Icotinib hydrochloride

Zhao Q, et al. Lung Cancer, 2011, 73(2), 195-202

Icotinib hydrochloride (BPI-2009H), a selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), was evaluated in a phase I clinical study for patients with advanced solid tumors, predominantly non-small-cell lung cancer (NSCLC). Oral icotinib was administered every 8 h (Q8H) across 28-day cycles until progression or intolerable toxicity. Pharmacokinetic analyses demonstrated a mean elimination half-life of 6 h and Tmax of 2 h, with higher steady-state levels at 125 mg Q8H compared to 100 mg Q8H. Tumor responses were assessed according to RECIST, and mutation profiling of EGFR and K-ras was performed using PCR-based direct sequencing. The trial confirmed favorable tolerability, with common adverse events including rash and diarrhea, while antitumor activity was evident with partial responses and stable disease in EGFR-mutant cases. A recommended phase II/III dose of 125-150 mg Q8H was established.