- Raw materials
- Dermatological Agents
- Retinoids
- Alitretinoin
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Alitretinoin | CAS No: 5300-03-8 | GMP-certified suppliers
A medication that provides topical treatment for cutaneous lesions in patients with AIDS-related Kaposi's sarcoma, supporting dermatological management through gene expression regulation.
Therapeutic categories
Primary indications
- For topical treatment of cutaneous lesions in patients with AIDS-related Kaposi's sarcoma
Product Snapshot
- Alitretinoin is available in oral capsule and topical formulations including cream and gel
- It is primarily indicated for the topical treatment of cutaneous lesions associated with AIDS-related Kaposi's sarcoma
- The product has approved status in the US, Canada, and EU markets, with some formulations under investigational status
Clinical Overview
Clinically, alitretinoin is approved for the topical treatment of cutaneous lesions associated with AIDS-related Kaposi's sarcoma. It has demonstrated the ability to inhibit the proliferation of Kaposi's sarcoma cells in vitro. Beyond this, retinoids including alitretinoin have been utilized in the management of various dermatological conditions such as psoriasis and acne vulgaris owing to their effects on skin cell differentiation and proliferation.
The pharmacological action of alitretinoin is mediated through its binding to all subtypes of intracellular retinoid receptors: RARα, RARβ, RARγ, RXRα, RXRβ, and RXRγ. Activation of these receptors modulates gene transcription, thereby regulating processes related to cellular differentiation, proliferation, and apoptosis in both normal and neoplastic cells.
Key pharmacokinetic parameters such as absorption, distribution, metabolism, and elimination are influenced by the molecule’s lipophilicity and its status as a substrate for P-glycoprotein transporters. However, its topical application in Kaposi's sarcoma limits systemic exposure relative to oral retinoids.
Safety considerations include the known teratogenic potential of retinoids, necessitating stringent risk management in women of childbearing potential. Other adverse effects may involve local skin irritation, and systemic toxicity is rare with topical dosing but must be monitored where applicable.
From a quality and sourcing perspective, alitretinoin API should comply with pharmacopeial standards where available, and manufacturers must ensure control of isomeric purity, stability, and absence of oxidative degradation products. Reliable suppliers with documented GMP compliance and validated analytical methods are recommended to ensure consistent quality and regulatory acceptability for pharmaceutical development.
Identification & chemistry
| Generic name | Alitretinoin |
|---|---|
| Molecule type | Small molecule |
| CAS | 5300-03-8 |
| UNII | 1UA8E65KDZ |
| DrugBank ID | DB00523 |
Pharmacology
| Summary | Alitretinoin is a retinoid that binds to and activates all subtypes of retinoic acid receptors (RARs and RXRs), modulating gene expression involved in cellular differentiation and proliferation. Its pharmacodynamic effect includes inhibition of Kaposi's sarcoma cell growth. It is primarily used topically for treating cutaneous lesions in AIDS-related Kaposi's sarcoma. |
|---|---|
| Mechanism of action | Alitretinoin binds to and activates all known intracellular retinoid receptor subtypes (RARa, RARb, RARg, RXRa, RXRb and RXRg). Once activated these receptors function as transcription factors that regulate the expression of genes that control the process of cellular differentiation and proliferation in both normal and neoplastic cells. |
| Pharmacodynamics | Alitretinoin (9-<i>cis</i>-retinoic acid) is a naturally-occurring endogenous retinoid indicated for topical treatment of cutaneous lesions in patients with AIDS-related Kaposi's sarcoma. Alitretinoin inhibits the growth of Kaposi's sarcoma (KS) cells <i>in vitro</i>. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Retinoic acid receptor alpha | Humans | agonist |
| Retinoic acid receptor RXR-alpha | Humans | agonist |
| Retinoic acid receptor beta | Humans | agonist |
Formulation & handling
- Alitretinoin is administered orally in capsule form and topically as creams and gels, indicating its suitability for both systemic and localized treatments.
- As a small molecule retinoid with high lipophilicity (LogP 5.01), formulation should consider enhancing solubility and stability in lipid-based vehicles.
- Oral capsules should be taken with food to improve bioavailability, requiring consideration of dosing schedules aligned with meals.
Regulatory status
| Lifecycle | The API's key patents in the United States expired in August 2016 and in Canada in August 2018, indicating that the product is in a mature market phase across the US, Canada, and the EU. Generic competition is likely established given the patent expirations. |
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| Markets | US, Canada, EU |
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Supply Chain
| Supply chain summary | Alitretinoin manufacturing is primarily associated with one originator company, Eisai Inc., supported by multiple packagers including Basilea Pharmaceuticals Corp. and Ortho-McNeil-Janssen Pharmaceuticals Inc. Branded products are available across key markets including the US, Canada, and the EU. Existing patent expiries in the US (2016) and Canada (2018) indicate the presence or potential for generic competition in these regions. |
|---|
Alitretinoin is a type of Retinoids
Retinoids are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in dermatology and skincare products. Derived from vitamin A, retinoids play a crucial role in promoting skin health and treating various skin conditions. They are popular due to their proven effectiveness in combating acne, reducing wrinkles, and improving overall skin texture.
Retinoids work by binding to specific receptors in the skin cells, influencing gene expression and cellular processes. This action helps regulate the growth and differentiation of skin cells, promoting the turnover of old cells and the production of new, healthier cells. As a result, retinoids can unclog pores, reduce sebum production, and prevent the formation of acne lesions.
Furthermore, retinoids stimulate collagen production, which enhances skin elasticity and reduces the appearance of fine lines and wrinkles. They also possess antioxidant properties, protecting the skin from damage caused by environmental factors such as UV radiation.
Common retinoids used in skincare formulations include retinol, retinaldehyde, and tretinoin (also known as all-trans retinoic acid). These compounds vary in their potency and stability, with tretinoin being the most potent and retinol requiring conversion within the skin to become active.
However, it is important to note that retinoids may cause skin irritation, redness, and dryness, especially during the initial stages of usage. Gradual introduction and proper skincare routines can help minimize these side effects.
In summary, retinoids are a highly sought-after subcategory of pharmaceutical APIs for their significant benefits in skincare. They offer a promising solution for those seeking to improve their skin's health, combat acne, and reduce signs of aging.
Alitretinoin (Retinoids), 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.
