テノホビル CAS:147127-20-6

Tenofovir is hardly absorbed through the gastrointestinal tract, for this reason, prodrug of Tenofovir has been developed by esterification, and then to make tenofovir fumarate ester. Tenofovir ester is water-soluble, can be rapidly absorbed and degraded into the active tenofovir, and then was metabolized to the active Tenofovir disoproxil. Tenofovir will reach the peak of plasma Concentration within 1-2 h after administration. When combined with food service, the bioavailability of Tenofovir can be increased by 40%. Intracellular half-life of Tenofovir disoproxil is about 10 h, it needs dosing everyday. Because Tenofovir is not a CYP-450 substrate, this may decrease the possibility of interactions with other drugs caused by CYP450. Elimination of Tenofovir is by glomerular filtration and active tubular secretion. Approximately 70% に 80% is recovered in urine as unchanged drug. Elimination half-life is approximately 17 h.

1. Antiviral drugs, Tenofovir is an acyclic nucleoside antiviral reverse transcriptase inhibitor. The active substance is Tenofovir disoproxil, while tenofovir is a prodrug that is used because of its better absorption in the gut.

2. Tenofovir can inhibit viral polymerase through direct competitively combine with natural deoxyribose or by insertion to terminate chain of human DNA. It is the first nucleotide analogs to treat HIV-1 infection that approved by the US Food and Drug Administration (FDA).

3. Tenofovir is a main medicine in AIDS cocktail therapy, researches has shown that it can effectively improve the monkeys` ability on prevention of immunodeficiency virus (similar to the human AIDS virus).