"Patients with medullary thyroid cancer are a highly underserved population as there is no active approved therapy available at this time. Targeted therapeutics, such as dual inhibitors of RET and VEGFR2, are the first compounds showing activity in this disease. The phase 1 results of XL184, the first such molecule in this class also to inhibit the oncogenic MET receptor, were reported today by Drs. Salgia and Kurzrock, and are remarkable, both in terms of the high frequency of responses and how rapidly they occur," said Steven I. Sherman, MD, Chair and Professor, Department of Endocrine Neoplasia and Hormonal Disorders, University of Texas M.D. Anderson Cancer Center, Houston, Texas. "I am looking forward to the phase 3 trial of XL184 in this indication and believe that studies like this will importantly advance the care of patients with medullary thyroid cancer."
The data indicate that XL184 was generally well-tolerated at the MTD of 175 mg QD (capsule). Adverse events related to study drug included diarrhea, nausea, fatigue, mucositis, anorexia, elevation of liver enzymes, hypertension, vomiting, hair hypopigmentation, and palmar-plantar erythema. Dose-limiting toxicities included palmar-plantar erythema, elevation of liver enzymes, lipase elevation, and mucositis.
Pharmacokinetic analyses indicate that the half-life of XL184 was
approximately 100 hours (range 59-136 hours), with exposure at the MTD
exceeding that required for efficacy in preclinical models. Pharma
|SOURCE Exelixis, Inc.|
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