Roxithromycin API Manufacturers & Suppliers
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Roxithromycin | CAS No: 80214-83-1 | GMP-certified suppliers
A medication that treats respiratory, urinary, and soft tissue infections with broad antibacterial activity against common Gram-positive and Gram-negative pathogens.
Therapeutic categories
Primary indications
- Used to treat respiratory tract, urinary and soft tissue infections
Product Snapshot
- Roxithromycin is available primarily as oral tablets, powders for suspension, granules, and capsules, encompassing both film-coated and soluble formulations
- It is indicated for the treatment of respiratory tract, urinary, and soft tissue infections
- Regulatory status varies by market, including approved, investigational, and withdrawn classifications
Clinical Overview
Pharmacologically, roxithromycin exerts its antibacterial activity by binding to the 50S subunit of bacterial ribosomes. This interaction inhibits the translocation step in peptide elongation during protein synthesis, resulting in bacteriostatic effects. Its spectrum of activity includes a range of pathogens such as Streptococcus pneumoniae, Neisseria meningitidis, Mycoplasma pneumoniae, Chlamydia trachomatis, Haemophilus species, and others. Roxithromycin is highly concentrated intracellularly within polymorphonuclear leukocytes and macrophages, achieving levels greater than those in extracellular fluids. This accumulation enhances phagocytic and chemotactic functions of immune cells, facilitating bacterial clearance through intracellular bactericidal activity.
From an absorption, distribution, metabolism, and excretion (ADME) perspective, roxithromycin is metabolized partially by cytochrome P450 isoenzymes, including CYP3A4 and CYP2B6, and is both a substrate and inhibitor of these enzymes. This dual role necessitates consideration of potential drug-drug interactions. It also acts as an inhibitor of organic anion-transporting polypeptides OATP1B1 and OATP1B3. Roxithromycin is classified among moderate risk QTc-prolonging agents, underscoring the importance of cardiac monitoring in susceptible patients.
Safety considerations include the potential for QT interval prolongation, hypersensitivity reactions typical for macrolides, and hepatotoxicity in rare cases. Careful patient history and monitoring are advised during therapy.
Roxithromycin is marketed in several regions, including Australia, where it is registered for systemic antibacterial indications. Given its involvement in cytochrome P450 pathways, stringent quality control during API manufacturing is crucial to ensure batch-to-batch consistency and minimize impurities that could impact metabolic profiles or safety. Procurement of roxithromycin API should prioritize suppliers compliant with good manufacturing practices (GMP) and regulatory standards relevant to the intended market.
Identification & chemistry
| Generic name | Roxithromycin |
|---|---|
| Molecule type | Small molecule |
| CAS | 80214-83-1 |
| UNII | 21KOF230FA |
| DrugBank ID | DB00778 |
Pharmacology
| Summary | Roxithromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit and blocking peptide translocation. It exhibits bacteriostatic and intracellular bactericidal activity against a broad spectrum of pathogens, including Streptococcus, Neisseria, Mycoplasma, and Chlamydia species. Additionally, roxithromycin accumulates in immune cells, enhancing phagocytic functions to support bacterial clearance. |
|---|---|
| Mechanism of action | Roxithromycin prevents bacterial growth by interfering with their protein synthesis. It binds to the 50S subunit of bacterial ribosomes and inhibits the translocation of peptides. |
| Pharmacodynamics | Roxithromycin has the following antibacterial spectrum <i>in vitro</i>: <i>Streptococcus agalactiae</i>, <i>Streptococcus pneumoniae</i> (Pneumococcus), <i>Neisseria meningitides</i> (Meningococcus), <i>Listeria monocytogenes</i>, <i>Mycoplasma pneumoniae</i>, <i>Chlamydia trachomatis</i>, <i>Ureaplasma urealyticum</i>, <i>Legionella pneumophila</i>, <i>Helicobacter</i> (Campylobacter), <i>Gardnerella vaginalis</i>, <i>Bordetella pertussis</i>, <i>Moraxella catarrhalis</i> (<i>Branhamella Catarrhalis</i>), and <i>Haemophilus ducreyi</i>. Roxithromycin is highly concentrated in polymorphonuclear leukocytes and macrophages, achieving intracellular concentrations greater than those outside the cell. Roxithromycin enhances the adhesive and chemotactic functions of these cells which in the presence of infection produce phagocytosis and bacterial lysis. Roxithromycin also possesses intracellular bactericidal activity. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 50S ribosomal protein L10 | Shigella flexneri | inhibitor |
| P-glycoprotein 1 | Humans |
ADME / PK
| Absorption | Very rapidly absorbed and diffused into most tissues and phagocytes. |
|---|---|
| Half-life | 12 hours |
| Protein binding | 96%, mainly to alpha1-acid glycoproteins |
| Metabolism | Hepatic. Roxithromycin is only partially metabolised, more than half the parent compound being excreted unchanged. Three metabolites have been identified in urine and faeces: the major metabolite is descladinose roxithromycin, with N-mono and N-di-demethyl roxithromycin as minor metabolites. The respective percentage of roxithromycin and these three metabolites is similar in urine and faeces. |
Formulation & handling
- Roxithromycin is a small molecule aminoglycoside antibiotic formulated exclusively for oral administration in various tablet and suspension forms.
- Due to its low water solubility (0.187 g/L) and moderate lipophilicity (LogP 3), formulation strategies should consider solubility enhancement for consistent bioavailability.
- As a small molecule, Roxithromycin does not have peptide/biologic sensitivity, but stability considerations should focus on protecting suspension forms from moisture and light exposure.
Regulatory status
Safety
| Toxicity | Roxithromycin primarily causes gastrointestinal adverse events, such as diarrhoea, nausea, abdominal pain and vomiting. Less common adverse events include headaches, rashes, abnormal liver function values and alteration in senses of smell and taste. |
|---|
- May cause gastrointestinal irritation including diarrhoea, nausea, abdominal pain, and vomiting upon exposure
- Handling requires precautions to avoid dermal or mucosal contact due to potential for rash and sensory alterations
- Monitor for signs of hepatotoxicity
Roxithromycin is a type of Macrolides
Macrolides are a significant subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the healthcare industry. These compounds belong to a class of antibiotics characterized by a large macrocyclic lactone ring, which is the key structural feature responsible for their therapeutic activity.
Macrolides possess a broad spectrum of activity against various bacteria, making them valuable in the treatment of many bacterial infections. They work by inhibiting the synthesis of bacterial proteins, thereby preventing their growth and replication. This mechanism of action makes macrolides effective against both Gram-positive and some Gram-negative bacteria.
One of the most well-known macrolide antibiotics is erythromycin, which has been used for decades to treat respiratory tract infections, skin infections, and sexually transmitted diseases. Over time, several derivatives and semi-synthetic macrolides have been developed, such as azithromycin and clarithromycin, which offer improved pharmacokinetic properties, increased efficacy, and broader spectrum of activity.
Macrolides are often preferred in clinical practice due to their favorable pharmacokinetics, including high tissue penetration, prolonged half-life, and low toxicity. They are commonly prescribed for patients who are allergic to penicillin or have other contraindications to beta-lactam antibiotics.
In conclusion, macrolides represent a vital subclass of pharmaceutical APIs with potent antibacterial properties. Their broad spectrum of activity, favorable pharmacokinetic profile, and versatility make them indispensable in the treatment of various bacterial infections.
Roxithromycin (Macrolides), classified under 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.
Roxithromycin API manufacturers & distributors
Compare qualified Roxithromycin API suppliers worldwide. We currently have 14 companies offering Roxithromycin 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 |
|---|---|---|---|---|---|
| Arshine Pharmaceutical Co... | Distributor | China | China | BSE/TSE, CoA, GMP, MSDS | 176 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS | 250 products |
| AXXO GmbH | Distributor | Germany | World | CEP, CoA, GMP, GDP, MSDS | 243 products |
| Chr. Olesen Group | Distributor | Denmark | China | CEP, CoA, GMP, MSDS, USDMF | 252 products |
| Envee Drugs Pvt Ltd | Producer | India | India | CoA, GMP, ISO9001 | 16 products |
| G.C. Chemie Pharmie Ltd | Producer | India | India | CoA | 21 products |
| HEC Pharm | Producer | Germany | China | CoA, GMP | 31 products |
| Hovione Farmaciencia | Producer | Portugal | Portugal | CoA, JDMF | 16 products |
| Kopran R.L. | Producer | India | India | CEP, CoA, FDA, GMP, WC | 8 products |
| Sanofi | Producer | France | France | CoA, GMP | 93 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 762 products |
| Zhejiang Guobang | Producer | China | China | CEP, CoA, GMP, WC | 6 products |
| Zhejiang Zhenyuan | Producer | China | China | CEP, CoA, GMP, KDMF | 3 products |
When sending a request, specify which Roxithromycin 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 Roxithromycin 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.
