 | |
| Names | |
|---|---|
| IUPAC name 2′-Deoxy-4′-ethynyl-2-fluoroadenosine | |
| Systematic IUPAC name (2R,3S,5R)-5-(6-Amino-2-fluoro-9H-purin-9-yl)-2-ethynyl-2-(hydroxymethyl)oxolan-3-ol | |
| Other names EFdA; MK-8591; 4′-Ethynyl-2-fluoro-2′-deoxyadenosine | |
| Identifiers | |
3D model (JSmol) | |
| ChemSpider | |
| UNII | |
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| Properties | |
| C12H12FN5O3 | |
| Molar mass | 293.258 g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
Islatravir (4′-ethynyl-2-fluoro-2′-deoxyadenosine,EFdA, orMK-8591) is an investigational drug for the treatment ofHIV infection.[1] It is classified as anucleoside reverse transcriptase translocation inhibitor (NRTTI).[2]Merck isdeveloping a subdermal drug-eluting implant to administer islatravir.[3][4]
In 2021,FDA placed a partial clinical hold for several studies under Islatravir.[5] The reason was a decline in CD4 T cells under therapy. Merck announced to restart the study program in 2023 with a decreased dose, however studies of islatravir forpre-exposure prophylaxis (PrEP) will be discontinued.[6]
In 2024, results from a phase II study combining islatravir withlenacapavir indicated that the regimen shows promise as a possible weekly oral regimen.[7]
Islatravir has activity against HIV inanimal models,[8] and is being studied clinically for HIV treatment and prophylaxis.[9] Islatravir is anucleoside reverse transcriptase translocation inhibitor (NRTTI) that unlike other such inhibitors, inhibits HIV through multiple mechanisms,[8] providing rapid suppression of the virus, when tested in macaques and mice.[10] Nevertheless, there are HIV strains resistant to islatravir and research is ongoing.[11][12]
