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A Phase 1 Study Of Trc102, An Inhibitor Of Base Excision Repair, And Pemetrexed In Patients With Advanced Solid Tumors, Michael S. Gordon, Lee S. Rosen, David Mendelson, Ramesh K. Ramanathan, Jonathan Goldman, Lili Liu, Yan Xu, Stanton L. Gerson, Stephen P. Anthony, William D. Figg, Shawn Spencer, Bonne J. Adams, Charles P. Theuer, Bryan R. Leigh, Glen J. Weiss
A Phase 1 Study Of Trc102, An Inhibitor Of Base Excision Repair, And Pemetrexed In Patients With Advanced Solid Tumors, Michael S. Gordon, Lee S. Rosen, David Mendelson, Ramesh K. Ramanathan, Jonathan Goldman, Lili Liu, Yan Xu, Stanton L. Gerson, Stephen P. Anthony, William D. Figg, Shawn Spencer, Bonne J. Adams, Charles P. Theuer, Bryan R. Leigh, Glen J. Weiss
Chemistry Faculty Publications
Introduction TRC102 potentiates the activity of cancer therapies that induce base excision repair (BER) including antimetabolite and alkylating agents. TRC102 rapidly and covalently binds to apurinic/apyrimidinic (AP) sites generated during BER, and TRC102-bound DNA causes topoisomerase II-dependent irreversible strand breaks and apoptosis. This study assessed the safety, maximum-tolerated dose (MTD), pharmacokinetics and pharmacodynamics of TRC102 alone and in combination with pemetrexed. Purpose Patients with advanced solid tumors received oral TRC102 daily for 4 days. Two weeks later, patients began standard-dose pemetrexed on day 1 in combination with oral TRC102 on days 1 to 4. The pemetrexed-TRC102 combination was repeated every …