Islatravir (4′-ethynyl-2-fluoro-2′-deoxyadenosine, EFdA, or MK-8591) is an investigational drug for the treatment of

HIV infection Human immunodeficiency virus infection and acquired immunodeficiency syndrome (HIV/AIDS) is a spectrum of conditions caused by infection with the human immunodeficiency virus (HIV), a retrovirus. Following initial infection an individual ma ...

. It is classified as a nucleoside reverse transcriptase translocation inhibitor (NRTTI).

Merck Merck refers primarily to the German Merck family and three companies founded by the family, including: * the Merck Group, a German chemical, pharmaceutical and life sciences company founded in 1668 ** Merck Serono (known as EMD Serono in the Unite ...

is developing a subdermal drug-eluting implant to administer islatravir.

Biological activity

Islatravir has activity against HIV in

animal model An animal model (short for animal disease model) is a living, non-human, often genetic-engineered animal used during the research and investigation of human disease, for the purpose of better understanding the disease process without the risk of ha ...

s, and is being studied clinically for HIV treatment and prophylaxis. Islatravir is a

nucleoside Nucleosides are glycosylamines that can be thought of as nucleotides without a phosphate group. A nucleoside consists simply of a nucleobase (also termed a nitrogenous base) and a five-carbon sugar (ribose or 2'-deoxyribose) whereas a nucleotide ...

analog

reverse transcriptase A reverse transcriptase (RT) is an enzyme used to generate complementary DNA (cDNA) from an RNA template, a process termed reverse transcription. Reverse transcriptases are used by viruses such as HIV and hepatitis B to replicate their genomes, ...

translocation inhibitor that unlike other such inhibitors, inhibits HIV through multiple mechanisms, providing rapid suppression of the virus, when tested in macaques and mice. Nevertheless, there are HIV strains resistant to islatravir and research is ongoing.

References

{{reflist Nucleoside analog reverse transcriptase inhibitors Ethynyl compounds Fluoroarenes Hydroxymethyl compounds