Tumor-directed Inhibition Research Unit

About Us

Our unit is responsible for research on Targeted Protein Degradation (TPD), a Primary Focus Candidate. Our goal is to create novel drugs targeting important cancer dependent aberrant proteins that have historically been considered undruggable.

*Please check here to learn more about the Primary Focus Candidate.
 

Our Approach

Our approach

 We focus on TPD, which is a heterobifunctional chemical molecule among targeted protein degradation-related modality. TPD promotes ubiquitination of target proteins by inducing the proximity between target proteins and E3 ubiquitin ligases, leading to protein degradation by the proteasome.
 Conventional small molecule drugs require a functional deep pocket in the target protein. TPD, however, only weakly binds to a shallow pocket on the target protein, catalytically inducing the proximity of the target protein to the E3 ligase, and selectively degrading the target protein. Thus, TPD can be applied to a wider range of proteins, including historical undruggable proteins, because it can even utilize a shallow pocket, which normally present in most proteins.
 

Our approach

 

ASP3082

Applying the concept of TPD, we have discovered ASP3082, a first-in-class and selective KRAS G12D degrader. Phase I clinical trials are currently underway in the U.S. to study the efficacy and safety of the drug for pancreatic cancer, colorectal cancer, and lung cancer with KRAS G12D mutation.
 


 

Teams

Masahiko Hayakawa, Ph.D.

Unit Head

Masahiko Hayakawa, Ph.D.

Dr. Hayakawa has led research activities in the field of oncology and urology, creating multiple clinical and launched products. In 2012, he moved to the planning department and participated in strategy planning for Astellas’ research division. He assumed the Executive Director role in Modality Management in 2018. He has been in his present position since 2019.
 

Message from Unit Head

Our goal is to deliver new therapeutic options to patients suffering from cancers that have been difficult to treat with conventional drug therapies. We will continue our efforts to contribute to the future of cancer patients and their families.

 

Partnering

To further enhance our research capabilities and portfolio, we are currently partnering or looking for potential partners in biotech and academia in the following areas:

  • Novel TPD platform technology
  • Research programs based on TPD technology
  • New technology to identify shallow pocket binders for the undruggable targets

Careers

We are excited about working with anyone who is interested in providing new value to patients through targeted protein degradation technology. Check out our open positions and please contact us if you are interested in working with us.