Zenopharm is a startup founded in 2012 to commercialize innovative oncology therapeutics based on its patented platform technology. ZB716 is an oral SERD developed to overcome clinical limitations of fulvestrant, including poor bioavailability, injection-related side effects, slow therapeutic action due to long time-to-steady state drug concentration, and low clinical response rate. ZB716 effectively enhances systemic drug exposure while bypassing first-pass metabolism of fulvestrant. In both wild type ER+ and ER mutant breast cancer cells, ZB716 blocks ER transcriptional activities, cell proliferation and degrades ER in a dose-dependent manner. Moreover, ZB716 has far superior oral bioavailability compared to fulvestrant and greater efficacy in blocking tumor growth in patient derived xenograft (PDX) breast cancer models. Zenopharm received SBIR Phase I and II awards to conduct IND-enabling studies of ZB716 to move towards a first in human clinical trial.
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