Overview
Pasireotide is a cyclohexapeptide somatostatin analogue developed for its potent binding affinity to somatostatin receptors, particularly subtype 5 (sst5). It is structurally distinct from older analogues like octreotide, offering improved efficacy in conditions such as Cushing's disease where other treatments fail. Approved by the FDA in 2012, it is marketed under the brand name Signifor®. As a second-generation somatostatin analogue, pasireotide exhibits a broader receptor binding profile and longer biological half-life, making it suitable for both subcutaneous and intramuscular administration. Its development addressed limitations of first-generation peptides, particularly in hormone-secreting tumors.
Physical and Chemical Properties
Pasireotide is a white to off-white powder with a molecular weight of 1071.21 g/mol. It is soluble in water and polar organic solvents like DMSO, facilitating formulation into injectable solutions. The peptide's stability is pH-dependent, requiring storage at 2-8°C to prevent degradation. Its cyclic structure (cyclohexapeptide) enhances metabolic stability compared to linear peptides. The presence of aromatic amino acids (e.g., phenylalanine) contributes to its high receptor affinity. Analytical methods for quality control typically include HPLC and mass spectrometry to verify purity ≥98%.
Main Applications
Pasireotide is primarily used to treat Cushing's disease, where it reduces cortisol secretion by binding to pituitary somatostatin receptors. Clinical trials demonstrate a 15-26% remission rate in patients unresponsive to surgery. It is also indicated for acromegaly and investigational uses in neuroendocrine tumors (NETs). In acromegaly, pasireotide suppresses growth hormone secretion more effectively than octreotide in approximately 60% of cases. Ongoing research explores its potential in diabetic retinopathy and polycystic liver disease due to its anti-proliferative effects.
Safety and Storage
Pasireotide's most notable adverse effect is hyperglycemia, occurring in up to 73% of patients, necessitating glucose monitoring. Other risks include bradycardia, QT prolongation, and gallstones. Proper handling requires gloves and eye protection to avoid inhalation or skin contact. Storage mandates refrigeration (2-8°C) in original vials protected from light. Reconstituted solutions are stable for up to 4 weeks when refrigerated. Stability under freezing conditions is not well-documented, making lyophilized powder the preferred procurement form for long-term storage.
B2B Procurement Guide
B2B buyers should prioritize suppliers compliant with Good Manufacturing Practice (GMP) to ensure pharmaceutical-grade quality. Key specifications include purity (≥98% by HPLC), endotoxin levels (<5 EU/mg), and sterility for injectable formulations. Bulk purchases (1-10 kg) commonly range between $500-$1,500 per 10 mg, with discounts for long-term contracts. Audit suppliers for ISO 13485 or equivalent certifications. Consider regional regulatory differences—EU and US require detailed CMC (Chemistry, Manufacturing, Controls) documentation. Cold chain logistics are critical; verify shipping conditions with temperature tracking.
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