Abstract
Bristol Myers Squibb has agreed to buy Turning Point Therapeutics in a deal valued at $4.1 billion. Turning Point’s lead drug candidate, repotrectinib, is a small-molecule tyrosine kinase inhibitor (TKI) for patients with ROS1 -positive advanced non-small-cell lung cancer (NSCLC) and other cancers. The drug would compete with Pfizer’s Xalkori and Roche’s Rozlytrek, both approved by the US Food and Drug administration to treat metastatic ROS1 -positive NSCLC. Receptor tyrosine kinases are proteins that are part of cellular signaling cascades, and their dysfunction is known to be behind many types of cancer. TKIs treat tumors by targeting these malfunctioning proteins. In the case of ROS1-positive NSCLC, the receptor tyrosine kinase–encoding gene ROS1 fuses with another gene, and the resulting kinase becomes a driver of cancer cell growth. Repotrectinib was designed to nestle into the ATP binding pocket of that kinase, preventing ATP binding and blocking the signal cascade that allows
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