On the same day, Express reached a cooperation of more than 2 billion US dollars with two major pharmaceutical companies. What is unique about this cutting-edge protein degradation agent?

▎WuXi AppTec Content Team Editor Today, Amphista Therapeutics announced that it has entered into R&D cooperation with Bristol-Myers Squibb (BMS) and Merck KGaA to develop a new generation of protein degradation based on its unique protein degradation agent discovery platform.
therapy
.

The company closed a $53 million Series B round last year with investors including Novartis Ventures and Eli Lilly
.

Targeted protein degradation is an emerging field of drug development in recent years.
Amphista has been continuously favored by many large pharmaceutical companies.
How is its technology platform different? Targeted protein degradation therapy usually utilizes the inherent protein degradation mechanism in cells to guide the degradation of specific target proteins
.

Protein degraders represented by PROTAC are usually bifunctional molecules, one end of which can bind to the target protein, and the other end binds to the ubiquitin E3 ligase, which prompts the E3 ligase to add ubiquitin modification to the target protein, resulting in the target protein.
Degradation of dot proteins
.

Several PROTAC molecules have shown promising activity in clinical trials
.

Amphista Therapeutics aims to overcome the limitations of first-generation protein degraders, including non-optimized druggable characteristics and oral availability of the molecule, potential resistance to protein degradation mechanisms, and limited cells and tissues in which to act and so on
.

Targeted protein degradation drugs developed by the company can link the target protein and the proteasome degradation system through innovative mechanisms, thereby expanding the application scope of protein degradation agents
.

Image source: Amphista's official website In addition, the company's protein degradation mechanism utilizes proteins that are necessary for tumor cell growth, which means that it is difficult for tumors to develop resistance by mutating these proteins, so the company's degradation mechanism may produce Longer lasting anti-cancer effect
.

Image source: Amphista's official website The company's technology platform also supports targeted protein degradation drugs with better drug characteristics, including oral availability, effective tissue penetration (including the central nervous system)
.

Image source: Amphista's official website In cooperation with Merck, Germany, the two companies will develop small-molecule protein degraders for 3 targets in the fields of oncology and immunology
.

Amphista could receive up to $1 billion in upfront and milestone payments in total
.

In the partnership with Bristol-Myers Squibb, which will collaborate on the discovery and development of small molecule protein degraders, Amphista received an upfront payment of $30 million and is eligible to receive a milestone payment of $1.
25 billion
.

Nicola Thompson, CEO of Amphista, said that the cooperation with two large pharmaceutical companies is a validation of the company's targeted protein degradation research and its next-generation technology platform
.

The company looks forward to working with the teams from Merck, Germany and Bristol-Myers Squibb
.

Reference: [1] Amphista Therapeutics Enters Strategic Collaboration with Merck for Discovery and Development of Targeted Protein Degradation Therapeutics.
Retrieved May 4, 2022, from https://amphista.
com/amphista-therapeutics-enters-strategic-collaboration-with- merck-for-discovery-and-development-of-targeted-protein-degradation-therapeutics/Disclaimer: The WuXi AppTec content team focuses on introducing global biomedical health research progress
.

This article is for information exchange purposes only, and the views expressed in this article do not represent WuXi AppTec's position, nor do they represent WuXi AppTec's support or opposition to the views expressed in this article
.

This article is also not a treatment plan recommendation
.

For guidance on treatment options, please visit a regular hospital
.