In a preclinical tauopathy model, a tau-targeted PROTAC® protein degrader crosses the blood brain barrier and removes more than 95% of pathologic tau
NEW HAVEN, Conn., July 18, 2019 (GLOBE NEWSWIRE) -- Arvinas, Inc. (ARVN), a biotechnology company creating a new class of drugs based on targeted protein degradation, announced it will present preclinical data from its tau-targeted PROTAC® protein degrader program at the Alzheimer's Association International Conference (AAIC®), held July 14-18, 2019, in Los Angeles, California. Angela Cacace, Ph.D., Vice President of Neuroscience and Platform Biology at Arvinas, was selected to chair the session entitled, Molecular and Cell Biology: Tau Biology, Aggregation and Spreading. In this session, Dr. Cacace will give an oral presentation entitled “A New Therapeutic Strategy for Tauopathies - Discovery of Highly Potent Brain-Penetrant PROTAC® Degrader Molecules That Target Pathologic Tau Protein Species.” This presentation will also discuss Arvinas’ strategy in creating PROTAC® targeted protein degraders for neurological disorders.
The preclinical studies show a tau-targeted PROTAC® protein degrader eliminated more than 95% of disease-causing (pathologic) tau protein in the brain of a well-characterized mouse tauopathy model, following parenteral (peripheral) administration. The data further indicate that the tau protein degradation is dose and concentration dependent, signifying the tau-targeted PROTAC® protein degrader molecule effectively crosses the blood brain barrier.
“These data indicate the potential for PROTAC® protein degraders in diseases of the central nervous system, reinforcing our belief that there are many indications, including previously ‘undruggable’ targets, for which our technology may be advantageous,” said Dr. Cacace. “The fact that these degraders have both crossed the blood-brain barrier, and specifically degraded pathologic tau, increases our conviction and excitement in moving additional PROTAC® protein degrader programs forward in neuroscience.”
Tau has been implicated in several neurological disorders, including Alzheimer’s disease. At AAIC, Dr. Cacace will detail Arvinas’ strategy in neuroscience, which will include initially pursuing indications that are “pure” tauopathies, such as progressive supranuclear palsy (PSP) and genetic tauopathies, such as frontotemporal dementia with parkinsonism-17 (FTDP-17), to prove the effectiveness of tau-directed PROTAC® protein degraders. Arvinas has additional preclinical neuroscience programs, including alpha-synuclein (implicated in Parkinson’s disease), as well as a robust, clinical-stage oncology pipeline.
AAIC® is the premier and largest international meeting focused on advancing Alzheimer’s and dementia science. The annual conference convenes the world's leading basic science and clinical researchers, next-generation investigators, clinicians and the care research community to share research discoveries supporting new methods of prevention, treatment and diagnosis of Alzheimer's disease.
- Session Title: Molecular and Cell Biology: Tau Biology, Aggregation and Spreading
- Talk Title: A New Therapeutic Strategy for Tauopathies - Discovery of Highly Potent Brain-Penetrant PROTAC® Degrader Molecules That Target Pathologic Tau Protein Species
- Date and Time: Thursday, July 18, 2019 at 12:45pm PT
- Location: Los Angeles Convention Center, Petree Hall D
About PROTAC® Protein Degraders
Arvinas’ PROTAC® protein degraders harness the body’s own natural protein disposal system to degrade disease-causing proteins. PROTAC® protein degraders recruit an E3 ligase to tag the target protein with ubiquitin, which directs its degradation through the proteasome, a large protein complex that breaks down the ubiquitinated target protein into small peptides and amino acids. As the target protein is degraded, the PROTAC® protein degrader is released and acts iteratively to destroy additional target protein.
PROTAC® protein degraders offer numerous potential advantages as a therapeutic, including broad tissue distribution (including the ability to design for blood brain barrier penetration), routes of administration that include oral delivery, and simpler manufacturing than other new modalities, such as cell-based therapies. Arvinas has developed and optimized a proprietary library of protein targeting ligands, E3 ligase ligands, and linkers, which allow the company to rapidly identify and optimize efficient protein degraders with favorable characteristics for successful drug development.
Arvinas is a clinical-stage biopharmaceutical company dedicated to improving the lives of patients suffering from debilitating and life-threatening diseases through the discovery, development, and commercialization of therapies that degrade disease-causing proteins. Arvinas uses its proprietary technology platform to engineer proteolysis targeting chimeras, or PROTAC® targeted protein degraders, that are designed to harness the body’s own natural protein disposal system to selectively and efficiently degrade and remove disease-causing proteins. The company’s lead program, ARV-110 for the treatment of patients with metastatic castrate-resistant prostate cancer, began a Phase 1 clinical trial in the first quarter of 2019. For more information, visit www.arvinas.com.
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Contacts for Arvinas
Will O’Connor, Stern Investor Relations
Cory Tromblee, ScientPR