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RX BIN: 015558
RX PCN: HT
Group ID: DDN6600
Card Holder ID: DDN6600

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2018 Price of Tenofovir alafenamide

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What is Tenofovir alafenamide

Tenofovir alafenamide fumarate (TAF) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir. Following oral administration, TAF is converted in vivo to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5 -monophosphate. Tenofovir mimics normal DNA building blocks but is lacking a 3′-OH molecule required for phosphodiester bond linkage. By competing with regular nucleotides for incorporation into proviral DNA and prevention of the formation of the 5′ to 3′ phosphodiester linkage required for DNA elongation, tenofovir causes early chain termination and prevents proviral DNA transcription. Although tenofovir (available as tenofovir disoproxil fumarate) has a good safety profile and efficacy, and is currently a cornerstone of HIV antiviral treatment, its use has been associated with nephrotoxicity and reduced bone mineral density. In comparison, TAF has been shown to have improved antiviral efficacy, enhanced delivery of TFV into peripheral blood mononuclear cells (PBMCs) and lymphatic tissues, a higher barrier to resistance, and an improved safety profile. Improved renal safety is likely attributable to lower circulating plasma concentrations of tenofovir and therefore less exposure and damage to bone and the kidneys, where tenofovir is metabolized. Because HIV antiretroviral therapy is usually life-long, reduced toxicity and improved efficacy results in better patient outcomes and improved adherence in the long term. Tenofovir alafenamide fumarate is currently available in two fixed dose combination products: Odefsey (emtricitabine, rilpivirine, and tenofovir alafenamide), and Descovy (emtricitabine and tenofovir alafenamide). Both products are indicated for the treatment of HIV-1 infection in adults and pediatric patients 12 years of age and older.

Tenofovir alafenamide mechanism of action

Tenofovir alafenamide fumarate (TAF) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir. Following oral administration, TAF is converted in vivo to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5 -monophosphate. Tenofovir mimics normal DNA building blocks but is lacking a 3′-OH molecule required for phosphodiester bond linkage. By competing with regular nucleotides for incorporation into proviral DNA and prevention of the formation of the 5′ to 3′ phosphodiester linkage required for DNA elongation, tenofovir causes early chain termination and prevents proviral DNA transcription.

Dosage forms of Tenofovir alafenamide

FormRouteStrength
Tabletoral
Prescription Generics

false

International Brands

Descovy

Synonyms

bis{9-[(2R,5S,7E)-2,7,10-trimethyl-5,8-dioxo-5-phenoxy-3,9-dioxa-6-aza-5 5-phosphaundecan-1-yl]-9H-purin-6-aminium} (2E)-but-2-enedioate bis{propan-2-yl N-[(S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl]-L-alaninate} (2E)-but-2-enedioate

Manufacturers

Gilead Sciences Canada Inc

CAS number

379270-37-8

UNII

EL9943AG5J

State

solid

Affected organisms

Indication of Tenofovir alafenamide

For use in the treatment of HIV infection and chronic hepatitis B.

Toxicity of Tenofovir alafenamide

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