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[Pharmacology](https://durgical.com/en/pharmacology/) · [Integrase strand transfer inhibitors (INSTIs)](https://durgical.com/en/pharmacology/classes/integrase-strand-transfer-inhibitors/)

# Bictegravir

A second-generation integrase inhibitor sold only in a single tablet with emtricitabine and tenofovir alafenamide.

Updated 2026-11-01

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

Also called: BIC

✂**HIV integrase (intasome)**Bictegravir

ⓘ The figure shows bictegravir bound to the two-magnesium active site of the HIV intasome, by cryo-electron microscopy.

**Target in 3D:** HIV integrase (intasome). PDB structure 6PUW (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6PUW) · Drag to rotate · pinch to zoom

## Mechanism of action

It binds the two magnesium ions in the active site of integrase bound to viral DNA and blocks strand transfer, like dolutegravir, with a high genetic barrier.

- It binds the magnesium ions of the integrase active site
- Strand transfer is blocked
- Viral DNA is not integrated into the chromosome

## Pharmacokinetics

**Absorption**
Oral, with or without food; polyvalent cations reduce absorption

**Metabolism**
Liver, by CYP3A4 and UGT1A1

## Indications

- HIV-1 infection, as a single tablet with emtricitabine and tenofovir alafenamide [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)

## Adverse effects

### Common

- Diarrhoea
- Nausea
- Headache
- Mild creatinine rise without kidney damage

### Serious (rare, important)

- Severe hepatitis B flare after stopping the combination (from its NRTI components)
- Lactic acidosis (from its NRTI components)
- Immune reconstitution syndrome

## Contraindications

- Rifamycins, carbamazepine and St John's wort (greatly lower bictegravir)

## Key interactions

**Rifampicin, carbamazepine, St John's wort**
Induce CYP3A4 and UGT1A1 and cause failure: not combined

**Metformin**
Raises metformin, somewhat less than dolutegravir

**Aluminium or magnesium antacids, calcium or iron supplements**
They chelate the drug and lower absorption: doses are separated

## What is monitored

- HIV and hepatitis B tests before starting
- Kidney function
- Viral load and CD4

## Administration and safety

- By mouth, one tablet with or without food
- Separate antacids, calcium, iron and mineral-containing multivitamins in time, as the label directs
- Do not combine with other products containing emtricitabine, lamivudine or tenofovir

## Nursing care

- Confirm hepatitis B serology
- Check TB drugs and anticonvulsants
- Teach not to run out of medicine

## 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

'BIC = Brilliant in one tablet, Inducers Contraindicated'.

## Test yourself

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

## Which drugs is bictegravir co-formulated with?

With emtricitabine and tenofovir alafenamide, in a single tablet.

## Why is bictegravir not used with rifampicin?

Rifampicin induces CYP3A4 and UGT1A1, the pathways that clear bictegravir, and its levels fall.

## What hepatitis B risk does the bictegravir combination carry?

Its emtricitabine and tenofovir components suppress hepatitis B; stopping it can cause a severe flare.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/bictegravir/)

## Related drugs

- [Dolutegravir](https://durgical.com/en/pharmacology/dolutegravir/)
- [Emtricitabine](https://durgical.com/en/pharmacology/emtricitabine/)
- [Tenofovir alafenamide](https://durgical.com/en/pharmacology/tenofovir-alafenamide/)

## 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: [Bictegravir, Emtricitabine, and Tenofovir Alafenamide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a618012.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=J05AR21) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 64 (McGraw Hill, 2023).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/bictegravir/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/bictegravir/