NNRTI (allosteric)
Non-nucleoside reverse-transcriptase inhibitor (allosteric)
- Binds a hydrophobic pocket beside the active site and distorts it — non-competitive, no activation step
- HIV-1 only; a single mutation (K103N, Y181C) can defeat the whole first generation
- CYP3A induction (efavirenz, nevirapine) and CNS effects are class features; rilpivirine needs gastric acid
- Binds a hydrophobic pocket beside the active site and distorts it — non-competitive, no activation step
- HIV-1 only; a single mutation (K103N, Y181C) can defeat the whole first generation
- CYP3A induction (efavirenz, nevirapine) and CNS effects are class features; rilpivirine needs gastric acid
Drugs with this mechanism (5)
- Doravirine — NNRTI with a cleaner lipid and CNS profile than efavirenz.
- Efavirenz — Non-nucleoside reverse-transcriptase inhibitor; vivid dreams and neuropsychiatric effects.
- Etravirine — Second-generation NNRTI retaining activity against common resistance mutations.
- Nevirapine — Non-nucleoside reverse-transcriptase inhibitor; rash and hepatotoxicity.
- Rilpivirine — NNRTI requiring a meal and normal gastric acid for absorption.
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