Elvucitabine is a new nucleoside reverse transcriptase inhibitor (NRTI) under development by Achillion Pharmaceuticals. It is also known as ACH-126,443 and its chemical name is beta-L-Fd4C.

Test tube studies have shown that elvucitabine is active against viruses which are resistant to other NRTIs. The drug has been tested against clinical isolates bearing all the key NRTI resistance mutations (M41L, M184V, T215Y, Q151M and 69SS), and showed no loss of sensitivity as measured by the IC₅₀.

In vitro studies have also looked at the impact of elvucitabine on mitochondrial DNA. It caused no mitochondrial toxicity, and reduced the level of mitochondrial damage caused by d4T (stavudine, Zerit) when the two drugs were combined.

Elvucitabine is a strong candidate for once daily dosing, with a half-life of more than 24 hours.

Elvucitabine is also active against hepatitis B virus (HBV). Phase II studies are currently evaluating elvucitabine in patients chronically infected with HBV, patients with chronic HBV infection that is resistant to 3TC (lamivudine, Epivir), and HIV-infected patients who have developed resistance to 3TC.

References

Dunkle LM et al. ACH-126,443: a new nucleoside analog with potent activity against wild type and resistant HIV-1 and a promising pharmacokinetic and mitochondrial safety profile. Eighth Annual Conference on Retroviruses and Opportunistic Infections, abstract 303, 2001.