NRTI (chain terminator)
Nucleoside/nucleotide reverse-transcriptase inhibitor (chain terminator)
- Host kinases make the triphosphate; viral RT incorporates it; no 3′-OH, so the DNA chain ends
- Competes at the active site — HIV-1, HIV-2 and (several) HBV
- Mitochondrial polymerase-γ inhibition underlies the older agents’ lactic acidosis, lipoatrophy and neuropathy; tenofovir adds renal tubular and bone effects
- Host kinases make the triphosphate; viral RT incorporates it; no 3′-OH, so the DNA chain ends
- Competes at the active site — HIV-1, HIV-2 and (several) HBV
- Mitochondrial polymerase-γ inhibition underlies the older agents’ lactic acidosis, lipoatrophy and neuropathy; tenofovir adds renal tubular and bone effects
Drugs with this mechanism (7)
- Abacavir — NRTI requiring HLA-B*5701 screening to prevent potentially fatal hypersensitivity.
- Didanosine — Older HIV nucleoside reverse-transcriptase inhibitor; pancreatitis, neuropathy, and mitochondrial toxicity limit its usefulness.
- Emtricitabine — Well-tolerated NRTI forming a backbone of HIV treatment and prevention regimens.
- Entecavir — Potent hepatitis B nucleoside analog with a high barrier to resistance.
- Lamivudine — Well-tolerated NRTI active against both HIV and hepatitis B.
- Tenofovir — Nucleotide reverse-transcriptase inhibitor; a backbone of HIV and PrEP therapy.
- Zidovudine — Older HIV nucleoside reverse-transcriptase inhibitor; useful in selected perinatal settings, but anemia and mitochondrial toxicity limit routine use.
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