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| Pronunciation | /ˌtəˈnoʊfəvɪərˌæləˈfɛnəmaɪd/ |
| Trade names | Vemlidy |
| Other names | GS-7340 |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Protein binding | ~80%[6] |
| Eliminationhalf-life | 0.51 hour |
| Excretion | Feces (31.7%), urine (<1%) |
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| Chemical and physical data | |
| Formula | C21H29N6O5P |
| Molar mass | 476.474 g·mol−1 |
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Tenofovir alafenamide, sold under the brand nameVemlidy, is anantiviral medication used againsthepatitis B andHIV. It is used for the treatment ofchronic hepatitis B virus (HBV) infection in adults withcompensated liver disease[8] and is given in combination with other medications for the prevention and treatment of HIV. It is takenby mouth.[6]
Tenofovir alafenamide is anucleotide reverse transcriptase inhibitor and is aprodrug oftenofovir. It was developed byGilead Sciences based on theprotide technology of Chris McGuigan and is applied in the form of tenofovir alafenamidefumarate (TAF). Closely related to the commonly used reverse-transcriptase inhibitortenofovir disoproxil fumarate (TDF), TAF has greater antiviral activity and better distribution intolymphoid tissues than that agent.[9][10] It was approved for use in the US for HIV in 2015,[11] and for hepatitis B in 2016.[12] Although the USFood and Drug Administration (FDA) has approved tenofovir alafenamide for manufacture as ageneric medication,[13] it is not available.[14]
Gilead announced aPhase III clinical trial evaluating a single-tablet regimen combining tenofovir alafenamide withcobicistat,emtricitabine andelvitegravir[45] and developed a coformulation of the drug with cobicistat, emtricitabine and theprotease inhibitordarunavir.[46][47][48] In a 48-week study comparingelvitegravir/cobicistat/emtricitabine/tenofovir disoproxil (Stribild) to elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (Genvoya), the results showed the newer drug's effects to be non-inferior to the established agent, but at much lower dosages and with lower incidence of adverse side effects such as impaired kidney function.[49][50][51] The FDA approved the TAF-based treatment regimen for treatment of HIV-1 in November 2015.[11] Genvoya is the first TAF-based regimen to receive approval.[11]
