Tenofovir was patented in 1996 and approved for use in the United States in 2001.
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10 Facts About Tenofovir
2.
Tenofovir disoproxil is used for HIV-1 infection and chronic hepatitis B treatment.
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3.
Tenofovir disoproxil is generally well tolerated with low discontinuation rates among the HIV and chronic hepatitis B population.
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4.
Tenofovir lacks a hydroxyl group in the position corresponding to the 3' carbon of the dAMP, preventing the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation.
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5.
Tenofovir disoproxil is a prodrug that is quickly absorbed from the gut and cleaved to release tenofovir.
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6.
Tenofovir is mainly excreted via the kidneys, both by glomerular filtration and by tubular secretion using the transport proteins OAT1, OAT3 and ABCC4.
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7.
Tenofovir is a derivative of adenine and this was the chemical starting point for its first published synthesis which was included in patents to the compound.
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8.
Tenofovir is formed when the diethyl phosphonate group is converted to its acid using trimethylsilyl chloride in the presence of sodium bromide, a further refinement of the original manufacturing route.
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9.
Tenofovir was initially synthesized by Antonin Holy at the Institute of Organic Chemistry and Biochemistry of the Czechoslovak Academy of Sciences in Prague.
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10.
Tenofovir disoproxil is available in pills which combine a number of antiviral drugs into a single dose.
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