Cyclosporin A is a cyclic polypeptide immunosuppressant and pharmaceutical active ingredient used to suppress immune-system activity. It is primarily associated with organ transplantation and the management of certain autoimmune and inflammatory conditions.
Cyclosporin A, also known as Cyclosporine, is a lipophilic cyclic peptide consisting of 11 amino acids. It is produced by fermentation of the fungus Tolypocladium inflatum and subsequently purified for pharmaceutical applications.
Cyclosporin A is identified by CAS No. 59865-13-3. Its molecular formula is C62H111N11O12 and its molecular weight is approximately 1202.61 g/mol.
Cyclosporin A is a potent immunosuppressive agent. It primarily affects T-lymphocyte activation, helping reduce immune responses that can contribute to organ-transplant rejection and certain immune-mediated diseases.
Cyclosporin A binds to the intracellular protein cyclophilin. The resulting complex inhibits the phosphatase activity of calcineurin, which prevents activation of the nuclear factor of activated T-cells (NFAT).
This reduces transcription of interleukin-2 and other cytokines, thereby suppressing T-cell activation and proliferation.
Cyclosporin A is used in pharmaceutical products associated with:
The approved indication depends on the final dosage form, formulation and applicable regulatory requirements.
Cyclosporin A may be incorporated into different pharmaceutical dosage forms, including:
Because Cyclosporin A has very low aqueous solubility and variable bioavailability, formulation and manufacturing technology are important considerations when developing pharmaceutical products.
Cyclosporin A API quality evaluation may include:
Analytical testing should be performed using validated methods appropriate for the API and intended formulation.
Cyclosporin A intended for pharmaceutical manufacturing should comply with applicable GMP, quality-control and regulatory requirements. Specifications should be established according to the intended market, applicable pharmacopoeial standards and the manufacturer's approved product specification.
A batch-specific Certificate of Analysis (CoA) should provide applicable test results and acceptance criteria.
Cyclosporin A should be stored in appropriately sealed packaging under the manufacturer's specified conditions. The API should be protected from excessive moisture, heat, light and other environmental conditions that could affect its quality.
Cyclosporin A is relevant to pharmaceutical manufacturers and formulation-development companies involved in immunosuppressive medicines, transplant-related therapies, autoimmune disease treatments and ophthalmic pharmaceutical development.
For commercial applications, customers should verify the API grade, assay, impurity profile, specification, regulatory documentation and batch-specific CoA before use.
Consistent Cyclosporin A quality is important because the API is used in products where accurate dosing and controlled drug exposure are particularly important. Appropriate control of identity, potency, purity and related substances supports reliable pharmaceutical manufacturing.
Cyclosporin A is an important immunosuppressive pharmaceutical active ingredient that acts primarily through the cyclophilin-calcineurin pathway to inhibit T-cell activation. It has established applications in transplant medicine and selected immune-mediated conditions, as well as specific ophthalmic formulations.
High-quality Cyclosporin A should be supplied with appropriate quality specifications, analytical documentation and batch-specific testing to support pharmaceutical development and manufacturing requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | Conforms to Cyclosporin A identity by validated analytical methods |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 1.0% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Water Content | NMT 0.5% |
| Melting Point | 150°C – 154°C |