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Drug information

Drug's link(s)
Generic name

Tenofovir alafenamide

Brand names

Biktarvy, Descovy, Genvoya, Odefsey, Vemlidy, Symtuza

Compound type

Small molecule

Drug class/category

NRTI

Summary

Tenofovir alafenamide (TAF), also known as GS-7340, is a tenofovir prodrug used for HIV-1 treatment and pre-exposure prophylaxis, in addition to chronic hepatitis B treatment. TAF is an alanine ester of tenofovir that provides high levels of intracellular drug concentration with low overall systemic exposure. TAF provides significant advantages over previous generation tenofovir prodrugs such as tenofovir disoproxil fumarate, including a superior pharmacokinetic profile, a higher resistance barrier, enhanced intracellular distribution and an improved safety profile. TAF is available in multiple formulations, including short-acting oral medication (Vemlidy) and combination tablets (Genvoya, Odefsey, Descovy, Biktarvy). Long-acting formulations of TAF are currently in development.

Approval status

Unknown

Regulatory authorities

WHO guidelines July 2025: Preferred NRTI backbones for initial and subsequent regimens: * Tenofovir (tenofovir disoproxil fumarate or tenofovir alafenamide fumarate (TAF)) +lamivudine (3TC) (or emtricitabine (FTC)) is the preferred NRTI backbone for initial and subsequent ART for adults, adolescents and children weighing more than 30 kg. This includes individuals previously treated with or exposed to tenofovir or zidovudine (ZDV). * Abacavir + 3TC or TAF + 3TC (or FTC) is the suggested NRTI backbone for subsequent ART for children weighing less than 30 kg. This includes children previously treated with ABC or ZDV.

Therapeutic area(s)

  • HIV
Use case(s)
  • Pre-Exposure Prophylaxis (PrEP)

Administration route

Oral, Subcutaneous

Associated long-acting platforms

Polymeric implant, Titanium implant

Use of drug

Ease of administration
  • Administered by a nurse
  • Administered by a specialty health worker
Frequency of administration

Not provided

User acceptance
Not provided

Dosage

Available dose and strength

Not provided

Maximum dose

Not provided

Recommended dosing regimen

Not provided

Additional comments

Not provided

Dosage link(s)

Not provided

Additional information

Not provided

Developer(s)

Gilead
Originator
United States

Gilead

Gilead Sciences, Inc. is a multinational biopharmaceutical company that develops and manufactures innovative medicines for life-threatening diseases, including anti-viral therapeutics for HIV/AIDS, Hepatitis B, Hepatitis C and Covid-19. Headquartered in Foster City, California, Gilead was originally founded in 1987 and is currently listed on both the S&P 500 and the NASDAQ Biotechnology Index.

Drug structure

Scale-up and manufacturing prospects

Scale-up prospects

Not provided

Tentative equipment list for manufacturing

Not provided

Manufacturing

Not provided

Specific analytical instrument required for characterization of formulation

Thermal stability characterization via thermogravimetric analysis and differential scanning calorimetry to the implantable, dissolving and/or pure drug formulations. Drug crystallinity can be tested using a powder diffractometer (e.g. Miniflex X-ray from Rigaku Coporation). Drug stability and quantification are determined using HPLC (e.g. SphereClone™ C18 ODS (length, 150 mm; particle size, 5 μm; pore size, 80 Å; internal diameter, 4.6 mm). In vitro drug release studied via dialysis membrane bags (e.g. Spectra-Por®, 12,000–14,000 MWCO, Spectrum Medical Industries, Los Angeles, CA, USA).

Excipients & delivery device(s)

Proprietary excipients used

Not provided

Novel excipients or existing excipients at a concentration above Inactive Ingredient Database (IID) for the specified route of administration

Not provided

Residual solvents used

Not provided

Delivery device(s)

Several pre-clinical implant devices are currently in development for Tenofovir Alafenamide HIV PrEP. These include but are not limited to; [1] OCIS-001 consisting of a permeable polyurethane membrane developed by Northwestern University currently in Phase I/II trials, [2] Titanium reservoir containing nanochannels housed in a silicon membrane created by the Houston Methodist Research Institute, [3] Non-permeable silicone reservoir implant from the Oak Crest Institute of Science, and [4] a biodegradable poly(ε-caprolactone) reservoir implant developed by RTI International.

Safety, Efficacy and Evidence Summary

Safety

Not provided

Efficacy

Not provided

Evidence Summary

Not provided

References and relevant studies

Not provided