Vandetanib, sold under the brand name Caprelsa, is an anti-cancer medication that is used for the treatment of certain tumours of the thyroid gland. It acts as a kinase inhibitor of a number of cell receptors, mainly the vascular endothelial growth factor + some more technical info. Vandetanib is an orally active small molecule that inhibits multiple receptor tyrosine kinases including RET, VEGFR2 and EGFR, thereby reducing tumour cell proliferation and tumour-associated angiogenesis through downstream pathways such as MAPK and PI3K-AKT. The compound shows high plasma protein binding, a long terminal half-life on the order of weeks leading to gradual attainment of steady state, and is metabolized primarily via CYP3A4 to an N-desmethyl metabolite; elimination involves both fecal and urinary routes. Clinical dosing and safety monitoring are determined by regulatory labeling and specialist guidance.
The impurity and related compound profile for vandetanib typically comprises controlled related substances such as N-desmethylvandetanib, oxidative and dealkylated degradants, N-oxide species and residual synthetic intermediates; analytical characterization is performed by HPLC and LC-MS and by forced-degradation studies to define stability-indicating impurities. Typical specification limits used in quality dossiers limit total impurities to around 2.0 percent w/w or less, with individual unspecified impurities commonly restricted to the range of 0.2 to 0.5 percent w/w and identified related compounds often limited to 0.5 to 1.0 percent pending qualification; exact limits are established per regulatory submission and batch release criteria.
Vandetanib is indicated for the treatment of certain progressive, unresectable or metastatic medullary thyroid carcinoma and is prescribed under specialist oncology guidance.
Vandetanib inhibits multiple receptor tyrosine kinases including RET, VEGFR2 and EGFR, blocking signal transduction pathways that drive tumour cell growth and tumour angiogenesis.
Vandetanib is also sold under the brand name Caprelsa and may be referenced chemically as vandetanib mesylate in some formulations.
Vandetanib was developed and marketed by AstraZeneca; brand availability and marketing authorization vary by country.
