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Clofazimine | CAS No: 2030-63-9 | GMP-certified suppliers
A medication that supports combination therapy for lepromatous leprosy, including resistant or erythema nodosum leprosum cases, helping address complex mycobacterial infection needs.
Therapeutic categories
Primary indications
- Clofazimine is indicated for the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum
- To prevent the development of drug resistance, it should be used only in combination with other antimycobacterial leprosy treatments
Product Snapshot
- Oral small‑molecule API supplied as hard gelatin capsule formulations
- Primary use is for multidrug regimens targeting lepromatous leprosy, including dapsone‑resistant cases
- Approved in the US with additional investigational status in certain programs
Clinical Overview
Clofazimine displays slow bactericidal activity against Mycobacterium leprae, primarily through membrane‑directed effects. Current evidence suggests that interaction with bacterial membrane phospholipids generates antimicrobial lysophospholipids, leading to membrane destabilization, impaired potassium uptake, and reduced ATP synthesis. Its anti‑inflammatory effect is attributed to inhibition of T‑lymphocyte activation and proliferation, possibly involving Kv1.3 channel antagonism and indirect modulation through neutrophil and monocyte mediators.
The compound is highly lipophilic with extensive tissue distribution and a prolonged residence time, contributing to a long functional half‑life and the need for daily administration despite slow clearance. Absorption increases with lipid‑rich meals. The drug accumulates in fatty tissues and macrophage‑rich organs, and elimination is predominantly fecal. Quantitative ADME parameters vary across studies, but prolonged tissue retention is consistently observed.
Safety considerations include a high incidence of reversible skin, conjunctival, and body fluid discoloration, which may persist for months after discontinuation. Gastrointestinal deposition of crystals can lead to abdominal pain, obstruction, or, rarely, fatal complications; dose adjustment or discontinuation should be considered if symptoms occur. Use is generally avoided in hepatic impairment. Clofazimine has been associated with photosensitivity and potential QTc prolongation. Clinically relevant discoloration should be discussed with patients to support adherence in long‑term therapy.
Clofazimine is available in several national leprosy control programs and has been incorporated into World Health Organization multidrug therapy. For API procurement, suppliers should provide evidence of controlled crystal form, impurity profile, and stability data due to the compound’s lipophilicity and coloration properties.
Identification & chemistry
| Generic name | Clofazimine |
|---|---|
| Molecule type | Small molecule |
| CAS | 2030-63-9 |
| UNII | D959AE5USF |
| DrugBank ID | DB00845 |
Pharmacology
| Summary | Clofazimine is a membrane‑directed antimycobacterial agent whose activity appears to arise from interactions with bacterial phospholipids that generate membrane‑disruptive lysophospholipids, impairing ion transport and ATP production. It also modulates immune responses by inhibiting T‑lymphocyte activation, potentially through effects on Kv1.3 potassium channels and PPAR‑gamma. These combined antimicrobial and anti‑inflammatory actions contribute to its therapeutic role in leprosy. |
|---|---|
| Mechanism of action | Although the precise mechanism(s) of action of clofazimine have not been elucidated, its antimicrobial activity appears to be membrane-directed. It was previously thought that, due to its lipophilicity, clofazimine participated in the generation of intracellular reactive oxygen species (ROS) via redox cycling, specifically H<sub>2</sub>O<sub>2</sub> and superoxide, which then exerted an antimicrobial effect.A more recent and compelling theory involves clofazimine interacting with bacterial membrane phospholipids to generate antimicrobial lysophospholipids - bactericidal efficacy may, then, arise from the combined membrane-destabilizing effects of both clofazimine and lysophospholipids, which interfere with K+ uptake and, ultimately, ATP production. The anti-inflammatory activity of clofazimine is the result of its inhibition of T-lymphocyte activation and proliferation.Several mechanisms have been proposed, including direct antagonism of T-cell Kv 1.3 potassium channels and indirect action by promoting the release of E-series prostaglandins and reactive oxygen species from bystander neutrophils and monocytes. |
| Pharmacodynamics | Clofazimine exerts a slow bactericidal effect on <i>Mycobacterium leprae</i> (Hansen's bacillus) due primarily to its action on the bacterial outer membrane, though there is some evidence that activity on the bacterial respiratory chain and ion transporters may play a role.It also exerts anti-inflammatory properties due to the suppression of T-lymphocyte activity. Clofazimine has a relatively long duration of action owing to its long residence time in the body, but is still administered daily. Approximately 75-100% of patients receiving clofazimine will experience an orange-pink to brownish-black discoloration of the skin, conjunctivae, and bodily fluids.Skin discoloration may take several months or years to reverse following the cessation of therapy. Clofazimine has also been implicated in abdominal obstruction, in some cases fatal, due to the deposition of drug and formation of crystals in the intestinal mucosa - complaints of abdominal pain and nausea/vomiting should be investigated promptly, and the doses of clofazimine should be lowered or discontinued if it is found to be the culprit. Its use should be avoided in patients with hepatic dysfunction. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Peroxisome proliferator-activated receptor gamma | Humans | modulator |
| Potassium voltage-gated channel subfamily A member 3 | Humans | antagonist |
ADME / PK
| Absorption | Absorption varies from 45 to 62% following oral administration in leprosy patients.Co-administration of a 200mg dose of clofazimine with food resulted in a C<sub>max</sub> of 0.41 mg/L with a T<sub>max</sub> of 8 h; administered in a fasting state, the corresponding C<sub>max</sub> was 30% lower while the time to Cmax was 12 h. |
|---|---|
| Half-life | The mean elimination half-life is approximately 25 days. |
| Protein binding | Clofazimine is bound primarily to beta-lipoproteins (and, to a lesser extent, alpha-lipoproteins) in the serum. This binding was saturable at concentrations of ~10 µg/mL. Binding to gamma-globulin and albumin is negligible. |
| Metabolism | Three metabolites have been identified in the urine following repeated oral doses of clofazimine.It is unclear whether these metabolites are pharmacologically active. Metabolite I may be the result of the hydrolytic dehalogenation of clofazimine and metabolite II presumably is formed by a hydrolytic deamination reaction followed by glucuronidation. |
| Route of elimination | Part of an ingested dose of clofazimine is found in the feces, which may represent excretion in the bile, and a small amount is also eliminated in the sputum, sebum, and sweat.Excretion of unchanged drug and metabolites in a 24-hour urine collection was negligible. |
| Volume of distribution | Clofazimine is highly lipophilic and therefore deposits primarily in fatty tissues and cells of the reticuloendothelial system, where it is taken up by macrophages and further distributed throughout the body. Crystalized deposits have been found in the mesenteric lymph nodes, adrenals, subcutaneous fat, liver, bile, gall bladder, spleen, small intestine, muscles, bones, and skin. |
Formulation & handling
- Oral small‑molecule API with very low aqueous solubility and high lipophilicity, typically formulated in capsules using lipidic or solubilizing excipients to enhance dispersion.
- Absorption is food‑dependent, so formulations should account for increased bioavailability when administered with meals.
- Solid-state stability is generally good, but handling should minimize light exposure due to phenazine chromophore sensitivity.
Regulatory status
| Lifecycle | Patent protection in the US appears to be at or near the end of its lifecycle, indicating that the API is transitioning toward, or already in, a mature and predominantly generic market stage. This reflects a stable commercial environment with limited remaining exclusivity. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Clofazimine is supplied primarily by a single originator, with several packagers supporting downstream distribution. The listed branded product is marketed in the United States, with no additional regional markets identified in the data. Patent expiry occurred long ago, indicating an established environment for generic production and potential broader sourcing options. |
|---|
Safety
| Toxicity | The reported oral LD<sub>50</sub> of clofazimine in rats and mice is 8400 mg/kg and >5000 mg/kg, respectively. No specific data are available regarding the treatment of clofazimine overdosage.In cases of overdose consider gastrointestinal decontamination via gastric lavage or induced vomiting. Employ symptomatic and supportive measures as clinically indicated. |
|---|
- High acute oral toxicity thresholds in rodents: LD50 approximately 8400 mg/kg in rats and greater than 5000 mg/kg in mice, indicating relatively low acute lethality but requiring standard controls for handling high‑dose exposures
- Overdose toxicology is poorly characterized
- Available reports cite limited data, emphasizing uncertainty in systemic response profiles at supratherapeutic levels
Written Confirmation
When an API is imported into the European Union from elsewhere in the world, it should be accompanied by a “written confirmation” (WC). A written confirmation is a document set up by the health authorities of the country where the API was manufactured. After inspections were successfully performed under EU/GMP equivalent standards, the health authorities can provide a WC. These inspections will also have to regularly take place in the future.
Clofazimine is a type of Other antibacterials
The Other Antibacterials subcategory within the pharmaceutical Active Pharmaceutical Ingredients (APIs) encompasses a diverse range of compounds used to combat bacterial infections. These antibacterials possess unique mechanisms of action, making them valuable tools in the fight against drug-resistant bacteria.
One class of Other Antibacterials is the cyclic lipopeptides, which include compounds such as daptomycin. These lipopeptides disrupt bacterial cell membranes, leading to cell death. They have demonstrated efficacy against a broad spectrum of Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA).
Another group of antibacterials in this subcategory is the nitroimidazoles. Metronidazole is a well-known representative of this class and is effective against anaerobic bacteria and protozoa. Nitroimidazoles exert their antibacterial activity by damaging DNA and disrupting essential cellular processes.
The polymyxins, such as polymyxin B and colistin, are also part of the Other Antibacterials group. These cyclic polypeptides possess a unique mechanism of action, targeting bacterial cell membranes and causing leakage, ultimately leading to cell death. Polymyxins are particularly effective against Gram-negative bacteria, including multidrug-resistant strains like carbapenem-resistant Enterobacteriaceae (CRE).
Furthermore, some miscellaneous antibacterials fall under this subcategory. For instance, fosfomycin, a phosphonic acid derivative, inhibits bacterial cell wall synthesis. Fosfomycin has shown efficacy against both Gram-positive and Gram-negative pathogens, including urinary tract infections caused by multidrug-resistant bacteria.
Clofazimine (Other antibacterials ), 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.
Clofazimine API manufacturers & distributors
Compare qualified Clofazimine API suppliers worldwide. We currently have 3 companies offering Clofazimine 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 |
|---|---|---|---|---|---|
| Derivados Quimicos | Producer | Spain | Spain | CoA, GMP | 18 products |
| Sandoz | Producer | Austria | Unknown | CoA, USDMF | 58 products |
| Sangrose Labs. | Producer | India | India | CoA, WC | 1 products |
When sending a request, specify which Clofazimine 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 Clofazimine 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.
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