HIV Integrase Inhibitors

HIV Integrase Inhibitors: Their role in Clinical management

Introduction:
Clinicians now have five classes of antiretroviral agents (ARVs) for the treatment of HIV infection in both treatment-naïve and treatment - experienced individuals.

1. Nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs)
2. non-nucleoside/nucleotide reverse transcriptase inhibitors (NNRTIs)
3. Protease inhibitors (PIs)
4. Entry and fusion inhibitors
5. Integrase strand transfer inhibitors (INSTIs)

Integrase strand transfer inhibitors, often abbreviated to "integrase inhibitors", target an enzyme called Integrase, a protein essential for HIV replication. As a result, proviral DNA is unable to insert into the host cell genome. This terminates the life cycle of the virus (see figure on the right).

Three INSTI's have been approved by the FDA: Raltegravir (Isentress), Dolutegravir (Tivicay) and elvitegravir (Vitekta). Raltegravir (RAL) and Dolutegravir (DTG) is registered and available for routine use in South Africa and will be the focus of this clinical update.

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