An Open-label, Multi-center, Dose-escalation Phase 1 Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of ETN101 in Patients With Advanced Hepatocellular Carcinoma
ETN101 is a multiple tyrosine kinase inhibitor (mTKI) targeting fms-like tyrosine kinase 3 (FLT3), receptor tyrosine kinase (KIT), vascular endothelial growth factor receptor 2 (VEGFR2), and platelet-derived growth factor receptor beta. Both in vitro and in vivo studies showed that ETN101 treatment/administration inhibited cancer cell survival and proliferation. In animal models, ETN101 had antitumor activity when administered to animals that did not respond to conventional targeted anticancer agents.
• Male and female adult at the age of ≥ 19 years old
• Patients with radiologically or histologically, and/or cytologically confirmed advanced HCC who have confirmed disease progression on standard therapies known to have clinical benefit or for whom there is no currently available standard therapy due to intolerance or incompatibility.
• Subject with Barcelona Clinic Liver Cancer (BCLC) stage B or C; Subject with Stage B must have had progressive disease (PD) after radical resection, liver transplant, embolization, or cauterization or must be ineligible for such treatment.
• Subject with Child-Pugh score A (5-6)
• Subject who has at least one measurable target lesion based on modified RECIST (mRECIST) which was not previously treated with local therapy. A lesion previously treated with local therapy may be selected as a target lesion if an increase of ≥20% in size is confirmed after treatment.
• Subject with Eastern Cooperative Oncology Group (ECOG) status performance 0-1.
• Subject with ≥ 12 weeks of life expectancy
• Subject who meets the following criteria for laboratory tests (Subject must not have been treated with granulocyte colony-stimulating factor (G-CSF) or blood transfusions within 14 days prior to the laboratory tests.):
‣ Hematology
• Absolute neutrophil count(ANC) ≥1,500/mm3
∙ Platelet count ≥60,000/mm3
∙ Hemoglobin(Hb) ≥8.5 g/dL
⁃ Kidney function: Serum creatinine ≤1.5 × upper limit of normal(ULN)
⁃ Liver function
• Aspartate aminotransferase(AST) and alanine aminotransferase(ALT) ≤5 × ULN
∙ Total bilirubin ≤2.0 × ULN (≤3.0 × ULN for Gilbert's disease)
⁃ Blood coagulation function: Prothrombin time (PT/INR) and activated partial thromboplastin time (aPTT) ≤1.5 × ULN
• Subject who voluntarily agrees to participate in the study and signs the informed consent form (ICF) after being fully informed of the study