- Raw materials
- Antibacterials
- Fidaxomicin
Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Fidaxomicin API Manufacturers & Suppliers
5 verified results
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Commercial-scale Suppliers
All certificates
Employees: 10+
All certificates
Employees: 50+
All certificates
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Fidaxomicin | CAS No: 873857-62-6 | GMP-certified suppliers
A medication that treats Clostridioides difficile-associated diarrhea in adults and children, reducing infection recurrence while preserving normal intestinal microbiota balance.
Therapeutic categories
Primary indications
- Fidaxomicin is indicated for the treatment of _Clostridioides_ (formerly _Clostridium_) _difficile_-associated diarrhea in adult and pediatric patients 6 months of age and older
- Fidaxomicin should only be used in patients with proven or strongly suspected _C
- Difficile_ infection to reduce the risk of development of drug-resistant bacteria and maximize the therapeutic effectiveness of fidaxomicin and other antimicrobial agents
Product Snapshot
- Fidaxomicin is an oral small molecule available in tablet and granule for suspension formulations
- It is primarily used for the treatment of Clostridioides difficile-associated diarrhea
- Fidaxomicin is approved for use in the US, Canada, and the EU
Clinical Overview
Pharmacologically, fidaxomicin is derived from natural fermentation and possesses a unique 18-membered lactone ring structure. It exhibits a narrow spectrum of antibacterial activity, primarily targeting gram-positive anaerobes with potent bactericidal effects against C. difficile. The agent acts by inhibiting bacterial RNA polymerase, an enzyme essential for the initiation of transcription and bacterial gene expression. Specifically, fidaxomicin binds to the DNA template-RNA polymerase complex, preventing strand separation necessary for mRNA synthesis, thereby disrupting bacterial transcription and leading to cell death. Its activity is time-dependent rather than concentration-dependent.
Key pharmacodynamic parameters reveal minimum inhibitory concentration values (MIC90) against C. difficile ranging from 0.0078 to 2 μg/mL in vitro, demonstrating greater potency compared to vancomycin, the prior standard of care. Unlike vancomycin, fidaxomicin minimally affects the normal colonic microbiota, which supports its narrow spectrum profile and potentially reduces the risk of dysbiosis associated with CDI treatment. Fidaxomicin metabolism involves hydrolysis to its active metabolite OP-1118 after oral administration.
Safety considerations emphasize that fidaxomicin should be prescribed only for confirmed or strongly suspected C. difficile infection to limit the emergence of resistant strains and maintain therapeutic efficacy. Resistance to rifamycins or other common antimicrobial classes does not confer cross-resistance to fidaxomicin, underscoring its distinct mechanism of action.
For pharmaceutical formulation and global sourcing, the fidaxomicin active pharmaceutical ingredient (API) requires rigorous quality control due to its complex macrocyclic structure and fermentation-derived nature. Consistency in purity, stability, and activity must be ensured, with attention to potential impurities arising from fermentation processes. Suppliers should comply with current Good Manufacturing Practice (cGMP) standards and provide comprehensive documentation to meet regulatory requirements for antimicrobial agents used in CDI therapy.
Identification & chemistry
| Generic name | Fidaxomicin |
|---|---|
| Molecule type | Small molecule |
| CAS | 873857-62-6 |
| UNII | Z5N076G8YQ |
| DrugBank ID | DB08874 |
Pharmacology
| Summary | Fidaxomicin is a narrow-spectrum bactericidal agent targeting RNA polymerase sigma factors in Clostridioides difficile, inhibiting the initiation of bacterial transcription by preventing DNA strand separation and mRNA synthesis. Its selective activity disrupts C. difficile gene expression while sparing much of the normal gut flora. Fidaxomicin exhibits time-dependent killing with minimal cross-resistance to other antibiotic classes. |
|---|---|
| Mechanism of action | _Clostridium difficile_ is a Gram-positive bacterium that causes various gastrointestinal complications, such as antibiotic-associated diarrhea. _C. difficile_ infection can be caused by antibiotic therapy, resulting in the disruption of the human gut flora leads to an overgrowth of _C. difficile_. The consequences of _C. difficile_ infection can be mild to severe and sometimes fatal. Fidaxomicin gets hydrolyzed to its active metabolite, OP-1118, upon oral administration. Both compounds mediate a bactericidal activity against _C. difficile_ by inhibiting bacterial RNA polymerase at the initiation phase of the transcription cycle. The RNA polymerase is an essential bacterial enzyme that regulates gene expression, catalyzes nucleic acid interactions, and promotes several bacterial enzymatic reactions critical for bacterial survival. The core RNA polymerase is composed of a complex of different subunits and contains the active site. To initiate bacterial transcription, the active site of the core RNA polymerase binds to a promoter-specificity σ initiation factor, which locates and binds to a promoter region of the DNA. The DNA-RNA polymerase interaction promotes subsequent steps of transcription, which involves the separation of DNA strands. Fidaxomicin binds to the DNA template-RNA polymerase complex, thereby preventing the initial separation of DNA strands during transcription and inhibiting messenger RNA synthesis. The narrow spectrum of antimicrobial activity of fidaxomicin may be explained by the unique target site of fidaxomicin and differing σ subunits of the core structure of RNA polymerase among bacterial species. |
| Pharmacodynamics | Fidaxomicin has a narrow-spectrum antibacterial profile, with potent bactericidal activity specifically against C. difficile. The minimum inhibitory concentration for 90% of organisms for fidaxomicin against _C. difficile_ ranged from 0.0078 to 2 μg/mL _in vitro_. The bactericidal activity of fidaxomicin is time-dependent. Other than _C. difficile_, fidaxomicin has moderate inhibitory activity against Gram-positive bacteria (_S. aureus_ and _Enterococcus spp._) and poor activity against normal colonic flora, including anaerobes and enteric Gram-negative bacilli. Isolates of _C. difficile_ that are resistant to rifamycins or other antimicrobial classes (such as cephalosporins, fluoroquinolones, clindamycin) were not shown to be cross-resistant to fidaxomicin. |
Targets
| Target | Organism | Actions |
|---|---|---|
| RNA polymerase sigma factor | Clostridium difficile (strain 630) | inhibitor |
ADME / PK
| Absorption | Following oral administration of a single dose of 200 mg fidaxomicin in healthy adults, the C<sub>max</sub> of fidaxomicin and its main metabolite OP-1118 were 5.20 ± 2.81 ng/mL and 12.0 ± 6.06, respectively. The median T<sub>max</sub> of fidaxomicin was 2 hours. The systemic absorption of fidaxomicin following oral administration is minimal. In a food-effect study involving healthy adults in either with a high-fat meal versus under fasting conditions, the C<sub>max</sub> of fidaxomicin and OP-1118 were decreased by 21.5% and 33.4%, respectively; however, this effect is deemed to be clinically insignificant as the therapeutic action of fidaxomicin does not depend on drug concentrations in the systemic circulation. |
|---|---|
| Half-life | Following oral administration of a single dose of 200 mg fidaxomicin in healthy adults, the elimination half-life of fidaxomicin was approximately 11.7 ± 4.80 hours. |
| Protein binding | Since fidaxomicin has minimal systemic absorption following oral administration, there is limited information on the plasma protein binding profile of fidoxamicin. |
| Metabolism | Following oral administration, fidaxomicin is transformed to its main and pharmacologically active metabolite, OP-1118, via hydrolysis at the isobutyryl ester. As cytochrome enzymes are not involved in the metabolism of fidaxomicin, it is speculated that this biotransformation is mediated by gastric acid or enzymatic activity of intestinal microsomes. |
| Route of elimination | Following oral administration, fidaxomicin is mainly excreted in feces. More than 92% of the dose was recovered in the faces as either the unchanged parent drug or metabolites in one study consisting of healthy adults receiving single doses of 200 mg and 300 mg of fidaxomicin. In another study of healthy adults, approximately 0.59% fo the oral dose (200 mg) administered was recovered in the urine as the main metabolite, OP-1118. |
| Volume of distribution | Fidaxomicin is mainly confined to the gastrointestinal tract when orally administered. There is limited information on the volume of distribution of fidaxomicin. |
| Clearance | There is limited information on the clearance of fidaxomicin. |
Formulation & handling
- Fidaxomicin is a small molecule antibiotic formulated exclusively for oral administration in tablet and granule forms.
- The compound exhibits very low water solubility and high lipophilicity (LogP 8.56), which may influence formulation strategies to enhance bioavailability.
- Food intake does not significantly affect the clinical efficacy of fidaxomicin, allowing flexible dosing with or without meals.
Regulatory status
| Lifecycle | The API is currently protected by patents in the United States, with key expirations occurring between 2024 and 2028. It is marketed in the US, Canada, and the EU, where the product is at various stages of market maturity depending on patent status. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Fidaxomicin is primarily supplied by a limited number of originator companies with branded products marketed across the US, Canada, and the EU. Several patent protections are in place in the United States, with key patents expiring between 2024 and 2028, indicating current protection as well as potential for upcoming generic competition following these expiry dates. |
|---|
Safety
| Toxicity | In rats, the LD<sub>50</sub> of fidaxomicin was approximately 200 mg/kg and the no observed adverse effect level (NOAEL) was determined to be 62.5 mg/kg following administration of a single intravenous dose. There is limited clinical data on acute overdose in humans. |
|---|
- Fidaxomicin exhibits an approximate LD50 of 200 mg/kg in rats following intravenous administration
- The no observed adverse effect level (NOAEL) in animal studies is 62
- 5 mg/kg after a single intravenous dose
Fidaxomicin is a type of Antibacterials
Antibacterials, a category of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in combating bacterial infections. These APIs are chemical compounds that target and inhibit the growth or kill bacteria, helping to eliminate harmful bacterial pathogens from the body.
Antibacterials are essential for the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and more. They are commonly prescribed by healthcare professionals to combat both mild and severe bacterial infections.
Within the category of antibacterials, there are different classes and subclasses of APIs, each with distinct mechanisms of action and target bacteria. Some commonly used antibacterials include penicillins, cephalosporins, tetracyclines, macrolides, and fluoroquinolones. These APIs work by interfering with various aspects of bacterial cellular processes, such as cell wall synthesis, protein synthesis, DNA replication, or enzyme activity.
The development and production of antibacterial APIs require stringent quality control measures to ensure their safety, efficacy, and purity. Pharmaceutical manufacturers must adhere to Good Manufacturing Practices (GMP) and follow rigorous testing protocols to guarantee the quality and consistency of these APIs.
As bacterial resistance to antibiotics continues to be a significant concern, ongoing research and development efforts aim to discover and develop new antibacterial APIs. The evolution of antibacterials plays a crucial role in combating emerging bacterial strains and ensuring effective treatment options for infectious diseases.
In summary, antibacterials are a vital category of pharmaceutical APIs used to treat bacterial infections. They are designed to inhibit or kill bacteria, and their development requires strict adherence to quality control standards. By continually advancing research in this field, scientists and pharmaceutical companies can contribute to the ongoing battle against bacterial infections.
Fidaxomicin API manufacturers & distributors
Compare qualified Fidaxomicin API suppliers worldwide. We currently have 5 companies offering Fidaxomicin API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, MSDS, USDMF | 229 products |
| BrightGene | Producer | China | China | CoA, USDMF | 11 products |
| Changzhou Comwin Fine Che... | Producer | China | China | BSE/TSE, CoA, MSDS | 235 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS | 144 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 144 products |
When sending a request, specify which Fidaxomicin 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 Fidaxomicin 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.
