cabotegravir
Apretude (cabotegravir) is a long-acting injectable integrase inhibitor from ViiV Healthcare used for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in adults and adolescents at risk. Given as an intramuscular injection every two months after the initial doses, it keeps protective drug levels in the body between shots.
This page is based on DailyMed prescribing information for cabotegravir (Apretude), cross-checked with MedlinePlus and the NCI Drug Dictionary; the mechanism is explained in plain language, and analogies are used only where they stay accurate.
How it works
Explains what the medicine does in the body, not dosing, side effects, or safety.
An analogy
HIV needs to file its genetic blueprint into the cell's own records so the cell starts making more virus. Cabotegravir is like a piece of gum stuck in the filing slot — the enzyme cannot slide the viral DNA into place, so the infection cannot take hold.
In simple terms
Cabotegravir blocks an enzyme called HIV integrase, which the virus needs to insert its genetic material into the DNA of human cells. Without this step, HIV cannot set up a lasting infection inside the cell. For PrEP, cabotegravir is given as an injection into the muscle every two months after the first two loading doses one month apart. The long-acting form keeps protective drug levels in the body between visits, reducing the risk of catching HIV through sex when taken as prescribed. It must only be started in people who are confirmed HIV-negative.
In depth
Cabotegravir is a second-generation integrase strand transfer inhibitor (INSTI) that chelates the two catalytic magnesium ions in the HIV-1 integrase active site, blocking the strand transfer step in which viral DNA is joined to host chromosomal DNA. The long-acting injectable formulation (cabotegravir sodium) forms a depot at the intramuscular injection site, releasing drug over weeks and maintaining plasma concentrations above the protein-adjusted 90% inhibitory concentration (PA-IC90) for approximately two months. As PrEP, it prevents HIV from establishing a foothold after exposure; as part of treatment regimens (with rilpivirine), it suppresses viral replication in people already living with HIV.
See it in motion
A schematic animation of the mechanism — simplified for clarity, not drawn to scale.
How cabotegravir, a long-acting injectable INSTI, blocks HIV-1 integrase
- HIV needs to file its genetic blueprint into the cell's own records so the cell starts making more virus.
- Cabotegravir is a second-generation integrase strand transfer inhibitor (INSTI) that chelates the two catalytic magnesium ions in the HIV-1 integrase active site, blocking the strand transfer step in which viral DNA is joined to host chromosomal DNA.
- The long-acting injectable formulation (cabotegravir sodium) forms a depot at the intramuscular injection site, releasing drug over weeks and maintaining plasma concentrations above the protein-adjusted 90% inhibitory concentration (PA-IC90) for approximately two months.
- As PrEP, it prevents HIV from establishing a foothold after exposure; as part of treatment regimens (with rilpivirine), it suppresses viral replication in people already living with HIV.
Target: HIV-1 integrase
The viral enzyme that inserts HIV DNA into the host cell's chromosomes, a step required for the virus to establish a persistent infection and produce new virus particles.
Approved uses
Approved uses differ by country and change over time. Always follow your local prescribing information.
Approved uses in United States
FDA- Pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in adults and adolescents weighing at least 35 kg who are at risk for HIV-1 acquisition; individuals must have a negative HIV-1 test prior to initiating Apretude
Approved uses in United States
MedlinePlus- Used to treat human immunodeficiency virus type 1 (HIV-1) infection (as Vocabria)
- Also used for certain periods to prevent HIV-1 infection (as Apretude, for PrEP)
Approved uses in United States
NCI- A human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI) used for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection; binds to the active site of HIV integrase and inhibits the activity of the enzyme, preventing integration of HIV-1 DNA into host genomic DNA
Official sources
The statements on this page trace back to these records.
- DailyMed: APRETUDE (cabotegravir) label
DailyMed, U.S. National Library of Medicine
- MedlinePlus: cabotegravir
MedlinePlus, U.S. National Library of Medicine
- National Cancer Institute: cabotegravir
National Cancer Institute
This page explains how the medicine works — it isn’t the patient leaflet. For anything that applies to you, read the leaflet that came with your medicine or ask your pharmacist.
MedUnfold provides educational content and is not medical advice. Always follow your local prescribing information and healthcare professional.