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Tenofovir disoproxil | CAS No: 201341-05-1 | GMP-certified suppliers
A medication that supports treatment of HIV‑1 infection, helps manage chronic hepatitis B, and contributes to HIV prevention when used in appropriate combination regimens.
Therapeutic categories
Primary indications
- Tenofovir disoproxil is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in patients ≥2 years old and weighing ≥10 kg
- It is also indicated for the treatment of chronic hepatitis B in patients ≥2 years old and weighing ≥10 kg
- Tenofovir disoproxil is also an ingredient in several combination products, all of which are indicated either alone or in combination with other antiretrovirals for the treatment of HIV-1 infection
Product Snapshot
- Tenofovir disoproxil is an oral small‑molecule API supplied mainly as film‑coated tablets and powders
- It is used in antiretroviral combinations for HIV‑1 treatment, chronic hepatitis B therapy, and in fixed‑dose combinations for HIV‑1 prevention
- It is approved in the US, EU, and Canada, with some presentations also noted as investigational
Clinical Overview
After administration, tenofovir disoproxil is rapidly hydrolyzed to tenofovir and then phosphorylated intracellularly to tenofovir diphosphate. The active metabolite competitively inhibits HIV‑1 reverse transcriptase and hepatitis B polymerase by mimicking the natural deoxyadenosine triphosphate substrate. Incorporation into viral DNA results in chain termination. Reduced susceptibility has been associated with the K65R substitution in HIV‑1 reverse transcriptase.
Tenofovir demonstrates in vitro antiviral activity across laboratory and clinical HIV‑1 isolates, with EC50 values ranging from 0.04 to 8.5 micromolar depending on cell type and viral strain. Additive or synergistic effects have been observed in combination with several nucleoside, non‑nucleoside, and protease inhibitor antiretrovirals, supporting its use in multidrug regimens.
Tenofovir is characterized by low plasma protein binding and predominant renal elimination via glomerular filtration and active tubular secretion, including transport through OAT1 and OAT3. Dose adjustment may be required in cases of reduced renal function. Prolonged exposure has been associated with nephrotoxicity and decreases in bone mineral density, and monitoring of renal parameters is recommended in routine clinical use. Drug interactions may occur with agents affecting renal transport pathways.
Well‑known usage contexts include Viread and several fixed‑dose antiretroviral combinations.
For API procurement, suppliers should demonstrate control of prodrug and fumarate salt quality attributes, including stereochemical integrity, impurity profiles, and residual solvent levels. Consistent particle size and stability data are important for ensuring reliable formulation performance and regulatory compliance.
Identification & chemistry
| Generic name | Tenofovir disoproxil |
|---|---|
| Molecule type | Small molecule |
| CAS | 201341-05-1 |
| UNII | F4YU4LON7I |
| DrugBank ID | DB00300 |
Pharmacology
| Summary | Tenofovir disoproxil is a prodrug converted intracellularly to tenofovir diphosphate, a nucleotide analog that competitively inhibits HIV‑1 reverse transcriptase and hepatitis B polymerase. By blocking incorporation of natural nucleotides, it terminates viral DNA chain elongation and reduces productive replication. Its activity focuses on suppression of HIV‑1 and HBV through targeted inhibition of these essential viral enzymes. |
|---|---|
| Mechanism of action | Tenofovir belongs to a class of antiretroviral drugs known as nucleotide analog reverse transcriptase inhibitors (NtRTIs), which block reverse transcriptase, an enzyme necessary for viral production in HIV-infected individuals. This enables the management of HIV viral load through decreased viral replication [FDA label]. Tenofovir disoproxil fumarate is the fumarate salt of the prodrug _tenofovir disoproxil_. Tenofovir disoproxil is absorbed and converted to its active form, _tenofovir_, a nucleoside monophosphate (nucleotide) analog. Tenofovir is then converted to the active metabolite, _tenofovir diphosphate_, a chain terminator, by constitutively expressed enzymes in the cell. Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and the Hepatitis B polymerase by direct binding competition with the natural deoxyribonucleotide substrate (deoxyadenosine 5’-triphosphate) and, after integration into DNA, causes viral DNA chain termination , [FDA label]. **A note on resistance** HIV-1 isolates with decreased susceptibility to tenofovir have been identified in cell culture studies. These viruses expressed a _K65R_ substitution in reverse transcriptase and showed a 2– 4 fold decrease in susceptibility to treatment with tenofovir [FDA label]. |
| Pharmacodynamics | This drug prevents viral DNA chain elongation through inhibition of enzymes necessary for host cell infection viral replication in HIV-1 and Hepatitis B infections , . **In vitro effects** The antiviral activity of tenofovir against in laboratory and clinical isolates of HIV-1 was studied in lymphoblastoid cell lines, primary monocyte/macrophage cells, in addition to peripheral blood lymphocytes. The EC50 (50% effective concentration) values of tenofovir against HIV-1 virus ranged between 0.04 μM to 8.5 μM. **Combination of tenofovir disoproxil with other drugs** In drug combination studies of tenofovir with nucleoside reverse transcriptase inhibitors (abacavir, didanosine, lamivudine, stavudine, zalcitabine, zidovudine), non-nucleoside reverse transcriptase inhibitors (delavirdine, efavirenz, nevirapine), and protease inhibitors (amprenavir, indinavir, nelfinavir, ritonavir, saquinavir), additive and synergistic effects were seen. Tenofovir demonstrated antiviral activities in cell cultures against HIV-1 [FDA label]. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | inhibitor |
| DNA polymerase/reverse transcriptase | HBV-D | inhibitor |
ADME / PK
| Absorption | After oral administration of tenofovir disoproxil to patients with HIV infection, tenofovir disoproxil is quickly absorbed and metabolized to tenofovir . Administration of tenofovir disoproxil 300 mg tablets after a high-fat meal increases the oral bioavailability of this drug, as demonstrated by an increase in tenofovir AUC0-∞ of about 40% as well as an increase in Cmax of about 14%. On the contrary, the administration of tenofovir disoproxil with a light meal did not exert a relevant effect on the pharmacokinetics of tenofovir when compared to administration under fasting conditions. The presence of ingested food slows the time to tenofovir Cmax by approximately 1 hour. Cmax and AUC of tenofovir are 0.33 ± 0.12 μg/mL and 3.32 ± 1.37 μg•hr/mL after several doses of tenofovir disoproxil 300 mg once daily in the fed state when meal content is not controlled [FDA label]. |
|---|---|
| Half-life | When a single oral dose is given, the terminal elimination half-life is approximately 17 hours [FDA label]. |
| Protein binding | _In vitro_ binding of tenofovir to human plasma or serum proteins is <0.7 and <7.2%, respectively, over the tenofovir concentration range 0.01 to 25 μg/mL [FDA label]. |
| Metabolism | Tenofovir disoproxil fumarate is the fumarate salt of the prodrug _tenofovir disoproxil_. Tenofovir disoproxil is absorbed and converted to its active form, _tenofovir_, a nucleoside monophosphate (nucleotide) analog. Tenofovir is then converted to the active metabolite, _tenofovir diphosphate_, a chain terminator, by constitutively expressed enzymes in the cell [FDA label]. Two phosphorylation steps are required to convert tenofovir disoproxil to the active drug form . The cytochrome P450 enzyme system is not involved with the metabolism of tenofovir disoproxil or tenofovir [FDA label]. |
| Route of elimination | Following IV administration of tenofovir, approximately 70–80% of the dose is recovered in the urine as unchanged tenofovir within 72 hours of dosing. Tenofovir is eliminated by a combination of glomerular filtration and active tubular secretion [FDA label]. There may be competition for elimination with other compounds that are also eliminated by the kidneys. |
| Volume of distribution | The volume of distribution at steady-state is 1.3 ± 0.6 L/kg and 1.2 ± 0.4 L/kg, following intravenous administration of tenofovir 1.0 mg/kg and 3.0 mg/kg [FDA label]. After oral administration of tenofovir disoproxil, tenofovir is distributed to the majority tissues with the highest concentrations measured in the kidney, liver and the intestinal contents (based on data from preclinical studies) . |
| Clearance | The clearance of tenofovir is highly dependent on renal function and may vary greatly. Total clearance has been estimated to be approximately 230 ml/h/kg (approximately 300 ml/min) . On average, renal clearance has been estimated to be approximately 160 ml/h/kg (approximately 210 ml/min), which is in excess of the glomerular filtration rate. This shows that active tubular secretion is an essential part of the elimination of tenofovir . The FDA label provides specific guidelines for dosing according to renal function. It is important to consult product labeling before administering tenofovir to individuals with renal dysfunction, as the clearance of this drug may vary greatly among these patients [FDA label]. |
Formulation & handling
- Tenofovir disoproxil is an orally administered small‑molecule prodrug formulated primarily as tablets or granules, with modest aqueous solubility that may influence excipient selection for dissolution enhancement.
- The prodrug is moisture‑ and hydrolysis‑sensitive, requiring dry‑granulation or controlled‑humidity processing and protective packaging to limit degradation.
- Suitable for solid oral dosage forms only; film coating is commonly used to improve stability and handling of the hygroscopic API.
Regulatory status
| Lifecycle | Most key patents for this API expired between 2017 and 2018 in Canada and the United States, indicating a mature IP landscape. With products marketed in Canada, the US, and the EU, the API is likely in the late lifecycle phase with broad generic availability. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Tenofovir disoproxil is produced by a single originator, with a broad network of repackagers and distributors supporting supply across the US, EU, and Canada. Branded and combination products are widely available in all three regions, indicating established global market penetration. Core patents in the US and Canada have expired, supporting the presence of existing generic competition. |
|---|
Safety
| Toxicity | **A note on breastfeeding** The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers not breast-feed their infants to prevent postnatal transmission of HIV-1. Mothers should be advised not to breast-feed if they are receiving tenofovir disoproxil [FDA label]. **Carcinogenesis** Long-term oral carcinogenicity studies of tenofovir disoproxil fumarate in mice and rats were performed at exposures up to approximately 16 times (mice) and 5 times (rats) those observed in humans at the therapeutic dose for HIV-1 infection. At the higher dose in female mice, liver adenomas were increased at exposures 16 times that in humans. In rats, the study was negative for carcinogenic findings at exposures up to 5 times that observed in humans at the therapeutic dose [FDA label]. **Pregnancy** This drug is considered a pregnancy Category B drug. Reproduction studies have been performed in rats and rabbits at doses up to 14 and 19 times the recommended human dose based on body surface area comparisons and revealed no evidence of impaired fertility or harm to the fetus due to tenofovir. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not consistently reflective of human effects, tenofovir disoproxil should be used during pregnancy only if clearly required. To monitor fetal outcomes of pregnant women taking tenofovir disoproxil, an Antiretroviral Pregnancy Registry has been formed. Healthcare providers are encouraged and advised to register patients by calling the number listed on the FDA label for tenofovir disoproxil [FDA label]. **Mutagenesis** Tenofovir disoproxil fumarate was mutagenic in the in vitro mouse lymphoma assay and negative for mutagenesis in an in vitro bacterial mutagenicity test (Ames test). In an in vivo mouse micronucleus assay, tenofovir disoproxil fumarate was negative when administered to male mice. **Impairment of Fertility** There were no observed effects on fertility, mating performance or early embryonic development when tenofovir disoproxil fumarate was given to male rats at a dose comparable to 10 times the human dose based on body surface area comparisons for 28 days before mating and to female rats for 15 days before mating through day seven of gestation. There was, however, changes in the estrous cycle in female rats [FDA label]. |
|---|
- High-dose animal studies showed increased liver adenomas in female mice at exposures far exceeding human therapeutic levels, indicating a potential for dose‑dependent hepatic tumorigenicity in rodent models
- Tenofovir disoproxil fumarate demonstrated mutagenicity in an in vitro mouse lymphoma assay, though results were negative in bacterial and in vivo micronucleus systems
- Reproductive toxicology evaluations revealed estrous cycle alterations in female rats at high exposures, despite no observed impairment of fertility or early embryonic development
US Drug Master File (USDMF)
A US Drug Master File (USDMF) is a confidential document submitted to the U.S. Food and Drug Administration (FDA) that provides detailed information about the manufacturing process of an Active Pharmaceutical Ingredient (API) or a finished pharmaceutical product. This document includes comprehensive details such as chemical properties, manufacturing facilities, production processes, packaging specifications, storage conditions, and more.
The USDMF ensures that proprietary information remains protected while allowing the FDA to review the data as part of drug approval processes. Unlike other types of DMFs used in different regions, the USDMF is specifically designed to meet the regulatory requirements set by the FDA, ensuring compliance with U.S. standards.
Tenofovir is a type of Antivirals
Antivirals are a crucial subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a pivotal role in combating viral infections. These specialized compounds are designed to inhibit the growth and replication of viruses within the human body.
Antivirals target various stages of the viral life cycle, including viral attachment, entry, and replication. They can interfere with viral enzymes, block viral receptors, or disrupt viral protein synthesis. By doing so, antivirals effectively suppress the viral infection, reduce symptoms, and improve patient outcomes.
The development of antiviral APIs requires extensive research and scientific expertise. Pharmaceutical companies employ cutting-edge technologies to identify potential antiviral compounds, screen their efficacy, and optimize their therapeutic properties. The most promising candidates undergo rigorous testing in preclinical and clinical trials to ensure their safety and effectiveness.
Antivirals have proven to be indispensable in the management of various viral infections, such as influenza, HIV, hepatitis B and C, herpes, and respiratory syncytial virus (RSV). They not only provide symptomatic relief but also prevent viral transmission and reduce the risk of complications.
With the ongoing global concern over emerging viral diseases and the impact of pandemics, the demand for effective antiviral therapies continues to rise. Pharmaceutical companies and researchers are actively exploring new avenues, such as broad-spectrum antivirals and novel drug delivery systems, to enhance the antiviral arsenal.
In conclusion, antiviral APIs are vital components of the pharmaceutical industry, offering hope in the fight against viral infections. Through continuous innovation and research, these substances contribute to improving public health by mitigating the impact of viral diseases.
Tenofovir (Antivirals), classified under Anti-infective Agents
Anti-infective agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various infectious diseases. These agents play a crucial role in combating bacterial, viral, fungal, and parasitic infections. The demand for effective anti-infective APIs has grown significantly due to the increasing prevalence of drug-resistant microorganisms.
Anti-infective APIs encompass a wide range of substances, including antibiotics, antivirals, antifungals, and antiparasitics. Antibiotics are particularly important in fighting bacterial infections and are further categorized into different classes based on their mode of action and target bacteria. Antivirals are designed to inhibit viral replication and are essential in the treatment of viral infections such as influenza and HIV. Antifungals combat fungal infections, while antiparasitics are used to eliminate parasites that cause diseases like malaria and helminthiasis.
The development and production of high-quality anti-infective APIs require stringent manufacturing processes and adherence to regulatory standards. Pharmaceutical companies invest heavily in research and development to discover new and more effective anti-infective agents. Additionally, ensuring the safety, efficacy, and stability of these APIs is of utmost importance.
The global market for anti-infective APIs is driven by factors such as the rising incidence of infectious diseases, the emergence of new and drug-resistant pathogens, and the growing demand for improved healthcare infrastructure. Continuous advancements in pharmaceutical technology and the development of innovative drug delivery systems further contribute to the expansion of this market.
In conclusion, anti-infective agents are a critical category of pharmaceutical APIs that play a pivotal role in treating infectious diseases. Their effectiveness in combating various types of infections makes them essential components in the arsenal of modern medicine.
Tenofovir API manufacturers & distributors
Compare qualified Tenofovir API suppliers worldwide. We currently have 21 companies offering Tenofovir API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Acebright Pharma | Producer | India | India | CoA, USDMF | 9 products |
| Apino Pharma Co., Ltd. | Producer | China | China | CoA, GMP, USDMF, WC | 229 products |
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hangzhou Coben Pharmaceut... | Producer | China | China | CoA, GMP, ISO9001 | 7 products |
| Hetero Labs | Producer | India | India | CoA, GMP, USDMF, WC | 90 products |
| Laurus Labs | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 50 products |
| Lupin | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 155 products |
| Mangalam Drugs & Organics... | Producer | India | India | CoA, GMP, WC | 10 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| Mylan | Producer | India | India | CoA, KDMF, USDMF, WC | 201 products |
| Qilu Antibiotics | Producer | China | China | CoA, USDMF | 33 products |
| Shandong Zhanhua Yonghao | Producer | China | China | CoA | 10 products |
| Shanghai Acebright | Producer | China | China | CoA | 23 products |
| Shanghai Desano Chem. | Producer | China | China | CoA, USDMF, WC | 22 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Shilpa Medicare Ltd | Producer | India | India | CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC, WHO-GMP | 54 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 757 products |
| Suzhou Lixin Pharmaceutic... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 34 products |
| Zhejiang Candorly | Producer | China | China | CoA, USDMF | 2 products |
| Zhejiang Supor | Producer | China | China | CoA, EDMF/ASMF, GMP, USDMF | 13 products |
When sending a request, specify which Tenofovir API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Tenofovir API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Tenofovir API
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Technical
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Regulatory
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