API Tenofovir Disoproxil Fumarate

Tenofovir Disoproxil Fumarate More Info

Tenofovir Disoproxil Fumarate, commonly abbreviated as TDF, is an oral antiviral medication belonging to the class of nucleotide reverse transcriptase inhibitors (NRTIs). It is widely used in the treatment and prevention of certain viral infections.

Core Medical Uses

Treatment of HIV InfectionTDF is a key component of combination antiretroviral therapy (cART) for human immunodeficiency virus (HIV)-1 infected adults and pediatric patients (with appropriate dosage adjustments). It works by inhibiting the reverse transcriptase enzyme, which HIV relies on to replicate its genetic material and spread within the body. When used in combination with other antiretroviral drugs, it can effectively suppress viral load, slow disease progression, and improve the immune function of patients.

Treatment of Chronic Hepatitis B (CHB)It is approved for the treatment of chronic hepatitis B virus (HBV) infection in adults and adolescents aged 12 years and older with compensated liver function. TDF inhibits HBV DNA polymerase, reducing viral replication, improving liver function indicators, and slowing the progression of liver fibrosis, cirrhosis, and the risk of hepatocellular carcinoma.

Pre-exposure Prophylaxis (PrEP) for HIVFor individuals at high risk of HIV infection (e.g., partners of HIV-positive people, men who have sex with men), TDF (often combined with emtricitabine) is used as PrEP. Daily oral administration can significantly reduce the risk of HIV acquisition through sexual contact or injection drug use.

Mechanism of Action

TDF is a prodrug. After oral administration, it is converted into the active metabolite tenofovir diphosphate in the body. This metabolite competes with natural deoxyadenosine triphosphate (dATP) to integrate into the viral DNA chain during viral replication, thereby terminating DNA chain elongation and inhibiting viral replication.

Key Specifications & Administration

Dosage Form: Film-coated tablets (common strengths: 300 mg per tablet).

Administration: Oral, once daily, with or without food. The dosage is adjusted based on the indication, patient age, and renal function.

Storage: Store at 25°C (77°F), with excursions permitted to 15–30°C (59–86°F). Protect from moisture.

Adverse Effects & Precautions

Common Adverse Effects

Gastrointestinal reactions: Nausea, diarrhea, abdominal pain, flatulence.

Systemic reactions: Headache, fatigue, dizziness.

These symptoms are usually mild and resolve with continued treatment.

Serious Precautions

Renal Toxicity: Long-term use may cause renal impairment (e.g., decreased glomerular filtration rate, Fanconi syndrome). Regular monitoring of serum creatinine and urine protein is required during treatment, especially for patients with pre-existing renal disease.

Bone Toxicity: May lead to decreased bone mineral density, increasing the risk of fractures. Monitoring of bone density is recommended for long-term users.

Lactic Acidosis and Severe Hepatomegaly: A rare but life-threatening adverse reaction, especially in women, obese patients, or those with prolonged nucleoside exposure. Discontinue the drug immediately if symptoms such as unexplained fatigue, nausea, vomiting, and abdominal pain occur.

Contraindications

Hypersensitivity to tenofovir disoproxil fumarate or any component of the formulation.

Pharmaceutical Applications

In the pharmaceutical raw material trade, TDF is a high-demand API (Active Pharmaceutical Ingredient). It requires strict quality control to meet international standards such as USP (United States Pharmacopeia), EP (European Pharmacopoeia), or CP (Chinese Pharmacopoeia) to ensure the safety and efficacy of finished dosage forms.