A phase Ia study of CC-90003, a selective extracellular signal regulated kinase (ERK) inhibitor, in patients with relapsed or refractory BRAF or RAS-mutant tumors.
Monica M Mita, Patricia LoRusso, Grant A McArthur, Edward S Kim, Gordon L Bray, Nanette H Hock, Eric J Laille, Ida Aronchik, Ellen Filvaroff, Xiaoling Wu, Johanna C Bendel
JOURNAL OF CLINICAL ONCOLOGY | AMER SOC CLINICAL ONCOLOGY | Published : 2017
2577 Background: CC-90003 is an irreversible inhibitor of ERK 1/2 with potent anti-proliferative activity in KRAS and BRAF mutant tumor models. We conducted a first-in-human study of CC-90003 in patients with RAS or BRAF mutant tumors. Methods: Patients received escalating doses of oral CC-90003 on a 21/28 day cycle. Standard safety (adverse events, chemistry/hematology, physical findings, ECGs and cardiac ECHO/MUGA scans) and PK parameters were assessed. Response was assessed per RECIST 1.1. A proprietary ELISA-based assay measured ERK levels unbound to CC-90003 in peripheral blood mononuclear cells. Results: Nineteen patients (median age: 60 yrs) harboring KRAS (n = 15), NRAS (n = 1), or ..View full abstract