ARRY-543, a small molecule that is administered orally, was well-tolerated up to 300 mg BID (twice daily). The maximally tolerated dose has not yet been established on the BID dose schedule.
Systemic concentrations of ARRY-543 increased with escalating doses at all dose levels tested and ARRY-543 was able to achieve blood levels that are predicted to provide continuous and profound inhibition of the molecular targets. In completed cohorts, 60% of patients receiving doses of 200 mg BID and higher had prolonged stable disease. Based on these results, the BID regimen has been chosen for phase II studies.
Mace Rothenberg, Ingram professor of cancer research, Vanderbilt-Ingram Cancer Center, said: “I believe ARRY-543 has the potential to be a clinically significant drug in the treatment of patients with ErbB-2/EGFR-driven tumors.”