Voclosporin is a synthetic cyclic peptide and a structural analog of cyclosporine A belonging to the calcineurin inhibitor class of immunosuppressive pharmaceutical compounds. It is an important active pharmaceutical ingredient used in the development and manufacture of medicines for lupus nephritis, an immune-mediated kidney disease associated with systemic lupus erythematosus.
Voclosporin is marketed under the brand name LUPKYNIS. It is a modified cyclosporine analog designed to inhibit calcineurin and thereby suppress T-cell activation and associated inflammatory signaling. Its specialized cyclic peptide structure distinguishes it from conventional small-molecule pharmaceutical APIs.
Voclosporin has the empirical molecular formula C63H111N11O12 and a molecular weight of 1214.6 g/mol. The FDA describes voclosporin as approximately 90–95% trans-isomer active ingredient. It appears as a white to off-white solid.
Voclosporin is also identified by the development codes ISA-247, ISA(TX)247, ISATX247 and LX211. Its CAS identifiers include 515814-00-3 and 515814-01-4, with 515814-01-4 commonly associated with the active substance in chemical databases. PubChem identifies UNII 2PN063X6B1 for voclosporin.
The molecule is a homodetic cyclic peptide structurally related to cyclosporine A. Its molecular architecture contains multiple amino-acid-derived residues and extensive stereochemistry, contributing to its high molecular weight and complex physical and analytical characteristics.
Voclosporin is a calcineurin inhibitor immunosuppressant. Calcineurin is involved in T-cell activation through regulation of nuclear factor of activated T cells (NFAT). Inhibition of calcineurin reduces T-cell activation, cytokine production and expression of T-cell activation-related proteins.
The FDA describes voclosporin as producing concentration-dependent calcineurin inhibition. The mechanism contributes to suppression of immune-mediated inflammation associated with lupus nephritis.
Voclosporin is structurally related to cyclosporine but incorporates a modification that distinguishes it from cyclosporine A. This modification is associated with the pharmacological and pharmacokinetic characteristics of the molecule.
Voclosporin API is relevant to pharmaceutical manufacturers and developers working on immunosuppressive and nephrology-related pharmaceutical products. As a Voclosporin API manufacturer and supplier in India, the product can be positioned for pharmaceutical development and manufacturing applications requiring controlled-quality cyclic peptide material.
Because Voclosporin has a complex cyclic peptide structure, its quality assessment requires appropriate analytical characterization. Important quality attributes include identity, assay, stereochemical integrity, trans-isomer content, related substances and other applicable process- and product-related impurities.
Voclosporin is used in combination with a background immunosuppressive regimen for the treatment of active lupus nephritis in adults. Lupus nephritis is a kidney manifestation of systemic lupus erythematosus in which immune-mediated inflammation can damage the renal glomeruli and impair kidney function.
The pharmaceutical application of Voclosporin is therefore primarily associated with nephrology, immunology and autoimmune disease treatment. Its pharmacological classification is a calcineurin inhibitor immunosuppressant.
Voclosporin is supplied commercially as an oral pharmaceutical product. The API is incorporated into finished dosage forms under controlled pharmaceutical manufacturing conditions.
Voclosporin is reported as a white to off-white solid. At ambient temperature, the FDA reports that it is freely soluble in acetone, acetonitrile, ethanol and methanol, while it is practically insoluble in heptanes.
In water, Voclosporin is described as practically insoluble, with solubility less than 0.1 g/L at 20°C. This corresponds to less than 0.1 mg/mL. The FDA also reports that Voclosporin melts above 144°C with decomposition.
These values are useful reference characteristics for the API. They should not automatically be treated as universal release specifications unless included in the applicable validated product specification.
Quality control of Voclosporin should account for its cyclic peptide structure and stereochemical complexity. Identity testing can involve suitable chromatographic and spectroscopic techniques capable of confirming the molecular structure.
Assay and related-substance testing are important for determining the purity and potency of the API. Because the FDA identifies the active ingredient as approximately 90–95% trans-isomer, control of isomeric composition is an important characteristic of the active substance.
Additional analytical controls may include residual solvents, water content, elemental impurities, degradation products and process-related impurities, as applicable to the manufacturing process and registered specification.
Voclosporin represents a specialized class of immunosuppressive APIs based on cyclic peptide chemistry. Its structure and mechanism distinguish it from conventional calcineurin inhibitors such as tacrolimus and from other traditional small-molecule immunosuppressants.
For pharmaceutical development, control of chemical identity, assay, purity, stereochemistry and degradation profile is important to ensure consistent API quality. Manufacturing processes should use validated analytical methods and appropriate pharmaceutical quality systems.
Voclosporin can be categorized as a cyclic peptide API, calcineurin inhibitor API, immunosuppressant API, lupus nephritis API and nephrology pharmaceutical ingredient.
Voclosporin API should be stored and handled according to its applicable quality specification, stability data, safety documentation and validated manufacturing requirements.
Because the substance is a complex cyclic peptide and is sensitive to its chemical environment, appropriate controls for temperature, moisture, light and container closure should be established from stability studies rather than assuming unsupported universal storage conditions.
Pharmaceutical manufacturing facilities should also implement suitable handling procedures and analytical controls when working with Voclosporin.
Voclosporin is an important specialized API for pharmaceutical development involving immune-mediated renal disease. Its cyclic peptide structure, calcineurin inhibition mechanism and application in lupus nephritis make it distinct from conventional low-molecular-weight pharmaceutical ingredients.
For manufacturers and pharmaceutical developers, appropriate control of the API's identity, assay, isomeric composition, purity and related substances is essential. Reliable analytical characterization supports consistent production of finished pharmaceutical formulations.
As a specialized pharmaceutical ingredient, Voclosporin can be positioned for applications involving immunosuppressive medicines, calcineurin inhibitor formulations, lupus nephritis therapies and nephrology-focused pharmaceutical development.
Voclosporin is a cyclic peptide and cyclosporine A analog classified as a calcineurin inhibitor immunosuppressant. It has the empirical formula C63H111N11O12 and a molecular weight of 1214.6 g/mol. The FDA describes the active ingredient as approximately 90–95% trans-isomer and as a white to off-white solid.
Voclosporin is practically insoluble in water at less than 0.1 g/L at 20°C, while it is freely soluble in acetone, acetonitrile, ethanol and methanol. Its reported thermal behavior is melting above 144°C with decomposition.
With its established application in lupus nephritis, Voclosporin is an important immunosuppressant, calcineurin inhibitor and cyclic peptide API for pharmaceutical manufacturing and development.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Water Content | NMT 0.5% |
| Melting Point | >144°C with decomposition |
| Solubility | <0.1 g/L at 20°C in water (<0.1 mg/mL) |