New Tenofovir Pro-Drug Offers Less Toxicity


CROI2013On March 6, 2013 The Physician’s Weekly reported that a new Tenofovir Pro-Drug had less potential for bone and kidney toxicity, but still remained efficacious as a treatment for both Hepatitis and HIV infection. The findings were revealed at the 20th Conference on Retroviruses and Opportunistic Infections 2013 in Atlanta, Georgia. Tenofovir is a vastly used nucleotide reverse transcriptase inhibitor analog known in the brands Viread, Truvada and Complera. This novel pro-drug formulation of tenofovir proved to work as well as the existing formula in tests conducted at Stanford University. Led by Andrew Zolopa, he and his colleagues compared both the new tenofovir alafenamide (TAF) in a quadruple regimen versus the current tenofovir disoproxil fumarate in the Stribild coformulation (elvitegravir/cobicistat/tenofovir/emtricitabine). The TAF was determined to show less detrimental effects on markers of renal function as compared to TDF. Additionally, the kidneys showed to be substantially less exposed to this new formulation of tenofovir, with approximately 90% less exposure. These finding are not only exciting, but they also offer promising research opportunities for a safer and more tolerable formula of tenofovir for those patients in great need of this treatment.

Tenofovir 202138-50-9Tenofovir CAS# 202138-50-9 is familiar to many as the brand name Viread, which is marketed by Gilead. With the patent for this powerhouse drug set to expire on July 25, 2017, research and development teams are eagerly awaiting generic opportunities. Tenofovir works as it prevents the HIV infection from altering the genetic material of healthy CD4 cells, which prevents these cells from producing new virus activity in the body. Tenofovir is a Nucleotide Reverse Transcriptase Inhibitor and it also successfully decreases the amount of the HIV virus in the body. Tenofovir has been dispensed by many physicians for the treatment of Hepatitis B, although the FDA has yet to approve tenofovir for this indication. The typical dose of tenofovir is a 300 milligram pill, to be taken once a day. Tenofovir is almost always given alongside other HIV drugs, or in fixed-dose combination tablets such as Truvada (Viread and Emtriva), Atripla (Viread, Emtriva, and Sustiva) and Stribild (Viread, Emtriva, elvitegravir and cobicistat). The FDA does not advise tenofovir to be taken as a monotherapy for the treatment of the HIV infection or AIDS.

Tenofovir (Viread) is unique in that it is active against many strains of HIV that are resistant to longtime therapies like Retrovir (AZT), Zerit (d4T) and Ziagen (abacavir). Severe adverse effects such as lactic acidosis and liver problems are rare. More common side effects of tenofovir include nausea, diarrhea, headache and weakness.

LGM Pharma offers API tenofovir for research and development purposes. Clients can be assured of quality products and continuous support throughout the R&D process.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

  • Share: