Table 1.
Common name | Abbrev. | Structural name | Natural analog | Year FDA approved | Common resistance mutations selected b | Mechanism of resistance |
---|---|---|---|---|---|---|
zidovudine | ZDV, AZT | β-d-(+)-3′-azido-3′-deoxythymidine | dTTP | 1987 | M41L, D67N, K70R, L210W, T215F/Y, K219Q/E | excision |
didanosine | ddI | β-d-(+)-2′,3-dideoxyinosine | dATP | 1991 | K65R, L74V | discrimination |
stavudine | d4T | β-d-(+)-2′,3′-didehydro-3′-deoxythymidine | dTTP | 1994 | M41L, D67N, K70R, L210W, T215F/Y, K219Q/E | excision |
lamivudine | 3TC | β-l-(−)-2′,3′-dideoxy-3′-thiacytidine | dCTP | 1995 | K65R, M184V/I | discrimination |
abacavir | ABC | (1S,4R)-4-[2-amino-6-(cyclopropyl-amino)-9H-purin-9-yl]-2-cyclopentene-1-methanol succinate | dGTP | 1998 | K65R, L74V, Y115F, M184V | discrimination |
tenofovirc | TFV | ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonic acid | dATP | 2001 | K65R, K70E | discrimination |
emtricitabine | FTC | β-l-(−)-2′,3′-dideoxy-5-fluoro-3′-thiacytidine | dCTP | 2003 | K65R, M184V/I | discrimination |
All NRTIs shown are approved by the U.S. Food and Drug Administration (FDA). Zalcitabine (ddC), which is not currently in use, is also FDA approved;
From the current listing of mutations associated with antiretroviral drug resistance compiled by the International AIDS Society—USA, Drug Resistance Mutations Group [19];
Prodrug is tenofovir disoproxil fumarate (TDF).