Last updated : 25 oct 2025 | 06:18 AM (IST)
Tenofovir was first synthesized by Antonín Holý in Prague and initially shown to have activity against herpes viruses. In 1985, its anti-HIV activity was discovered in collaboration with Erik De Clercq. Gilead Sciences later partnered to explore its use in HIV treatment. The original form had poor oral absorption, so Gilead developed a prodrug, tenofovir disoproxil, which improved bioavailability. It was approved in the U.S. in 2001 for HIV and 2008 for hepatitis B.
Tenofovir Disoproxil Fumarate 300 mg is used to treat HIV-1 infection in combination with other antiretroviral medicines and to manage chronic hepatitis B infection. It is also used for HIV prevention (PrEP) in individuals at high risk of exposure.
Tenofovir disoproxil blocks the viral reverse transcriptase enzyme needed for HIV and hepatitis B to replicate. Once converted to its active form in the body, it gets inserted into viral DNA and stops further DNA formation, preventing the virus from multiplying.
Tenofovir disoproxil fumarate is taken by mouth as a tablet once daily, with or without food.
Tenofovir disoproxil fumarate may cause nausea, diarrhea, headache, dizziness, fatigue, or abdominal discomfort. Less common but serious risks include kidney problems, reduced bone density, lactic acidosis, and liver enlargement. Long-term treatment may require monitoring of kidney and bone health.
Tenofovir disoproxil fumarate should not be used by individuals allergic to the drug. Caution is needed in patients with kidney problems or bone disorders, as it may worsen renal function and reduce bone density. In HIV and hepatitis B co-infection, stopping the drug may cause hepatitis flare-ups. Monitoring of kidney and liver function is recommended, especially when used with other medicines that affect the kidneys.
Tenofovir disoproxil fumarate is an effective once-daily antiviral used to treat and prevent HIV-1 and chronic hepatitis B. It is generally well-tolerated but requires monitoring of kidney and bone health during long-term use. With proper precautions, it remains an important treatment option worldwide.
TDF and TAF are both prodrugs of tenofovir but differ in pharmacokinetics. TAF delivers tenofovir more efficiently into cells at lower doses, resulting in less systemic exposure, which reduces the risk of renal and bone toxicity compared to TDF.
Baseline serum creatinine, eGFR, and serum phosphate should be assessed before initiation. During therapy, renal function should be monitored periodically, especially in patients at risk of kidney impairment or those receiving nephrotoxic drugs.
TDF should be used with caution in patients with renal impairment. Dose adjustment is required based on creatinine clearance, and TAF may be preferred due to its better renal safety profile.
TDF is associated with a reduction in bone mineral density (BMD), particularly in children and adolescents or with long-term use. Dual-energy X-ray absorptiometry (DEXA) scans may be considered in high-risk patients.
Yes, TDF is highly effective in suppressing HBV DNA levels and is a preferred agent for chronic hepatitis B. However, discontinuation can lead to HBV reactivation, so hepatic function must be monitored post-therapy.
TDF is classified as safe during pregnancy and is recommended as part of antiretroviral therapy for pregnant women with HIV to reduce perinatal transmission. It is also considered safe for HBV-infected pregnant women when indicated.
TDF may interact with nephrotoxic agents (e.g., aminoglycosides, NSAIDs), boosted protease inhibitors (which may increase tenofovir levels), and didanosine (increases risk of toxicity). Always review the patient’s medication profile for interactions.
Information provided is for educational purposes only and should not replace professional medical advice. Always consult your doctor before use.
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