Pasireotide API is a synthetic cyclic peptide and somatostatin analogue developed as a long-acting pharmaceutical active ingredient. Pasireotide is also known by the development code SOM230 and is structurally different from first-generation somatostatin analogues because it has a broader somatostatin receptor binding profile. It acts primarily through somatostatin receptor subtypes and is used in pharmaceutical treatment of endocrine disorders.
The active moiety Pasireotide has CAS Number 396091-73-9, molecular formula C58H66N10O9, and molecular weight 1047.20 g/mol. PubChem identifies Pasireotide as a synthetic homodetic cyclic peptide containing seven defined stereocenters.
For the approved pharmaceutical product, the active substance is supplied as Pasireotide Diaspartate. Pasireotide diaspartate has CAS Number 820232-50-6, molecular formula C66H80N12O17, and molecular weight 1313.41 g/mol. FDA documentation confirms that the pharmaceutical active substance is pasireotide diaspartate.
Regulatory documentation describes Pasireotide Diaspartate as a fully synthetic active substance produced through peptide synthesis, purification, formation of the diaspartate salt and lyophilization. The drug substance is described as a white to slightly greyish powder.
Pasireotide is a somatostatin receptor agonist used in pharmaceutical treatment of endocrine disorders. The approved injectable product Signifor contains pasireotide as the diaspartate salt. FDA documentation describes strengths of 0.3 mg/mL, 0.6 mg/mL and 0.9 mg/mL for subcutaneous injection.
Pasireotide is particularly associated with treatment of Cushing's disease in patients for whom pituitary surgery is not an option or has not been curative. Regulatory approvals also include use in other endocrine indications depending on the specific formulation and jurisdiction.
For pharmaceutical API documentation, it is important to distinguish Pasireotide free active moiety from Pasireotide Diaspartate.
Pasireotide free active moiety:
CAS: 396091-73-9
Formula: C58H66N10O9
Molecular Weight: 1047.20 g/mol
Pasireotide Diaspartate:
CAS: 820232-50-6
Formula: C66H80N12O17
Molecular Weight: 1313.41 g/mol
FDA and PubChem records support these separate identities.
Because Pasireotide is a synthetic peptide, its quality control differs from conventional small-molecule APIs. EMA documentation reports testing of the active substance for appearance, clarity and colour of solution, IR and RP-HPLC identification, related substances, RP-HPLC assay, aspartic acid content, amino-acid composition, residual solvents, water, sulphated ash, specific optical rotation, heavy metals, microbial purity and endotoxins.
This broad analytical profile is appropriate for a complex synthetic peptide and its salt form. Related substances are controlled using criteria applicable to synthetic peptides under the European Pharmacopoeia framework.
A qualified Pasireotide API Manufacturer in India should maintain strict control over peptide synthesis, coupling reactions, deprotection, purification, salt formation and lyophilization. Regulatory documentation describes a solid-phase peptide synthesis route followed by chromatographic purification and formation of the diaspartate salt.
Manufacturing controls should address peptide identity, stereochemical integrity, related peptide impurities, counter-ion content, residual solvents, water, endotoxins and microbiological quality.
Pasireotide is also described as hygroscopic and light-sensitive, making appropriate packaging, storage and stability controls important.
Pasireotide should not be treated as a conventional small-molecule API when entering CMS specification values. In particular, the pharmaceutical drug substance is a synthetic peptide and is supplied as a defined salt. Therefore, assay, related substances, water, optical rotation and counter-ion content should be controlled according to the applicable approved specification.
Public regulatory assessment reports confirm the analytical tests but do not disclose every numerical commercial acceptance limit. Therefore, unsupported numerical assay or impurity limits should not be inserted into the CMS.
Pasireotide active substance is light-sensitive and hygroscopic. Regulatory stability data support controlled storage conditions, and the Australian assessment reported a drug-substance retest period supported by storage at −15°C to −25°C.
Actual commercial storage conditions should be taken from the applicable approved specification and validated stability data.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |