Basic Chemical Information:

• Chemical Name: Tenofovir Alafenamide Hemifumarate

• Molecular Formula: C23H31O7N6P (for Tenofovir Alafenamide) + C4H4O4 (for Hemifumarate)

• Molecular Weight: 534.514 g/mol (for Tenofovir Alafenamide) + 116.07 g/mol (for Hemifumarate)

• CAS Number: 1392275-56-7 (for Tenofovir Alafenamide)

  
  

Pharmacological Action:

Tenofovir Alafenamide Hemifumarate is an antiviral medication used for the treatment of HIV-1 infection and chronic hepatitis B. It is a prodrug of tenofovir, which means that it is converted into the active drug, tenofovir, within the body. The primary mechanisms of action are:

1. Nucleotide Reverse Transcriptase Inhibitor      (NRTI):

• Tenofovir alafenamide is metabolized to tenofovir diphosphate inside HIV-infected cells.

• Tenofovir diphosphate acts as a competitive  inhibitor for HIV-1 reverse transcriptase (RT).

• It incorporates into viral DNA during replication,  leading to chain termination and preventing further DNA synthesis.

2. Increased Plasma Stability and Enhanced Delivery:

• Compared to its predecessor, Tenofovir Disoproxil  Fumarate (TDF), Tenofovir Alafenamide (TAF) is more stable in plasma  which allows for lower dosing.

• TAF is taken up more effectively by cells, allowing  for higher intracellular concentrations of the active form, tenofovir diphosphate, thus reducing systemic exposure and potential renal and bone  toxicities.