Tafetinib is an oral multitargeted tyrosine kinase inhibitor that inhibits Vascular Endothelial Growth Factor Receptor (VEGFR).

This phase I trial was conducted to evaluate the pharmacokinetics (PK), safety, and preliminary efficacy of tafetinib in Chinese patients with advance solid tumor. The study are conducting in Cancer Hospital Chinese Academy of Medical Sciences.

Inclusion Criteria:

• Adult patients with histologically confirmed advanced solid malignancies.
• ECOG score 0-1.
• 18-65 years old.
• Withdrawal other chemotherapy drugs more than 30 days. No nitrosoureas or mitomycin C within the previous 6 weeks.
• Function of organs must meet the following requirements:
• Neutrophil count ≥1500/ul;
• AST and ALT≤1.5 times the upper limit of normal (ULN);
• Total serum bilirubin≤1.5 times ULN;
• Hemoglobin≥90g/L;
• Platelet≥100000/ul;
• The creatinine in the normal range or creatinine clearance rate ≥60ml/min;
• Left ventricular ejection fraction (LVEF) ≥50%;
• Females of childbearing age are required to be practicing effective contraceptive measures and to have a negative serum or urine pregnancy test before study.
• Written informed consent is obtained.

Exclusion Criteria:

• included a history of or current brain metastases, clinically significant cardiovascular disease or uncontrolled hypertension.