Apricitabine 160707-69-7

History

It was first developed by BioChem Pharma (where it was called BCH10618). BioChem Pharma was then sold to Shire Pharmaceuticals (where apricitabine was called SPD754). Shire then sold the rights to develop the drug to Avexa Pharmaceuticals, an Australian pharmaceutical company. , and has been granted fast track status by the United States Food and Drug Administration. Avexa announced its decision to end work on apricitabine in May 2010, which Avexa spent more than A$100 million ($90 million) developing and was in the final of three stages of patient studies usually needed for U. S. regulatory approval. The pill was designed to be taken twice a day, putting it at a disadvantage to Gilead Sciences Inc. s once-daily Truvada, the worlds top-selling AIDS drug. (May 10 (Bloomberg))

Dosage

As a monotherapy, 1200 mg apricitabine per day reduced the viral load by up to 1. 65 logs (45 fold) in a small, 10-day randomized controlled trial. In a six-month trial, common adverse effects were nausea, diarrhea, elevated blood levels of triglycerides, and upper respiratory infection—similar to those of lamivudine; apricitabine was not associated with abnormal lipase levels, bone marrow suppression, or liver and kidney toxicity. No patients in either study had to stop taking apricitabine because of side effects.

Drug resistance

In vitro, apricitabine was effective against NRTI-(lamivudine and zidovudine)-resistant viruses. In early studies, no mutations causing drug resistance were observed. Newer trials showed that apricitabine may induce K65R mutations, resulting in resistance against didanosine and tenofovir.