Islatravir triphosphate – CAS 950913-56-1

Description

Islatravir triphosphate is synthesised by Sigut Labs (Prague, Czech Republic). Islatravir (EFdA, or MK-8591) is an investigational drug for the treatment of HIV infection developed by company Merck. It is classified as a nucleoside reverse transcriptase translocation inhibitor (NRTTI).  Islatravir has activity against HIV in animal models and is being studied clinically for HIV treatment and prophylaxis. Islatravir is a nucleoside analogue reverse transcriptase translocation inhibitor that, unlike other such inhibitors, inhibits HIV through multiple mechanisms, providing rapid suppression of the virus, when tested in macaques and mice.  Islatravir inhibits HIV reverse transcriptase but has a different mechanism of action with respect to all other approved NRTIs because of its unique structural features: a 3’-hydroxyl group makes this nucleotide a translocation inhibitor rather than a chain terminator. Introducing a 4’-ethynyl group enhances the selectivity towards the HIV reverse transcriptase. Similarly to other nucleoside antiviral drugs, Islatravir is first transformed to islatravir-5’-triphosphate (ISL-TP), which is the biologically active form of Islatravir. When ITP is incorporated into forming DNA strand by the reverse transcriptase, it acts as a chain terminator by preventing the translocation.

Based on its unique properties, Merck is currently developing a sub-dermal implant for the long-term release of Islatravir. This implant is now under clinical evaluation and is likely to cause a revolution in HIV treatment. You can find more information about Islatravir in our article.

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References

• Schürmann, D., Rudd, D. J., Zhang, S., De Lepeleire, I., Robberechts, M., Friedman, E., … & Matthews, R. P. (2020). Safety, pharmacokinetics, and antiretroviral activity of islatravir (ISL, MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor, following single-dose administration to treatment-naive adults infected with HIV-1: an open-label, phase 1b, consecutive-panel trial. The lancet HIV, 7(3), e164-e172.
• Michailidis, E., Huber, A. D., Ryan, E. M., Ong, Y. T., Leslie, M. D., Matzek, K. B., … & Sarafianos, S. G. (2014). 4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) inhibits HIV-1 reverse transcriptase with multiple mechanisms. Journal of Biological Chemistry, 289(35), 24533-24548.
• Michailidis, E., Marchand, B., Kodama, E. N., Singh, K., Matsuoka, M., Kirby, K. A., … & Sarafianos, S. G. (2009). Mechanism of inhibition of HIV-1 reverse transcriptase by 4′-ethynyl-2-fluoro-2′-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor. Journal of biological chemistry, 284(51), 35681-35691.