Table 3.
FDA approved non‐nucleoside reverse transcriptase inhibitors, including Efavirenz, Etravirine, Nevirapine, and Rilpivirine
| 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| Efavirenz (EFV) | Sustiva | Bristol‐Myers Squibb | 3–9 | 50 | 52–76 | 99.5 | 0.26–1.19 | Capsule, tablet | 600 mg once daily | 1998 |
| Etravirine (ETR) | Intelence | Janssen Pharmaceuticals, Inc. | 1–5 | ND | ∼41 | 99.9 | ND | Tablet | 200 mg twice daily | 2008 |
| Nevirapine (NVP and extended‐release nevirapine NVP XR) | Viramune | Boehringer Ingelheim | 10–100 | 93 (tablet) 91 (solution) | 25 ‐ 30 | ∼60 | 45 | Tablet, oral suspension | 200 mg twice daily | 1996 |
| Viramune XR | Boehringer Ingelheim | 10–100 | 80–94 | 25–30 | ∼60 | 45 | Tablet | 400 mg once daily | 2011 | |
| Rilpivirine (RPV) | Edurant | Janssen Pharmaceuticals, Inc. | 42 | ND | ∼50 | 99.7 | ND | Tablet | 25 mg once daily | 2011 |
| Enfuvirtide (T‐20) | Fuzeon | Hoffman‐La Roche; Genentech | 0.1–1,700 | 84 (subcutaneous injection) | 3.8 ± 0.6 | 92 | UD | Subcutaneous injection | 90 mg twice daily | 2003 |
| Ibalizumab | Trogarzo | TaiMed Biologics USA Corp. | 53 | NA | 2.7–64 (dose dependent) | ND | ND | Intravenous injection | 800 mg every two weeks | 2018 |
| Maraviroc (MVC) | Selzentry | ViiV Healthcare | 0.1–4.5 | 23–33 | 14–18 | 76 | 2.8 | Tablet, oral solution | 150, 300, or 600 mg twice daily (depending on combination therapeutics) | 2007 |
| Bictegravir (BIC) | Biktarvy | Gilead Sciences, Inc | 7.5 | ND | 14.9–20.9 | >99 | ND | Tablet | 50 mg once daily (in combination with 200 mg FTC and 25 mg TAF) | 2018 (for combo therapy) |
| Elvitegravir (EVG) | Vitekta | Gilead Sciences, Inc | 44 | ND | 8.7 | 98–99 | ND | Tablet | 85 or 150 mg once daily (depending on combination therapeutics) | 2014 |
| Dolutegravir (DTG) | Tivicay | ViiV Healthcare | 2.7–12.6 | ND | 14 | 98.9 | 0.11–0.66 | Tablet | 50 mg once daily or 50 mg twice daily (depending on past and combinedtherapeutics) | 2013 |
| Raltegravir (RAL) | Isentress | Merck and Co., Inc. | 6–50 (IC95) | ND | 9 | 83 | 5.8 | Tablet, oral suspension | 400 mg twice daily or 1200 mg once daily | 2007 |
| Isentress HD | Merck and Co., Inc. | 6–50 (IC95) | ND | 9 | 83 | 5.8 | Tablet | 400 mg twice daily or 1200 mg once daily | 2017 |