Integrase inhibitors are the class of HIV medicine most often used as the anchor of modern treatment. Dolutegravir and bictegravir are the two best known members of this class. This guide explains what integrase inhibitors are, how they work, and why current guidance places them first among the available options.
The class is sometimes abbreviated to INSTIs, short for integrase strand transfer inhibitors. The name describes exactly what these medicines do.
| Important note This article is general information about medicines used in HIV care. It does not include dosing instructions and is not a substitute for medical advice. All HIV medicines are prescription-only and are selected, started, and changed by a qualified doctor. |
Quick Summary / Key Takeaways
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Integrase inhibitors are the class of HIV medicine most often used as the anchor of modern treatment. Dolutegravir and bictegravir are the two best known members of this class. This guide explains what integrase inhibitors are, how they work, and why current guidance places them first among the available options.
The class is sometimes abbreviated to INSTIs, short for integrase strand transfer inhibitors. The name describes exactly what these medicines do.
What Are Integrase Inhibitors?
Integrase inhibitors are a class of antiretroviral medicine that blocks an enzyme called integrase. HIV depends on this enzyme to insert its genetic material into the DNA of a human immune cell. Once that step is blocked, the virus cannot establish itself inside the cell or produce new copies.
How the Class Works
The process HIV uses to multiply has several stages, and different classes interrupt different stages. Integrase inhibitors act at the point where the virus would otherwise become part of the cellโs own genetic instructions. Because this step is essential, blocking it is highly effective. This is why an integrase inhibitor is usually combined with two NRTIs, as described in first-line ART regimens explained.
Members of the Class
| Medicine | Where it fits |
|---|---|
| Dolutegravir | The most widely used integrase inhibitor in India, commonly part of the TLD combination |
| Bictegravir | Used within a single-tablet combination regimen |
| Raltegravir | An earlier member of the class, used in particular situations |
Why This Class Is Preferred
Guidance from the World Health Organization, updated in January 2026, continues to recommend dolutegravir-based regimens as the preferred option both for people starting treatment and for those moving to a subsequent regimen. Several features explain that position:
- Effectiveness, with high rates of viral suppression reported in programme settings.
- Good tolerability compared with several older options.
- A high barrier to resistance, meaning the virus does not adapt to it easily.
- Availability in single-tablet combinations, which simplifies daily treatment.
Dolutegravir and Bictegravir Compared
Both medicines belong to the same class and work in the same broad way. Dolutegravir is the more widely available option in India and appears in the most commonly used fixed-dose combination. Bictegravir is supplied as part of a complete single-tablet regimen.
Safety Points Doctors Monitor
Integrase inhibitors are generally well tolerated. As with any medicine, there are points a treating doctor keeps under review:
- Mild effects when treatment begins, such as headache, sleep changes, or stomach upset, which often settle.
- Changes in body weight in some people taking this class.
- Interactions with certain other medicines and supplements.
- Routine monitoring of treatment response through HIV lab testing.
Myths vs Facts: Integrase Inhibitors
| Myth | Fact |
|---|---|
| Integrase inhibitors can be taken on their own. | They are used in combination with other ART medicines. |
| Newer classes are less studied and less reliable. | This class is extensively studied and is the preferred option in current guidance. |
| All integrase inhibitors are identical. | They share a mechanism but differ in availability and combinations. |
| Weight change affects everyone on this class. | It is reported in some people, and treating doctors monitor it. |
| Resistance develops quickly with this class. | These medicines have a high barrier to resistance. |
| When to Consult a Doctor Medical advice is appropriate before starting or changing any integrase inhibitor, where side effects appear or persist, and where other medicines or supplements are being taken alongside treatment. A consultation can be arranged through an HIV doctor consultation. |
Conclusion
Integrase inhibitors block the step HIV needs to insert itself into human cells, which makes them a highly effective foundation for treatment. Dolutegravir and bictegravir lead this class, and dolutegravir-based regimens remain the preferred choice in current international guidance. As with all ART, these medicines are prescribed and monitored by a treating doctor.
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Frequently Asked Questions
What are integrase inhibitors?
Integrase inhibitors are a class of HIV medicine that blocks an enzyme called integrase. HIV needs this enzyme to insert its genetic material into human immune cells, so blocking the step prevents the virus from establishing itself and multiplying.
Which medicines belong to this class?
Dolutegravir and bictegravir are the most widely used, with raltegravir as an earlier member of the class. Dolutegravir is the most commonly used integrase inhibitor in India.
Why are integrase inhibitors preferred?
Current World Health Organization guidance recommends dolutegravir-based regimens as the preferred option because of their effectiveness, good tolerability, high barrier to resistance, and availability in simple single-tablet combinations.
What is the difference between dolutegravir and bictegravir?
Both belong to the same class and work in the same broad way. Dolutegravir is more widely available in India and appears in the commonly used TLD combination, while bictegravir is supplied within a complete single-tablet regimen.
Are integrase inhibitors taken alone?
No. They are used in combination with other antiretroviral medicines, most often two NRTIs, so that HIV is blocked at more than one stage at the same time.
What does a high barrier to resistance mean?
It means the virus does not adapt easily to the medicine. This is one reason integrase inhibitors are favoured, as treatment is more likely to remain effective over time when taken consistently.
What side effects are associated with this class?
The class is generally well tolerated. Some people notice mild effects when treatment begins, such as headache, sleep changes, or stomach upset, which often settle. Changes in body weight are also monitored.
Do integrase inhibitors interact with other medicines?
Certain medicines and supplements can affect how these medicines work. A treating doctor reviews everything being taken, including over-the-counter products, before starting or changing treatment.
