A ‘pro-drug’ of tenofovir achieves higher cellular concentrations than the normal formulation of the drug and is more potent, results of a small study show.
A total of 38 people with viral loads of at least 2000 copies/ml were randomised to take one of three doses of the pro-drug, GS-7340; the standard 300mg once-daily dose of tenofovir (Viread); or a placebo. The study lasted for ten days and the participants received no other anti-HIV drugs.
A pro-drug is an inactive drug that is converted into an active therapeutic drug in the body. In this case, people taking the pro-drug achieved greater reductions in viral load, and the 25mg and 40mg doses were superior to the standard dose of tenofovir.
Plasma and cellular concentrations of GS-7340 were also superior.
The pro-drug was well tolerated. There was no evidence that it caused kidney or bone toxicities, known to be side-effects of the current form of tenofovir.
Investigators are hopeful that it will be suitable for co-formulation with other anti-HIV drugs.
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