Overview
Alpelisib is a small molecule inhibitor of the phosphatidylinositol-3-kinase (PI3K) pathway, specifically targeting the alpha isoform (PI3Kα). It is primarily used in the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer. Developed by Novartis, it is marketed under the brand name Piqray. Alpelisib works by inhibiting the PI3K pathway, which is often hyperactive in cancer cells, leading to uncontrolled cell growth. It is typically used in combination with fulvestrant, an estrogen receptor antagonist, to enhance therapeutic efficacy.
Physical and Chemical Properties
Alpelisib is a white to off-white powder with a molecular weight of 441.47 g/mol. Its molecular formula is C19H22F3N5O2S, and it is soluble in dimethyl sulfoxide (DMSO) and slightly soluble in water. The compound is stable under recommended storage conditions but should be protected from light and moisture to prevent degradation. The chemical structure of alpelisib includes a trifluoromethyl group and a sulfonylurea moiety, which contribute to its selective inhibition of PI3Kα. Its pharmacokinetic properties include good oral bioavailability and a half-life that supports once-daily dosing.
Main Applications
Alpelisib is primarily used in the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer, particularly in patients with PIK3CA mutations. These mutations are present in approximately 40% of HR-positive breast cancers and are associated with resistance to endocrine therapy. In clinical trials, alpelisib in combination with fulvestrant has shown significant improvement in progression-free survival compared to fulvestrant alone. It is also being investigated for use in other cancers with PI3K pathway alterations, such as head and neck squamous cell carcinoma and gynecological cancers.
Safety and Storage
Alpelisib should be handled with care, as it is a potent pharmaceutical compound. Personal protective equipment, including gloves and safety glasses, should be worn to avoid skin contact and inhalation. The compound should be stored at -20°C in a tightly sealed container, protected from light and moisture. Common side effects of alpelisib include hyperglycemia, rash, diarrhea, and fatigue. Patients receiving this drug should be monitored for signs of severe hypersensitivity reactions and elevated blood glucose levels. Proper disposal methods should be followed to prevent environmental contamination.
B2B Procurement Guide
When procuring alpelisib, B2B buyers should prioritize suppliers who adhere to Good Manufacturing Practices (GMP) and can provide a Certificate of Analysis (CoA) to verify purity and potency. The reference price range is approximately $10,000 - $15,000 per kilogram, but prices may vary based on quantity and supplier. Buyers should also consider the stability and shelf life of the product, ensuring that storage and transportation conditions meet the recommended guidelines. It is advisable to establish long-term relationships with reputable suppliers to ensure consistent quality and availability.
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