Abstract: 【Objective】 To determine the dose limited toxicities and maximum tolerated dose of continuous daily XC302 in Chinese patients with advanced solid tumors

as well as it’s tolerability and preliminary antitumor activity. 【Methods】 Patients with histologically confirmed advanced/refractory solid tumors were assigned into 4 cohorts to received oral XC302 once or twice daily. Dosing of XC302 escalated from 50 mg/d and guided by a “3+3”model or modified according to previous results. Adverse events were recorded according to NCI CTCAE version 3.0. Assessment of response was performed radiologically according to RECIST version 1.0.【Results】 Totally 30 patients were enrolled. Frequent treatment -related adverse events included leukopenia(23.3%)

Ganemia (30%)

nausea (20%)

increased ALT(63.3%)/AST(50%)/ALP(23.3%)/GGT(26.7%) levels. Reversible abnormal hepatic function (increased ALT/AST levels) was documented as it’s DLT. MTD for continuous administration of XC302 was 100 mg qd (fasting) and 75mg qd (postprandial). Best overall response was stable disease for 12 of 23 patients who underwent response evaluation

including one experienced long PFS of 64 weeks. 【Conclusion】 Continuous daily XC302 treatment demonstrates a manageable safety profile and promising disease control rate in Chinese patients with advanced solid tumors

which deserves further investigation.