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Anthralin | CAS No: 1143-38-0 | GMP-certified suppliers
A medication that treats stable plaque psoriasis and other dermatoses topically by normalizing skin cell growth and reducing inflammation, suitable for dermatological formulations in major markets.
Therapeutic categories
Primary indications
- Stable plaque psoriasis of the skin and scalp
- It is also used topically in the management of psoriasis, dermatoses, and alopecia areata
- Anthralin is also used in biomedical research due to its effect on EGFR autophosphorylation
Product Snapshot
- Anthralin is formulated as topical ointments, creams, lotions, and shampoos
- It is primarily indicated for the treatment of stable plaque psoriasis, dermatoses, and alopecia areata
- Anthralin products have regulatory approval in the United States and Canada
Clinical Overview
Pharmacologically, anthralin exerts its effects by modulating epidermal cell kinetics. It inhibits keratinocyte proliferation and interferes with T-cell activity, potentially through mechanisms involving mitochondrial dysfunction and the generation of reactive oxygen species. These actions are associated with inhibition of DNA synthesis, prolongation of the prophase stage of mitosis, and promotion of cell differentiation. The compound’s anti-inflammatory and anti-proliferative properties contribute to normalization of epidermal hyperplasia and keratinization characteristic of psoriatic lesions. Additional effects include lipid peroxidation and reduction of endothelial adhesion molecules elevated in psoriasis, which may further mitigate inflammatory responses.
Anthralin demonstrates suitable dermal absorption, facilitated by its chemical structure supporting dual solubility, which permits effective epidermal penetration. Pharmacokinetic data indicate local activity with minimal systemic absorption, and systemic side effects have not been reported, distinguishing it from many other antipsoriatic agents. Safety considerations primarily involve local skin irritation and staining/discoloration of treated areas, necessitating careful patient counseling and appropriate formulation to balance efficacy with tolerability.
Clinically, anthralin formulations are frequently combined with salicylic acid to enhance stability and dermal penetration. The use of anthralin remains primarily topical, with no systemic formulations approved. It also finds application in biomedical research related to epidermal growth factor receptor modulation.
From a sourcing perspective, procurement of anthralin API requires attention to purity, stability, and consistency due to its light-sensitivity and propensity to oxidize. Quality control measures should ensure compliance with pharmacopeial standards and suitability for incorporation into dermatological preparations.
Identification & chemistry
| Generic name | Anthralin |
|---|---|
| Molecule type | Small molecule |
| CAS | 1143-38-0 |
| UNII | U8CJK0JH5M |
| DrugBank ID | DB11157 |
Pharmacology
| Summary | Anthralin acts primarily by inhibiting keratinocyte proliferation and DNA synthesis, leading to normalization of epidermal cell growth and differentiation. It exerts anti-inflammatory effects through suppression of T-lymphocyte activation and promotion of reactive oxygen species generation, potentially via mitochondrial pathways. These combined actions target hyperproliferative skin disorders such as psoriasis by modulating cellular mitotic activity and inflammatory responses. |
|---|---|
| Mechanism of action | Anthralin inhibits the proliferation of keratinocytes (epidermal skin cells), prevents the action of T-cells, and promotes cell differentiation, likely through mitochondrial dysfunction. In addition, the production of free radicals may contribute to its anti-psoriatic effect . In vitro studies demonstrate that anthralin prolongs the prophase component of mitosis for keratinocytes and leukocytes . Prophase is the first step of mitosis, the process separating the duplicated genetic material carried in the nucleus of a parent cell into two identical daughter cells . In vivo studies demonstrate that anthralin blocks DNA synthesis and can increase the release of reactive oxygen species . Anthralin is believed to normalize the rate of epidermal cell proliferation and keratinization by reducing the mitotic activity of the epidermal hyperplasia in psoriasis . Anti-proliferative and anti-inflammatory effects of anthralin have been demonstrated on both psoriatic and healthy skin. The anti-proliferative effects of anthralin are thought to be due to a combination of inhibition of DNA synthesis and its strong reducing properties. The effectiveness of anthralin as an anti-psoriatic agent is partly owed to its ability to promote lipid peroxidation and reduce the concentration of endothelial adhesion molecules, which are found to be elevated in psoriatic patients , . Recent studies suggest that its ability to prevent T-lymphocyte activation and normalize keratinocyte differentiation may occur by a direct effect on mitochondria . |
| Pharmacodynamics | Anthralin is a natural anthraquinone derivative, anti-psoriatic and anti-inflammatory agent. It controls skin growth by reducing the synthesis of DNA and the mitotic activity in the hyperplastic epidermis, normalizing the rate of cell proliferation and keratinization . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Keratin, type II cytoskeletal 2 epidermal | Humans | antagonist |
| Keratin, type I cytoskeletal 12 | Humans | antagonist |
| C-Jun-amino-terminal kinase-interacting protein 1 | Humans | agonist |
ADME / PK
| Absorption | Anthralin penetrates damaged skin and psoriatic lesions faster and to a greater extent than normal skin, likely due to increased vascularity of psoriatic lesions . |
|---|---|
| Metabolism | Anthralin is administered topically. Although the extent of systemic absorption after topical application has not been determined, no traces of anthraquinone metabolites were detected in the urine of treated subjects in a limited clinical study of anthralin cream , . Anthralin does not inhibit hepatic microsomal enzyme activity . |
Formulation & handling
- Anthralin is a small molecule intended for topical formulations such as ointments, creams, lotions, and shampoos.
- The compound exhibits low water solubility and a high logP, indicating lipophilic properties relevant for formulation strategies.
- Stability and handling should consider the anthracene structure, which may be sensitive to light and oxidation.
Regulatory status
| Lifecycle | The API is currently marketed in Canada and the US, with primary patents having expired, leading to increased availability of generic versions and a mature market environment. Ongoing product lifecycle management focuses on regulatory compliance and market adaptation. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The supply landscape for Anthralin includes multiple originator companies offering branded products primarily in the US and Canadian markets. The presence of various brand formulations indicates an established branded product base in these regions. Patent expiry status is not specified, but the existing multiple concentrations and creams suggest opportunities for generic manufacturing and competition. |
|---|
Safety
| Toxicity | Some mild adverse effects include alterations in nail coloring, hair coloring, increase in photosensitivity, and skin irritation . The most common side effects of anthralin are skin irritation and staining of nearby skin, nails, clothing, and other objects that come in contact with the treated patient. The incidence of irritation of psoriatic/surrounding healthy skin is higher in patients who leave anthralin on the skin without rinsing than in those who use short-contact therapy of 2 hours or less, followed by rinsing . If the psoriatic plaques are well circumscribed, the surrounding normal skin may be protected by the use of a coating agent such as zinc oxide ointment. Anthralin should be applied cautiously to the face and intertriginous areas due to the risk of severe skin irritation . There is no current evidence of any long-term anthralin toxicity related either to skin exposure or to systemic issues . Some long-term studies in mice have demonstrated anthralin to be tumorigenic in mouse skin. This carcinogenic potential has not been thoroughly evaluated. Tumorigenic and carcinogenic effects of anthralin have not been observed in humans at this time . Anthralin is classified as FDA pregnancy risk category C drug . It is not known if anthralin can cause fetal harm when administered during gestation. Because of the lack of evidential human data, anthralin should be used during pregnancy only when clearly required . |
|---|
- May cause skin irritation and staining of skin, nails, clothing, and other materials upon contact
- Increased photosensitivity and risk of severe irritation when applied to facial or intertriginous areas
- Use protective barriers as needed
Dithranol is a type of Other dermatological agents
Others
Dithranol (Other dermatological agents), classified under Dermatological Agents
Dermatological agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the formulation of various skincare and dermatology products. These APIs are specifically designed to target and treat skin conditions, offering effective solutions for a wide range of dermatological concerns.
Dermatological agents encompass a diverse array of compounds, including corticosteroids, antifungal agents, antibacterials, retinoids, and immunomodulators. Each API within this category possesses unique properties and mechanisms of action, enabling them to address specific skin-related issues.
Corticosteroids, for instance, are potent anti-inflammatory agents commonly used in the treatment of skin conditions like eczema, psoriasis, and dermatitis. Antifungal agents, on the other hand, combat fungal infections such as athlete's foot or ringworm. Antibacterials are effective against bacterial infections, while retinoids promote skin cell turnover and treat acne and photoaging. Immunomodulators regulate the immune response, providing relief from conditions like atopic dermatitis.
The development and application of dermatological APIs involve rigorous research, clinical trials, and regulatory compliance. These APIs are typically integrated into topical creams, ointments, gels, and lotions, ensuring targeted delivery to the affected areas of the skin.
Dermatological agents play a crucial role in the management and treatment of various skin disorders. By harnessing the therapeutic properties of these APIs, pharmaceutical companies can develop innovative skincare products that cater to the diverse needs of individuals seeking effective dermatological solutions.
Dithranol API manufacturers & distributors
Compare qualified Dithranol API suppliers worldwide. We currently have 7 companies offering Dithranol 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 |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| Caesar & Loretz GmbH (CAE... | Distributor | Germany | Unknown | BSE/TSE, CoA, GMP, ISO9001, MSDS | 211 products |
| Chiracon | Producer | Germany | Unknown | CoA | 6 products |
| Duchefa Farma B.V. | Distributor | Netherlands | France | CoA, GMP, ISO9001, MSDS | 170 products |
| Prachi Pharmaceuticals | Producer | India | India | CoA, FDA, GMP, ISO9001, USDMF, WHO-GMP | 12 products |
| Seratec | Producer | France | France | CoA, GMP | 5 products |
| Somet | Producer | Monaco | Monaco | CoA | 4 products |
When sending a request, specify which Dithranol 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 Dithranol 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.
