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Pimecrolimus | CAS No: 137071-32-0 | GMP-certified suppliers
A medication that supports management of mild to moderate atopic dermatitis by helping reduce inflammatory skin symptoms, offering a non‑steroidal option for chronic dermatologic needs.
Therapeutic categories
Primary indications
- For treatment of mild to moderate atopic dermatitis
Product Snapshot
- Topical small‑molecule immunomodulator supplied as a cutaneous cream formulation
- Used for management of mild to moderate atopic dermatitis
- Approved in the US and Canada with additional investigational status in some settings
Clinical Overview
The compound exerts pharmacologic activity through selective inhibition of T‑cell and mast‑cell activation. Pimecrolimus binds with high affinity to FKBP‑12, forming a complex that inhibits the calcium-dependent phosphatase calcineurin. This blocks transcription of early cytokines in T cells, including interleukin‑2, interferon‑gamma, interleukin‑4, and interleukin‑10. In mast cells, it reduces release of cytokines and inflammatory mediators following IgE‑mediated stimulation. These actions contribute to attenuation of pruritus, erythema, and other inflammatory manifestations of atopic dermatitis.
Systemic exposure after topical administration is generally low due to limited dermal absorption, and the compound is metabolized primarily via CYP3A pathways when absorbed. Pimecrolimus is not intended for systemic immunosuppression, and pharmacokinetic parameters vary with skin barrier integrity, application area, and duration of use.
Safety considerations center on local tolerability, including transient burning or irritation at the application site. Due to theoretical risks related to systemic calcineurin inhibition, long‑term or occlusive use and application on compromised skin surfaces are approached cautiously. Use in populations with high systemic absorption potential, such as very young children or those with extensive erosive lesions, is typically subject to additional clinical oversight.
Pimecrolimus is marketed in several regions, with historical association to Novartis and later commercialization by Galderma in Canada. As an approved and sometimes investigational calcineurin inhibitor, its regulatory status may vary globally.
For API procurement, sourcing should prioritize suppliers with demonstrated control of macrolide lactam synthesis, validated impurity profiles, and compliance with regional GMP and dossier requirements to support consistent topical formulation performance.
Identification & chemistry
| Generic name | Pimecrolimus |
|---|---|
| Molecule type | Small molecule |
| CAS | 137071-32-0 |
| UNII | 7KYV510875 |
| DrugBank ID | DB00337 |
Pharmacology
| Summary | Pimecrolimus is a topical calcineurin pathway inhibitor that binds FKBP‑12, blocking calcineurin activity and suppressing downstream T‑cell cytokine transcription. This action reduces production of key Th1- and Th2‑type cytokines and limits mast‑cell mediator release. Its pharmacologic effect is focused on dampening immune-driven inflammation associated with mild to moderate atopic dermatitis. |
|---|---|
| Mechanism of action | Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T cells. Also, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/lgE. |
| Pharmacodynamics | Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Serine/threonine-protein kinase mTOR | Humans | potentiator |
| Peptidyl-prolyl cis-trans isomerase FKBP1A | Humans | potentiator |
ADME / PK
| Absorption | Because of the low systemic absorption of pimecrolimus following topical application the calculation of standard pharmacokinetic measures such as AUC, C<sub>max</sub>, half-life, etc. cannot be reliably done. |
|---|---|
| Protein binding | 74%-87% (in vitro, bound to plasma proteins) |
| Metabolism | No drug metabolism was observed in human skin in vitro. Oral administration yielded metabolites produced from O-demethylation and oxygenation reactions. |
| Route of elimination | 80% of the drug is excreted in the feces. |
Formulation & handling
- Low aqueous solubility and high lipophilicity favor incorporation into lipid‑rich topical or dermal delivery systems rather than aqueous vehicles.
- Macrolide lactam structure can be sensitive to hydrolysis, so formulations typically require controlled moisture and antioxidant/stabilizer considerations.
- As a topical-only small molecule with minimal systemic absorption, handling focuses on uniform dispersion in semi-solid bases and protection from excessive heat or light during processing.
Regulatory status
| Lifecycle | The active ingredient’s key Canadian and U.S. patents expired between 2015 and 2018, indicating that exclusivity has lapsed in both markets. With products established in the United States and Canada, the API is in a mature, post‑patent stage. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Pimecrolimus is supplied primarily by a single originator, with packaging handled by the same company and select third‑party packagers, indicating a centralized manufacturing base. Branded products are available mainly in the US and Canada, reflecting a focused but established market presence. Patent expiries between 2015 and 2018 suggest that generic competition is already possible in these regions. |
|---|
Safety
| Toxicity | Side effects include burning sensation, irritation, pruritus, erythema, and skin infections, at the application site. |
|---|
- Contact with the compound may provoke localized burning, pruritus, erythema, or irritation
- Appropriate controls should be used to limit dermal exposure during handling
- Residual material on equipment or surfaces can support secondary skin infection risk
US Drug Master File (USDMF)
A US Drug Master File (USDMF) is a confidential document submitted to the U.S. Food and Drug Administration (FDA) that provides detailed information about the manufacturing process of an Active Pharmaceutical Ingredient (API) or a finished pharmaceutical product. This document includes comprehensive details such as chemical properties, manufacturing facilities, production processes, packaging specifications, storage conditions, and more.
The USDMF ensures that proprietary information remains protected while allowing the FDA to review the data as part of drug approval processes. Unlike other types of DMFs used in different regions, the USDMF is specifically designed to meet the regulatory requirements set by the FDA, ensuring compliance with U.S. standards.
Pimecrolimus is a type of Calcineurin inhibitors
Calcineurin inhibitors are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the treatment of various medical conditions. These inhibitors work by suppressing the activity of calcineurin, an enzyme that plays a crucial role in the immune response.
The primary application of calcineurin inhibitors is in the field of immunosuppression, particularly in organ transplantation. These medications prevent the rejection of transplanted organs by inhibiting the production of cytokines, such as interleukin-2, which are responsible for triggering the immune response. By modulating the immune system, calcineurin inhibitors enable successful transplantation and enhance patient outcomes.
Furthermore, calcineurin inhibitors find utility in the treatment of autoimmune disorders, including psoriasis and rheumatoid arthritis. These medications help alleviate symptoms and reduce inflammation by interfering with the immune system's response.
The two most commonly used calcineurin inhibitors are cyclosporine and tacrolimus. These compounds exhibit high specificity and affinity for calcineurin, ensuring effective immunosuppression. Both drugs are available in various formulations, including oral capsules, injectables, and topical preparations, enabling healthcare professionals to tailor treatment to individual patient needs.
It is important to note that calcineurin inhibitors may have certain side effects, including nephrotoxicity, hypertension, and increased susceptibility to infections. Close monitoring of patients and appropriate dosage adjustments are crucial to maintaining the delicate balance between immune suppression and overall health.
In summary, calcineurin inhibitors represent a vital subcategory of pharmaceutical APIs used in immunosuppressive therapy for organ transplantation and autoimmune disorders. Their ability to modulate the immune response plays a crucial role in achieving successful patient outcomes.
Pimecrolimus (Calcineurin inhibitors), 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.
Pimecrolimus API manufacturers & distributors
Compare qualified Pimecrolimus API suppliers worldwide. We currently have 4 companies offering Pimecrolimus API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Biocon | Producer | India | India | CoA, USDMF | 36 products |
| BrightGene | Producer | China | China | CoA, USDMF | 11 products |
| Euticals | Producer | Italy | Unknown | CoA, USDMF | 48 products |
| Lek Pharma | Producer | Slovenia | Slovenia | CoA, GMP | 32 products |
When sending a request, specify which Pimecrolimus 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.).
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Technical
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Regulatory
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