New Preclinical Data from Arvinas’ Investigational PROTAC Degraders
Arvinas, Inc. (Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation, recently presented new preclinical data from its investigational degraders at two separate events.
ARV-393’s Anti-Tumor Activity in B-Cell Lymphoma Models
At the European Hematology Association (EHA) 2024 Annual Congress held in Madrid, Spain, Arvinas presented preclinical data on its investigational BCL6 PROTAC degrader ARV-393, which showed anti-tumor activity in models of B-cell lymphoma.
BCL6 is a transcriptional repressor and major driver of B-cell lymphomas. ARV-393 potently and rapidly degraded the BCL6 protein, inhibiting cell growth in diffuse large B-cell lymphoma (DLBCL) and Burkitt cell lines. In various DLBCL cell line-derived xenograft (CDX) models and in multiple patient-derived xenograft (PDX) models of non-Hodgkin lymphoma (NHL), including germinal center B-cell-like (GCB), activated B-cell (ABC), GCB/ABC, BCL not otherwise specified (BCL/NOS) subtypes of DLBCL, and Burkitt lymphoma, ARV-393 showed tumor growth inhibition, including tumor regression.
According to John Houston, Ph.D., Chairperson, President, and Chief Executive Officer at Arvinas, “These encouraging results suggest that ARV-393 could be developed into a potential new treatment for patients with certain types of non-Hodgkin lymphoma, particularly those who have not responded to other treatments.”
PROTAC LRRK2 Degraders in Neurodegenerative Diseases
Arvinas also presented preclinical data from its PROTAC LRRK2 degrader program at the Biennial International LRRK2 Meeting held in Crete, Greece. The presentation highlighted the promise of PROTAC-induced leucine-rich repeat kinase 2 (LRRK2) degradation as a potential treatment for neurodegenerative diseases.
Human genetics indicate that increased activity and expressions of LRRK2 are genetically involved in the pathogenesis of neurological diseases, including Parkinson’s Disease and progressive supranuclear palsy. Arvinas’ oral, blood-brain-barrier penetrant PROTAC degraders of LRRK2 showed tremendous potential in preclinical studies conducted in mice. Full target engagement and near-complete LRRK2 degradation were observed with substantially fewer side effects.
ARV-393 and ARV-102 in Clinical Trials
Arvinas is currently conducting a phase 1 clinical trial for ARV-393, an investigational PROTAC designed to degrade BCL6 protein, in patients with non-Hodgkin lymphoma. It also has an oral, blood-brain-barrier penetrant PROTAC LRRK2 degrader, ARV-102, currently being investigated in a phase 1 clinical trial in healthy volunteers.
About Arvinas
Arvinas is a clinical-stage biotechnology company dedicated to improving the lives of patients suffering from debilitating and life-threatening diseases. Through its PROTAC (PROteolysis Targeting Chimera) protein degrader platform, the company is pioneering the development of protein degradation therapies designed to harness the body’s natural protein disposal system to selectively and efficiently degrade and remove disease-causing proteins.
Arvinas is advancing multiple investigational drugs through clinical development programs, including vepdegestrant, targeting estrogen receptor for patients with locally advanced or metastatic ER+/HER2- breast cancer; ARV-102, targeting LRRK2 for neurodegenerative disorders; and ARV-393, targeting BCL6 for relapsed/refractory non-Hodgkin Lymphoma.
Arvinas is headquartered in New Haven, Connecticut. For more information about the company, please visit their official website: https://arvinas.com/.
Conclusion
Arvinas’ recent presentations of preclinical data for its investigational degraders at the EHA 2024 Annual Congress and the Biennial International LRRK2 Meeting showed great promise for the treatment of neurodegenerative diseases and non-Hodgkin lymphoma. With ARV-393 and ARV-102 continuing their phase 1 clinical trials, the company is one step closer to providing patients with new treatment options.
Originally Post From https://www.morningstar.com/news/globe-newswire/9157200/arvinas-announces-presentations-for-two-of-its-protac-investigational-programs-targeting-bcl6-and-lrrk2
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