Diarylpyrimidines

Diarylpyrimidines (DAPYs) are a class of antiretroviral drugs used in the treatment of HIV/AIDS. They are non-nucleoside reverse transcriptase inhibitors (NNRTIs) that bind to the reverse transcriptase enzyme, preventing the conversion of RNA into DNA, a crucial step in the replication of the HIV virus.

History

The development of diarylpyrimidines began in the late 1990s, with the aim of overcoming the limitations of the first-generation NNRTIs. The first DAPY to be approved for clinical use was etravirine (Intelence), in 2008.

Mechanism of Action

Diarylpyrimidines work by binding to the reverse transcriptase enzyme in a different way than other NNRTIs. This unique binding method allows them to retain their effectiveness against HIV strains that have developed resistance to other NNRTIs.

Clinical Use

Diarylpyrimidines are used in combination with other antiretroviral drugs as part of highly active antiretroviral therapy (HAART) for the treatment of HIV/AIDS. They are particularly useful in cases where the virus has developed resistance to other NNRTIs.

Side Effects

Common side effects of diarylpyrimidines include rash, nausea, and fatigue. More serious side effects can include liver damage and severe skin reactions.

Research

Research is ongoing into the development of new diarylpyrimidines with improved effectiveness and fewer side effects.

See Also

• Antiretroviral drug
• HIV/AIDS
• Reverse transcriptase
• RNA
• DNA
• Etravirine