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# Cabotegravir

An integrase inhibitor available as a long-acting injection: it prevents HIV (PrEP) and, with rilpivirine, treats it with spaced injections.

Updated 2026-11-01

- Class: [Integrase strand transfer inhibitors (INSTIs)](https://durgical.com/en/pharmacology/classes/integrase-strand-transfer-inhibitors/)
- Enzyme: HIV integrase (intasome)
- ATC code: J05AJ04

Also called: CAB

✂**HIV integrase (intasome)**Cabotegravir

ⓘ No structure with cabotegravir was found. The figure shows dolutegravir, its close structural analogue, which occupies the same two-magnesium site of the HIV-1 intasome.

**Target in 3D:** HIV integrase (intasome). PDB structure 8FN7 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8FN7) · Drag to rotate · pinch to zoom

## Mechanism of action

A close analogue of dolutegravir: it binds the magnesium ions of the integrase active site and blocks integration of viral DNA. Its structure allows a nanocrystal formulation for intramuscular injection that releases drug over weeks.

- It is released slowly from the intramuscular depot
- It binds the magnesium ions of the integrase active site
- Integration of viral DNA is blocked

## Pharmacokinetics

**Absorption**
Oral (with food) or long-acting intramuscular

**Metabolism**
Mainly by UGT1A1

**Half-life**
The injectable lasts weeks and can be detected in blood more than a year after the last injection

## Indications

- Prevention of HIV-1 infection (injectable PrEP) [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)
- Treatment of suppressed HIV-1 infection, with injectable rilpivirine [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)

## Adverse effects

### Common

- Injection-site reactions (pain, swelling, nodules) in most people
- Fever, tiredness, headache
- Nausea, abnormal dreams, anxiety, insomnia

### Serious (rare, important)

- Hypersensitivity reactions
- Hepatotoxicity
- Depression or suicidal thoughts
- INSTI resistance if HIV is acquired during PrEP or in the low-level 'tail' after stopping

## Contraindications

- Previous hypersensitivity to cabotegravir
- Use as PrEP without a negative HIV test

## Key interactions

**Rifampicin and other strong UGT1A1 inducers**
Lower cabotegravir with risk of failure

**Calcium, magnesium or aluminium antacids (oral form)**
Lower absorption of oral cabotegravir: doses are separated

## What is monitored

- Negative HIV test before each PrEP injection
- Symptoms of acute HIV infection
- Mood
- Liver tests

## Administration and safety

- The injectable is given intramuscularly in the buttock by health staff
- Keep to the appointment schedule: a long delay leaves low levels and a resistance risk
- It may start with an oral phase to check tolerance

## Nursing care

- Confirm a negative HIV test before each PrEP injection
- Check the injection site and teach to recognise reactions
- Record the next appointment date and ask to be told of any delay
- Ask about depressive symptoms

## Pregnancy and breastfeeding

Antiretroviral treatment in pregnancy protects the mother and lowers HIV transmission to the baby; the treating team chooses the regimen.

## Memory aid

'CABotegravir: Come And get a Buttock shot': injectable PrEP, HIV test before each dose.

## Test yourself

Think of the answer, then tap the question to see it.

## Which test is needed before each PrEP cabotegravir injection, and why?

A negative HIV test: if the person already has HIV, cabotegravir alone would select INSTI-resistant virus.

## What is the pharmacokinetic 'tail' of injectable cabotegravir?

After stopping, levels fall very slowly over months; if HIV is acquired then, resistance can emerge.

## Which drug is injectable cabotegravir combined with to treat HIV?

With long-acting injectable rilpivirine.

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## Related drugs

- [Dolutegravir](https://durgical.com/en/pharmacology/dolutegravir/)
- [Rilpivirine](https://durgical.com/en/pharmacology/rilpivirine/)

## Related conditions

- [HIV infection and AIDS](https://durgical.com/en/conditions/hiv-infection-and-aids/)

[← Back to the class: Integrase strand transfer inhibitors (INSTIs)](https://durgical.com/en/pharmacology/classes/integrase-strand-transfer-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Cabotegravir Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a622053.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [Cabotegravir: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a621010.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [HIV and AIDS](https://www.who.int/news-room/fact-sheets/detail/hiv-aids) (World Health Organization, 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 64 (McGraw Hill, 2023).

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Representative model, for educational purposes only.

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