Recent disclosures of clinical candidates - Highlights from the Society for Medicines Research Symposium, held on December 8, 2011 at The National Heart and Lung Institute, South Kensington, London, UK
Drugs of The Future(2012)
摘要
Dr. Mark Mulvihill (OSI Pharmaceuticals) described the discovery and development of linsitinib (OSI-906), a potent and highly selective dual inhibitor of insulin-like growth factor 1 receptor (IGF-I receptor) and insulin receptor (IR) signaling, currently undergoing clinical evaluation in a number of cancers, including adrenocortical carcinoma (ACC) (1). IGF-I receptor, IR and IGF-I receptor/IR dimers are receptor tyrosine kinases (RTKs), which when activated on binding of their cognate ligands IGF-I, IGF-II and insulin, trigger critical signaling pathways involved in the etiology, progression and prognosis for a number of human cancers. Signaling through the IGF-I receptor has been linked to tumor cell proliferation and survival, as well as a key contributor toward tumor cells acquiring resistance to current anticancer therapeutics, including chemoand radiotherapies, as well as targeted small-molecule agents or antibodies. Although the IR signaling axis is still being unraveled, evidence has accumulated supporting a role in promoting tumor cell proliferation. Clinically, in both prostate and breast cancer patients, elevated
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关键词
clinical candidates,medicines research symposium,lung institute,recent disclosures
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