Etravirine

Definition

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV-1. It works by binding to and inhibiting the reverse transcriptase enzyme, preventing viral replication.

5 Must Know Facts For Your Next Test

1. Etravirine is specifically effective against HIV-1 strains that are resistant to first-generation NNRTIs.
2. It is commonly used in combination with other antiretroviral agents as part of a highly active antiretroviral therapy (HAART).
3. Etravirine binds to the reverse transcriptase enzyme at an allosteric site, causing conformational changes that reduce enzyme activity.
4. Common side effects include rash, nausea, and diarrhea, but it is generally well tolerated.
5. The drug has a high genetic barrier to resistance, meaning it requires multiple mutations in the virus for resistance to develop.

Review Questions

• How does etravirine inhibit HIV-1 replication?
• What makes etravirine effective against strains resistant to first-generation NNRTIs?
• What are some common side effects associated with etravirine use?

Related terms

Reverse Transcriptase Inhibitor (RTI): A class of antiretroviral drugs that inhibit the action of reverse transcriptase, an enzyme crucial for viral replication.

Highly Active Antiretroviral Therapy (HAART): A treatment regimen for HIV infection that uses a combination of three or more antiretroviral drugs.

Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI): A subclass of RTIs that non-competitively bind to reverse transcriptase and inhibit its function without mimicking nucleotides.