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Etravirine | CAS No: 269055-15-4 | GMP-certified suppliers
A medication that treats HIV-1 infection in treatment-experienced patients aged two years and older, used in combination with other antiretroviral agents to manage resistant viral strains.
Therapeutic categories
Primary indications
- Etravirine is indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection in treatment-experienced patients ≥2 years of age
Product Snapshot
- Etravirine is an oral small molecule formulated as tablets
- It is primarily used in combination regimens for the treatment of HIV-1 infection in treatment-experienced patients aged two years and older
- The product holds approval status in key regulatory markets including the US, EU, and Canada
Clinical Overview
Pharmacologically, etravirine acts by directly binding to the HIV-1 reverse transcriptase enzyme, thereby inhibiting both DNA-dependent and RNA-dependent polymerase activities essential for viral replication. This mechanism specifically targets the viral enzyme without inhibiting human DNA polymerases alpha, beta, or gamma. Clinical trials have reported no significant prolongation of the QT interval following short-term dosing.
Key pharmacokinetic considerations include its interaction with cytochrome P450 enzymes, notably CYP2C19, CYP2C9, and CYP3A4, where etravirine functions both as a substrate and modulates enzyme activity through induction and inhibition. It also affects P-glycoprotein transporters, which may influence drug distribution and disposition.
Safety profiles identify common adverse reactions such as mild to moderate rash during the first six weeks of therapy, nausea, diarrhea, and peripheral neuropathy. Postmarketing surveillance highlighted severe hypersensitivity reactions including Stevens-Johnson syndrome, toxic epidermal necrolysis, and erythema multiforme, prompting updates to warnings and precautions. Additionally, immune reconstitution-related autoimmune disorders such as Graves’ disease, polymyositis, and Guillain-Barré syndrome have been reported.
Etravirine’s chemical classification places it among diarylethers, characterized by two aryl groups connected via an ether linkage. From a sourcing perspective, procurement of etravirine active pharmaceutical ingredient requires rigorous quality control to ensure purity and consistency, given its complex synthesis and the critical role in managing resistant HIV infections. Compliance with international regulatory standards and verification of manufacturing processes are essential to support global distribution and clinical use.
Identification & chemistry
| Generic name | Etravirine |
|---|---|
| Molecule type | Small molecule |
| CAS | 269055-15-4 |
| UNII | 0C50HW4FO1 |
| DrugBank ID | DB06414 |
Pharmacology
| Summary | Etravirine is a non-nucleoside reverse transcriptase inhibitor that targets the HIV-1 reverse transcriptase enzyme by binding directly to inhibit its DNA- and RNA-dependent polymerase activities. It selectively inhibits viral reverse transcriptase without affecting human DNA polymerases alpha, beta, or gamma. Its primary pharmacodynamic effect is suppression of HIV-1 replication through interference with viral Gag-Pol polyprotein processing. |
|---|---|
| Mechanism of action | Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1). It directly binds reverse transcriptase and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma. |
| Pharmacodynamics | Clinical trials have shown no prolongation of QT intervals on electrocardiograms after 8 days of dosing. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gag-Pol polyprotein | ||
| Gag-Pol polyprotein | ||
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | Maximum oral absorption is achieved in 2.5-4 hours. Absorption is unaffected by the concomitant use of oral ranitidine or omeprazole, which decrease gastric acidity. Administration under fasting conditions resulted in a near 50% decrease in systemic exposure (AUC) when compared to administration after a meal. |
|---|---|
| Half-life | Half life of 9.05-41 hours. |
| Protein binding | Plasma protein binding is about 99.9% in vitro. In vitro, 99.6% is bound to albumin, and 97.66% - 99.02% is bound to 1-alpha glycoprotein. |
| Metabolism | Metabolized (in vitro) by the liver CYP450 enzymes: CYP3A4, CYP2C9, CYP2C19. The major metabolites formed by a methyl hydroxylation of the dimethylbenzonitrile moiety retained less than 90% of etravirine's activity. |
| Route of elimination | After a 800mg dose of radio-labelled etraverine, 93.7% was found to undergo fecal elimination, with 81.2% - 86.4% eliminated unchanged. 1.2% of the dose was renally eliminated, changed. Etravirine is dialyzable (hemodialysis). |
| Volume of distribution | Distribution of etravirine into compartments other than plasma has not been evaluated in humans. |
| Clearance | Renal clearance of etravirine is negligible (<1.2%), thus no dose adjustments are required in patients with renal impairment. Clearance is shown to be reduced in patients with Hepatitis B and/or co-infection, however, the safety profile of etravirine does not call for dosage adjustments. |
Formulation & handling
- Etravirine is a small molecule intended for oral administration in tablet form.
- Bioavailability is enhanced when taken post-meal, indicating potential food-dependent absorption.
- Metabolism is affected by CYP3A modulators; avoid grapefruit products and St. John's Wort during handling and formulation considerations.
Regulatory status
| Lifecycle | The API is in a mature market phase with key patents expired in the US and Canada between 2019 and 2021, while one patent remains active in Canada until mid-2027. This allows for generic competition primarily in the US and EU, with some patent protection still potentially affecting the Canadian market. |
|---|
| Markets | US, EU, Canada |
|---|
Supply Chain
| Supply chain summary | Etravirine is manufactured by a limited number of originator companies with branded products available across the US, EU, and Canadian markets. Patent expirations in the US and Canada between 2019 and 2027 indicate that some patents have already expired while others are due to expire soon, supporting the presence of existing and upcoming generic competition. The current supply landscape is influenced by these patent timelines across multiple jurisdictions. |
|---|
Etravirine is a type of Anti HIV
The Anti-HIV pharmaceutical API subcategory encompasses a range of active pharmaceutical ingredients (APIs) specifically designed to combat the human immunodeficiency virus (HIV), which causes acquired immunodeficiency syndrome (AIDS). These APIs play a vital role in the development of effective antiretroviral therapy (ART) regimens used to manage and treat HIV infections.
The primary objective of Anti-HIV APIs is to target the various stages of the HIV life cycle, inhibiting viral replication and reducing the viral load in the patient's body. These APIs typically act through mechanisms such as reverse transcriptase inhibition, protease inhibition, integrase inhibition, and fusion inhibition.
Common Anti-HIV APIs include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), integrase inhibitors (INIs), and fusion inhibitors. Each class of API targets different stages of the virus's replication cycle, thereby preventing its spread and reducing the viral load.
These APIs undergo rigorous testing and are subject to strict regulatory guidelines to ensure their safety and efficacy. Pharmaceutical companies and research institutions employ advanced techniques like high-performance liquid chromatography (HPLC), mass spectrometry, and nuclear magnetic resonance (NMR) to analyze the purity, potency, and quality of Anti-HIV APIs.
The development and production of Anti-HIV APIs require expertise in synthetic organic chemistry, process optimization, and quality control. Pharmaceutical manufacturers must adhere to stringent quality standards, good manufacturing practices (GMP), and follow international guidelines to ensure the consistent production of high-quality Anti-HIV APIs.
Overall, Anti-HIV APIs are crucial components in the development of effective antiretroviral medications, playing a vital role in managing HIV infections and improving the quality of life for millions of people living with HIV/AIDS.
Etravirine (Anti HIV), 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.
Etravirine API manufacturers & distributors
Compare qualified Etravirine API suppliers worldwide. We currently have 9 companies offering Etravirine API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Acura Labs | Producer | India | India | CoA, GMP | 18 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Hetero Labs | Producer | India | India | CoA, USDMF | 90 products |
| Janssen Pharma | Producer | Belgium | Unknown | CoA, GMP, USDMF | 63 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| MSN Life Sciences | Producer | India | India | CoA, USDMF, WC | 46 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Shanghai Acebright | Producer | China | China | CoA | 23 products |
| Zhejiang Hengkang Pharmac... | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 31 products |
When sending a request, specify which Etravirine 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 Etravirine 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.
