DWP221 / Daewoong Pharma, Pin Therap - LARVOL DELTA

Discovery of an orally bioavailable AKT degrader with sustained in vivo efficacy and translational potential (AACR 2026) - "Exploratory combination with fulvestrant further improved tumor growth control, supporting potential therapeutic complementarity in hormone receptor-positive tumors. DWP221/PIN002 was well tolerated throughout the study period, without notable body-weight loss or overt signs of systemic toxicity, and maintained a favorable exposure-response relationship consistent with its drug-like properties.This study demonstrates that an orally bioavailable AKT degrader can achieve durable target suppression and in vivo efficacy through sustained exposure and efficient target engagement. These findings support that targeted protein degradation may overcome key limitations of conventional kinase inhibition and provide a differentiated approach toward next-generation targeted therapies for PI3K-AKT-driven cancers."

Preclinical • Oncology • Solid Tumor • PIK3CA