RET Inhibitor Tested in Multiple Tumor Types

Arielz Katz
Published: Wednesday, Aug 01, 2018
Dr Alexander Drilon

Alexander Drilon, MD
Investigators are evaluating the potential of LOXO-292, an oral small molecule inhibitor of RET signaling, to improve outcomes in patients with RET fusion–positive non–small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), and other tumors with increased RET activity. RET mutations drive tumor proliferation and growth and are particularly common in NSCLC and MTC.

These cancers represent an unmet need because no targeted agents are currently approved for patients with RET mutation–specific tumors, according to Alexander Drilon, MD, clinical director of the Early Drug Development Service at Memorial Sloan Kettering Cancer Center (MSK) in New York, New York. “It’s a substantial population,” he said. “RET fusions are found [commonly] in NSCLC, papillary thyroid cancers, and other tumors; RET point mutations are enriched in medullary thyroid cancers.”

The phase I/II open-label LIBRETTO-001 clinical trial (NCT03157128) is currently testing LOXO-292 in these patient populations (Table). The phase I portion of the trial sought to determine the safety and recommended dosage of the drug. This is still ongoing, but a recommended phase II dose for LOXO-292 was determined to be 160 mg twice per day.

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