Table 1.
FDA approved nucleoside reverse transcriptase inhibitors for the treatment of HIV
| Generic name (abbreviation) | Brand name | Manufacturer | IC‐50 (nM) | Bioavailability (%) | Elimination half‐life (hr) | Plasma protein binding (%) | CSF‐plasma ratio (%) | Dosage form | Adult dosage | Approval year |
|---|---|---|---|---|---|---|---|---|---|---|
| Abacavir (ABC) | Ziagen | ViiV Healthcare | 70–5,800 | 83 | 1.54 ± 0.63 | ∼50 | 30 | Tablet, oral solution | 300 mg twice daily or 600 mg once daily | 1998 |
| Didanosine (ddl or enteric‐coated didanosine ddl EC) | Videx | Bristol‐Myers Squibb | 10–10,000 | 42 | 1.5 ± 0.4 | <5 | 21 | Powder (oral solution) | 125–200 mg twice daily or 250–400 mg once daily | 1991 |
| Videx EC | Bristol‐Myers Squibb | 10–10,000 | 42 | 1.19 ± 0.21 | <5 | 21 | capsule | 200–400 mg once daily | 2000 | |
| Emtricitabine (FTC) | Emtriva | Gilead Sciences, Inc | 2–30 | 93 (capsule) 75 (solution) | ∼10 | <4 | 26 | Capsule, oral solution | 200 mg once daily (capsules) 240 mg once daily (solution) | 2003 |
| Lamivudine (3TC) | Epivir | ViiV Healthcare | 2–670 | 86 (tablet) 87 (solution) | 5–7 | <36 | 15 | Tablet, oral solution | 150 mg twice daily or 300 mg once daily | 1995 |
| Stavudine (d4T) | Zerit | Bristol‐Myers Squibb | 9–4,000 | 86.4 | 1.6 ± 0.23 | <5 | 40 | Capsule, powder | 30–40 mg twice daily | 1994 |
| Tenofovir disoproxil fumarate (TDF) | Viread | Gilead Sciences, Inc | 2–7 | 25 | ∼17 | 7.2 | 5 | Powder, tablet | 300 mg once daily | 2001 |
| Tenofovir alafenamide (TAF) | Vemlidy | Gilead Sciences, Inc | 5 (EC50) | 80 |
0.51 (plasma) 150–180 (cellular) |
80 | ND | Tablet | 25 mg once daily | 2016 (for combo therapy) |
| Zidovudine (AZT or ZDV) | Retrovir | ViiV Healthcare | 10–48 | 64 | 0.5–3 | <38 | 60 | Capsule, sirup, injection | 300 mg twice daily (oral) or 1 mg per kg every 4 hr (infusion) | 1987 |