Table 2.

Summary of Properties from Clinical Trials

Preclinical Trial Properties

IC50: 0.004µm to 0.032 µm

Phase 1 Clinical Trial Properties

Half-life: 5.5 hours Tmax: 1.1 Confirmed response rate: 35.5% Disease control: 91.2% Median time to response: 1.4 months Median DOR: 10.9 months PFS: 6.3 months Most common side effects: Diarrhea, nausea Patients with grade ¾ events: 11.6% Grade 3 events: Elevated ALT and AST, diarrhea, anemia, hepatitis, lymphopenia, elevated GGT, hyponatremia Grade 4 event: Elevated ALT

Phase 2 Clinical Trial Properties

ORR: 37.1% Disease Control: 80.6% Stable disease: 43.5% Progressive disease: 16.1% Median DOR = 11.1 months Median time to response: 1.4 months Median duration of treatment: 5.5 months PFS: 6.8 months Most common side effects: diarrhea, nausea, fatigue, arthralgia, elevated ALT or AST

Abbreviations: ORR, objective response rate; DOR, duration of response; PFS, progression-free survival; ALT, alanine aminotransferase; AST, aspartate aminotransferase.