About Us
Our division is responsible for research on Targeted Protein Degradation (TPD), a Primary Focus. 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.
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.
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
Division 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.