Primary Focus Targeted Protein Degradation

Approach

Only about 20% of disease-related proteins have active binding sites (or sufficiently deep pockets) suitable for inhibition by conventional molecular targeted drugs. The remaining 80% have shallow binding pockets and their function cannot be significantly controlled by binding alone. These are called ‘undruggable’ targets as they are considered difficult to be drug targets. We are using Targeted Protein Degradation to access these undruggable targets. The advantages of protein degraders, in addition to their ability to access undruggable targets, includes their permeability (they can penetrate the cell membrane and blood brain barrier), and their high levels of specificity to the target. We are confident that this Targeted Protein Degradation technology will bring innovative clinical benefits to patients.

Click here to learn more about the mechanism of action of protein degraders.

Astellas has the following capabilities:

• Chemical synthesis expertise and technology to create protein degrader compounds
• Proprietary target protein binders and next-generation E3 binders
• State-of-the-art compound modeling technology utilizing AI and robotics
• Development and commercialization experience and expertise in various disease areas including oncology

Targeted Protein Degradation offers expandability through the leverage of our established technology platform. For example, by converting target proteins, we believe it can be applied in a wide variety of indications and therapeutic areas. We are also challenging ourselves to create next-generation protein degraders that can be combined with other technologies and that have tissue selectivity.

Pipeline

Our lead program, ASP3082, is a novel protein degrader, originally discovered by Astellas, that targets mutated KRAS G12D, and is currently in Phase I clinical trials for the treatment of solid tumors. KRAS mutations are one of the most frequently occurring cancer-causing genetic mutations, of which KRAS G12D is known as one of the main ones. Astellas has established strong R&D and commercial expertise in developing and commercializing targeted medicines such as XOSPATA^® (gilteritinib). We are passionate in our efforts to deliver effective treatments to cancer patients as soon as possible.

We also have a robust and competitive pipeline consisting of differentiated protein degraders and their backups for ‘undruggable’ targets.

Partnering

We are pursuing innovation by maximizing the advantages of our Targeted Protein Degradation technology platform.

Assets and capabilities of interest:

• Target molecules which best fit to TPD technology
• New technology to identify shallow pocket binders for undruggable targets
• Novel TPD platform technology/E3 binder

Talent:

• Astellas is actively recruiting talented professionals with extensive experience and knowledge in cutting-edge science and who are passionate about research and development of innovative drugs

Our aim is to create a brighter future for our patients and their caregivers by working to make undruggable targets druggable. With our team’s diversity and strong expertise in research, development, manufacturing and commercialization, we strive daily towards creating innovative new drugs to meet this aim. Collaboration with highly specialist partners is also indispensable for us to achieve our goal.
By calling upon the wisdom of both in-house and external professionals, we are pursuing research and development into new innovative treatments to provide relief, at the soonest moment possible, to patients suffering from a range of diseases.

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