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Ethionamide | CAS No: 536-33-4 | GMP-certified suppliers
A medication that treats pulmonary and extrapulmonary tuberculosis resistant to first-line drugs, providing bacteriostatic activity against Mycobacterium tuberculosis in multidrug regimens.
Therapeutic categories
Primary indications
- For use in the treatment of pulmonary and extrapulmonary tuberculosis when other antitubercular drugs have failed
Product Snapshot
- Ethionamide is an oral small molecule formulated primarily as film-coated and coated tablets
- It is indicated for the treatment of pulmonary and extrapulmonary tuberculosis, especially in cases where other antitubercular agents have failed
- The product is approved for marketing in the US
Clinical Overview
Pharmacologically, ethionamide exhibits bacteriostatic activity against Mycobacterium tuberculosis. Its efficacy has been demonstrated in preclinical models where oral administration reduced viable bacterial loads in infected tissues. However, resistance can develop when ethionamide is used as monotherapy, emphasizing the importance of combination regimens with other agents such as streptomycin or isoniazid to mitigate resistance emergence.
The mechanism of action of ethionamide involves inhibition of mycolic acid synthesis, a critical component of the mycobacterial cell wall. Structurally related to isoniazid and classified as a nicotinic acid derivative, ethionamide undergoes intracellular activation. It is believed to exert its antimycobacterial effect by targeting InhA, the enoyl-acyl carrier protein reductase of M. tuberculosis. The drug forms a covalent adduct with the NAD cofactor, creating a tight-binding inhibitor that disrupts the enzymatic activity necessary for mycolic acid biosynthesis.
Key pharmacokinetic data include oral bioavailability and tissue distribution adequate for systemic antimycobacterial activity. Pharmacodynamic responses vary depending on the concentration achieved at the infection site and the susceptibility profile of the mycobacterial strain.
From a safety and toxicity perspective, ethionamide is associated with adverse effects that require monitoring, including hepatotoxicity and potential neurological effects. It also can cause photosensitivity reactions. These safety considerations necessitate careful clinical supervision during therapy.
Ethionamide is approved internationally and categorized among anti-bacterial agents targeting mycobacteria, specifically as a fatty acid synthesis inhibitor. It is utilized mainly in multidrug-resistant tuberculosis contexts and specialized leprosy treatment protocols.
For pharmaceutical API sourcing, quality assurance must ensure compliance with current Good Manufacturing Practices (cGMP) and pharmacopeial standards. Given ethionamide’s chemical characteristics and clinical use, APIs should be evaluated for purity, consistency, and absence of impurities or degradation products that could impact efficacy or safety in finished formulations.
Identification & chemistry
| Generic name | Ethionamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 536-33-4 |
| UNII | OAY8ORS3CQ |
| DrugBank ID | DB00609 |
Pharmacology
| Summary | Ethionamide is a nicotinic acid derivative that exhibits bacteriostatic or bactericidal activity against Mycobacterium tuberculosis by inhibiting mycolic acid synthesis, a critical component of the bacterial cell wall. It undergoes intracellular activation and forms a covalent adduct with the NAD cofactor, competitively inhibiting InhA, an enoyl- reductase essential for mycolic acid production. This mechanism disrupts bacterial cell wall integrity, contributing to its antitubercular effects, particularly in cases resistant to other therapies. |
|---|---|
| Mechanism of action | Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of infection and the susceptibility of the infecting organism. Ethionamide, like prothionamide and pyrazinamide, is a nicotinic acid derivative related to isoniazid. It is thought that ethionamide undergoes intracellular modification and acts in a similar fashion to isoniazid. Isoniazid inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. Specifically isoniazid inhibits InhA, the enoyl reductase from <i>Mycobacterium tuberculosis</i>, by forming a covalent adduct with the NAD cofactor. It is the INH-NAD adduct that acts as a slow, tight-binding competitive inhibitor of InhA. |
| Pharmacodynamics | Ethinamate is bacteriostatic against <i>M. tuberculosis</i>. In a study examining ethionamide resistance, ethionamide administered orally initially decreased the number of culturable <i>Mycobacterium tuberculosis</i> organisms from the lungs of H37Rv infected mice. Drug resistance developed with continued ethionamide monotherapy, but did not occur when mice received ethionamide in combination with streptomycin or isoniazid. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis | inhibitor |
| Catalase-peroxidase | Mycobacterium tuberculosis | other/unknown |
ADME / PK
| Absorption | Essentially completely absorbed following oral administration and not subjected to any appreciable first pass metabolism. Bioavailability approximately 100%. |
|---|---|
| Half-life | 2 to 3 hours |
| Protein binding | Approximately 30% bound to proteins. |
| Metabolism | Hepatic and extensive. Metabolized to the active metabolite sulfoxide, and several inactive metabolites. The sulphoxide metabolite has been demonstrated to have antimicrobial activity against <i>Mycobacterium tuberculosis</i>. |
| Route of elimination | Less than 1% of the oral dose is excreted as ethionamide in urine. Ethionamide is extensively metabolized to active and inactive metabolites. |
| Volume of distribution | * 93.5 L [healthy volunteers] |
Formulation & handling
- Ethionamide is a small molecule oral API available as coated tablets suitable for solid dosage form development.
- The API exhibits moderate water solubility and low lipophilicity, favoring formulation for oral absorption.
- It can be administered with or without food; however, taking with food may alleviate gastrointestinal side effects, informing patient counseling.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is approaching patent expiry in the United States, leading to increased availability of generic formulations. This transition contributes to a more mature and competitive market landscape. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Ethionamide is primarily manufactured by a single originator company, with multiple packagers involved in distributing branded products. Its presence is mainly concentrated in the US market under the brand name Trecator. Patent expiration indicates the potential for existing or imminent generic competition in this therapeutic area. |
|---|
Safety
| Toxicity | Symptoms of overdose include convulsions, nausea, and vomiting. |
|---|
- Overdose may result in convulsions, nausea, and vomiting
- Handle with appropriate precautions
- Avoid exposure routes that could lead to systemic toxicity
Ethionamide is a type of Antituberculars
Antituberculars are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of tuberculosis (TB). TB is a highly contagious infectious disease caused by the bacteria Mycobacterium tuberculosis, primarily affecting the lungs but also capable of affecting other organs. Antitubercular APIs play a crucial role in eradicating and controlling this global health concern.
These APIs exhibit powerful antimicrobial properties specifically targeting Mycobacterium tuberculosis. They act by inhibiting the growth and replication of the bacteria, preventing the spread of the infection. Antitubercular APIs are often used in combination therapies to maximize efficacy and minimize the development of drug resistance.
Common antitubercular APIs include isoniazid, rifampicin, pyrazinamide, ethambutol, and streptomycin. These APIs are typically administered orally or through injectable formulations, allowing for effective delivery and distribution throughout the body.
The development and production of antitubercular APIs require stringent quality control measures to ensure safety and efficacy. Pharmaceutical companies adhere to Good Manufacturing Practices (GMP) guidelines and rigorous regulatory standards to guarantee the production of high-quality APIs.
In conclusion, antitubercular APIs play a critical role in the treatment and control of tuberculosis. By effectively targeting and inhibiting the growth of Mycobacterium tuberculosis, these APIs contribute to reducing the burden of this infectious disease worldwide. Their development and production follow strict quality control standards to ensure safe and efficacious treatment options for patients.
Ethionamide API manufacturers & distributors
Compare qualified Ethionamide API suppliers worldwide. We currently have 3 companies offering Ethionamide 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 |
|---|---|---|---|---|---|
| Liaoning Beiqi | Producer | China | China | CoA, JDMF | 1 products |
| Orgapharm | Producer | France | France | CoA, GMP, USDMF | 9 products |
| Pen Tsao Chemical Industr... | Producer | Germany | China | CoA | 18 products |
When sending a request, specify which Ethionamide 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 Ethionamide 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.
