Arvinas announces presentations for two PROTAC research programs

Arvinas presented new preclinical data from its investigational BCL6 degrader PROTAC ARV-393 at the European Hematology Association 2024 Annual Congress held June 13-16, 2024 in Madrid, Spain, and presented new preclinical data from its PROTAC LRRK2 degrader program at the International Biennale. LRRK2 meeting which took place June 18-21, 2024 in Crete, Greece. Data presented at EHA showed antitumor activity of the company’s investigational PROTAC BCL6 degrader, ARV-393, in preclinical models of B-cell lymphoma. In these preclinical models, ARV-393 potently and rapidly degraded BCL6 protein and inhibited cell growth in diffuse large B-cell lymphoma and Burkitt cell lines. ARV-393 showed inhibition of tumor growth, including tumor regression, in various xenograft models derived from DLBCL cell lines and in several xenograft models derived from non-Hodgkin’s lymphoma patients, including activated B cells. B cell type of the germinal center, the GCB. /ABC, BCL, unspecified subtypes of DLBCL and Burkitt lymphoma. Preclinical data presented at the LRRK2 Biennial Meeting highlighted the potential of the Company’s PROTAC LRRK2 oral degraders to treat neurodegenerative diseases. Preclinical studies in mice demonstrated complete target engagement of the LRRK2 kinase inhibitor and near complete degradation of LRRK2 with PROTAC LRRK2 degraders, but significantly less type II pneumocyte hypertrophy compared to an inhibitor. experimental of the LRRK2 kinase. Additionally, the more visible type II pneumocyte enlargement phenotype observed with the investigational LRRK2 kinase inhibitor was corroborated by the accumulation of surfactant protein C in the lungs, which was not observed after a treatment with a PROTAC LRRK2 degrader. Arvinas’ PROTAC BCL6 oral degrader, ARV-393, is currently in a Phase 1 clinical trial in NHL patients, and Arvinas also has a PROTAC LRRK2 oral degrader, ARV-102, currently studied in a phase 1 clinical trial in healthy volunteers.