctly and is effective in a diverse population group (such as cisgender men who have sex with men, non-binary, and trans people). A negative HIV test is required before starting treatment and before each injection.

Apretude and daily oral PrEP medications like Truvada and Descovy all work to prevent HIV-1 infection, but they differ in how they're taken and how they work in the body. The key differences are outlined below.

Apretude will be given to you as an injection by your healthcare provider.

• Apretude is initially given as an injection into the muscle of your buttock 1 time every month for the first 2 months, then as an injection 1 time every 2 months.
• Before receiving your first injection dose of Apretude, your healthcare provider may have you take 1 Vocabria (cabotegravir) tablet 1 time a day for 1 month (at least 28 days). This will allow your healthcare provider to assess how well you will tolerate cabotegravir.
• Apretude is a long-acting medicine and may stay in your body for 12 months or longer after your last injection.
• Stay under the care of a healthcare provider while receiving Apretude. You must receive Apretude as scheduled.
• If you stop receiving Apretude, talk to your healthcare provider about other options to reduce the risk of getting HIV-1 infection.

Important information for people who receive Apretude to help reduce their risk of getting human immunodeficiency virus-1 (HIV-1) infection, also called pre-exposure prophylaxis or “PrEP”.

Apretude carries a Boxed Warning for the risk of developing drug-resistant HIV-1 if used in individuals with undiagnosed HIV infection.

Before receiving Apretude to reduce your risk of getting HIV-1:

• You must be HIV-1 negative to start Apretude. You must get tested to make sure that you do not already have HIV-1 infection.
• Do not receive Apretude for HIV-1 PrEP unless you are confirmed to be HIV-1 negative.
• Some HIV-1 tests can miss HIV-1 infection in a person who has recently become infected. If you have flu-like symptoms, you could have recently become infected with HIV-1. Tell your healthcare provider if you had a flu-like illness within the last month before starting Apretude or at any time while receiving Apretude. Symptoms of new HIV-1 infection include: Tiredness Joint or muscle aches Sore throat Rash Enlarged lymph nodes in the neck or groin Fever Headache Vomiting or diarrhea Night sweats.

While you are receiving Apretude for HIV-1 PrEP:

• Apretude does not prevent other sexually transmitted infections. Practice safer sex by using a latex or polyurethane condom to reduce the risk of getting sexually transmitted infections.
• You must stay HIV-1 negative to keep receiving Apretude for HIV-1 PrEP. Know your HIV-1 status and the HIV-1 status of your partners. Ask your partners with HIV-1 if they are taking anti-HIV-1 medicines and have an undetectable viral load. An undetectable viral load is when the amount of virus in the blood is too low to be measured in a lab test. To maintain an undetectable viral load, your partners must keep taking HIV-1 medicine as prescribed. Your risk of getting HIV-1 is lower if your partners with HIV-1 are taking effective treatment. Get tested for HIV-1 with each Apretude injection or when your healthcare provider tells you. You should not miss any HIV-1 tests. If you become HIV-1–infected and continue receiving Apretude because you do not know you are HIV-1–infected, the HIV-1 infection may become harder to treat. Get tested for other sexually transmitted infections such as syphilis, chlamydia, and gonorrhea. These infections make it easier for HIV-1 to infect you. If you think you were exposed to HIV-1, tell your healthcare provider right away. They may want to do more tests to be sure you are still HIV-1 negative. Get information and support to help reduce sexual risk behaviors. Do not miss any Apretude injections. Missing injections increases your risk of getting HIV-1 infection. If you do become HIV-1 positive, you will need to take other medicines to treat HIV-1. Apretude is not approved for the treatment of HIV-1.

If you have HIV-1 and receive only Apretude, over time, your HIV-1 may become harder to treat.

Do not receive Apretude if you:

• Already have an HIV infection. If you are HIV-1 positive, you will need to take other medicines to treat this infection because Apretude is not approved for HIV treatment
• Do not know your HIV-1 infection status. You may already be HIV-1 positive. You need to take other medicines to treat HIV-1. Apretude injection can only help reduce your risk of getting HIV-1 infection before you are infected.
• Have ever had an allergic reaction to cabotegravir, Apretude, or any of the inactive ingredients in the injection
• Are taking any of the following medicines: carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, or rifapentine.

Before receiving Apretude, tell your healthcare provider about all your medical conditions, including if you:

• have ever had a skin rash or an allergic reaction to medicines that contain cabotegravir
• have or have had liver problems.
• have ever had mental health problems
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

Pregnancy

It is not known if Apretude will harm your unborn baby. Apretude can remain in your body for up to 12 months or longer after the last injection. Tell your healthcare provider if you become pregnant while or after receiving Apretude.

Pregnancy Registry: There is a pregnancy registry for those who receive Apretude during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk to your healthcare provider about how you can take part in this registry.

Breastfeeding

Apretude may pass into your breast milk. Talk with your healthcare provider about the best way to feed your baby while or after receiving Apretude.

Common side effects

The most common side effects of Apretude are:

• Pain, tenderness, hardened mass or lump, swelling, bruising, redness, itching, warmth, loss of sensation at the injection site, abscess, and discoloration where the injection was given
• Diarrhea
• Headache
• Fever
• Tiredness
• Sleep problems
• Nausea
• Dizziness
• Passing gas
• Stomach pain
• Vomiting
• Muscle pain
• Rash
• Loss of appetite
• Drowsiness
• Back pain
• Upper respiratory infection.

Serious Side Effects and Warnings

Apretude may cause the following serious side effects:

• Allergic reactions. Stop receiving Apretude and get medical help right away if you develop a rash with Apretude, as it may be a sign of a more serious reaction, such as Stevens-Johnson syndrome (SJS)/toxic epidermal necrolysis (TEN). The rash may occur with other symptoms, such as:
• fever generally ill feeling tiredness muscle or joint aches trouble breathing blisters or sores in the mouth blisters redness or swelling of the eyes swelling of the mouth, face, lips, or tongue.
• Liver problems. Liver problems have happened in people with or without a history of liver problems or other risk factors. Your healthcare provider may do blood tests to check your liver function. Call your healthcare provider right away if you develop any of the following signs or symptoms of liver problems: your skin or the white part of your eyes turns yellow (jaundice) dark or “tea-colored” urine light-colored stools (bowel movements) nausea or vomiting loss of appetite pain, aching, or tenderness on the right side of your stomach itching.
• Depression or mood changes. Apretude may affect your mood. Call your healthcare provider or get medical help right away if you develop any of the following symptoms: feeling sad or hopeless feeling anxious or restless have thoughts of hurting yourself (suicide) or have tried to hurt yourself.

These are not all the possible side effects of Apretude. If you experience side effects, contact your doctor. You can also report side effects to the FDA at 1-800-FDA-1088.

Apretude (cabotegravir) works by blocking HIV integrase, a key enzyme required by HIV to replicate. This prevents HIV from establishing an infection. Specifically, cabotegravir binds to the integrase active site and prevents the strand transfer step, a critical process where viral DNA is inserted into human chromosomes.

Apretude belongs to a class of medications called integrase strand transfer inhibitors (INSTIs). It works by blocking an enzyme called HIV integrase, which the virus needs to replicate inside the body. Specifically, cabotegravir prevents HIV's genetic material from being inserted into human DNA, a process known as strand transfer, effectively stopping the virus from establishing an infection in the first place.

Because Apretude is an extended-release formulation, a single injection protects for up to two months, although the medication can remain detectable in the body for up to 12 months or longer after the final dose.

Initial Dose of Apretude for HIV-1 Prevention for Adults and Adolescents

• 600 mg/3 mL (1 injection).
• Repeat the dose 1 month later.
• Give the injection on the last day or within 3 days of lead-in of oral cabotegravir (Vocabria) if used.

Maintenance Dose of Apretude for HIV-1 Prevention for Adults and Adolescents

• 600 mg/3 mL (1 injection) every 2 months.

If you miss or plan to miss a scheduled injection of Apretude by more than 7 days, call your healthcare providerright away to discuss your PrEP options.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Some medicines may interact with Apretude. Keep a list of your medicines and show it to your healthcare provider and pharmacist when you get a new medicine. Especially tell your healthcare provider if you take:

• Carbamazepine
• Oxcarbazepine
• Phenobarbital
• Phenytoin
• Rifampin
• Rifapentine.

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

Active ingredient: cabotegravir

Inactive ingredients: mannitol, polyethylene glycol (PEG) 3350, polysorbate 20, and Water for Injection.

Apretude is available as a single-dose vial of 600 mg/3 mL (200 mg/mL) of cabotegravir extended-release injectable suspension.

Apretude is manufactured by ViiV Healthcare, a global pharmaceutical company headquartered in Brentford, United Kingdom.

ViiV Healthcare is a collaboration between GlaxoSmithKline (majority owner), Pfizer, and Shionogi, and specializes in HIV/AIDS treatments.