spec sheet6 rows
Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor used against HIV and against chronic hepatitis B.
- One of the genuinely great drugs of the last thirty years
- The backbone of HIV therapy for decades
- Also the backbone of chronic hepatitis B suppression
- Terminates the growing viral DNA chain
- The older and cheaper tenofovir ester
- TDF is an oral prodrug: it is hydrolysed to tenofovir and then phosphorylated to tenofovir diphosphate, which terminates both HIV-1 reverse transcriptase and HBV polymerase; one of very few agents active against both viruses (PMID 16421366, PMID 19052126).
- iPrEx established oral pre-exposure prophylaxis: 2,499 HIV-negative men and transgender women randomised to TDF/emtricitabine or placebo saw a 44% reduction in HIV incidence (95% CI 15-63, p=0.005), and detectable drug levels correlated strongly with protection; drug was found in only 51% of seronegative and 9% of seroconverting participants [3].
- Partners PrEP showed TDF alone works, not just the combination: among 4,747 serodiscordant heterosexual couples, TDF monotherapy reduced HIV-1 incidence by 67% (95% CI 44-81) and TDF/FTC by 75% (95% CI 55-87), with no significant difference between them [4].
- Against adefovir in chronic hepatitis B, TDF produced no detectable resistance mutations at 48 weeks and higher rates of HBsAg loss (3% vs 0%, p=0.02) [2].
- The renal and bone toxicity of TDF is dose-driven by plasma tenofovir exposure; tenofovir alafenamide delivers the same intracellular active metabolite at roughly a tenth of the plasma exposure, which is why the two prodrugs are not interchangeable in patients with renal impairment or osteoporosis.
Mechanism
It is a of tenofovir, an acyclic nucleotide analogue of monophosphate; once diphosphorylated inside the cell it is incorporated by viral reverse transcriptase and terminates the growing DNA chain, because it has no 3' hydroxyl for the next base to attach to. The disoproxil ester delivers far higher plasma tenofovir than the newer alafenamide ester, which is why it carries more renal tubular toxicity and bone density loss.
receptor fingerprint
HIV-1 reverse transcriptase (RT, pol)Competitive inhibition and obligate DNA chain termination by the active metabolite tenofovir diphosphate
Hepatitis B virus DNA polymerase / reverse transcriptaseInhibition and chain termination
Renal proximal tubule organic anion transporters OAT1/OAT3 (SLC22A6/SLC22A8) and MRP4 effluxSubstrate; intracellular accumulation drives mitochondrial injury
Bone mineral metabolism (secondary to renal phosphate wasting)Indirect bone mineral density loss
Safetyrisks and cautions, not medical advice
an antiretroviral: taken without HIV and hepatitis B testing and renal monitoring it breeds resistance, and stopping it abruptly in someone with hepatitis B can cause a dangerous hepatic flare
Where to buy
Suppliers
Vendors carrying Tenofovir Disoproxil Fumarate, with live product details and codes. Links are affiliate links that support the wiki at no cost to you.
RUPharma🌐
Tenofovir Disoproxil Fumarate
Research
- 2006first citedTenofovir DF, emtricitabine, and efavirenz vs. zidovudine, lamivudine, and efavirenz for HIV
- 2012most recentAntiretroviral prophylaxis for HIV prevention in heterosexual men and women
- 1.Tenofovir DF, emtricitabine, and efavirenz vs. zidovudine, lamivudine, and efavirenz for HIV
- 2.Tenofovir disoproxil fumarate versus adefovir dipivoxil for chronic hepatitis B
- 3.Preexposure chemoprophylaxis for HIV prevention in men who have sex with men
- 4.Antiretroviral prophylaxis for HIV prevention in heterosexual men and women
4 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
Notes and cautions
- TDF carries a US boxed warning for post-treatment severe acute exacerbation of hepatitis B: hepatic function must be monitored for at least several months after stopping the drug in anyone co-infected with HBV, and reinitiation may be required.
- When TDF-containing products are used for PrEP there is an additional boxed warning about the risk of drug-resistant HIV-1 if the drug is started in someone with undiagnosed HIV-1 infection, so a negative HIV test is mandatory before initiation and at regular intervals.
- The characteristic chronic toxicities are renal; proximal tubulopathy, Fanconi syndrome and progressive eGFR decline; and reduced bone mineral density; both require baseline and periodic monitoring of renal function, phosphate and urine protein.
- Older labelling also carried a lactic acidosis and severe hepatomegaly with steatosis warning for the nucleoside/nucleotide class.