October 15, 2020

SAN DIEGO - Cullgen Inc., a leading biotechnology company developing small molecule therapeutics based on its proprietary uSMITE™ platform of targeted protein degradation technology, today announced that the company’s internal program to develop selective degraders that target key proteins within the TRK family has been published by the Journal of Medicinal Chemistry. The paper, entitled “Discovery of First-in-class Potent and Selective Tropomyosin Receptor Kinase Degraders”, has been selected as a Featured Article by the editors of the journal based on the novelty and scientific merit of the work.

TRK fusion proteins have been found across a wide range of human malignancies, including lung cancer, colorectal cancer, and soft tissue sarcoma. In addition, TRK fusions appear to be the primary oncological drivers of some rare cancers, such as infantile fibrosarcoma, secretory breast carcinoma, and mammary analogue secretory carcinoma (MASC). The first-in-class degraders developed by Cullgen efficiently degrade mutated, disease causing forms of the TRK protein and subsequently inhibit cancer cell growth. Existing therapies to treat TRK fusions have elicited modest ontarget adverse effects, including dizziness and weight gain. In addition, acquired drug resistance has been reported in patients after treatment with approved TRK protein inhibitors. Hence, Cullgen’s TRK degraders could offer patients a new therapeutic approach to treat TRK-mediated cancer diseases with reduced drug resistance.

“We are honored that the Journal of Medicinal Chemistry has selected our publication as a Featured Article. Our tireless team has significantly advanced our TRK degrader program over the past year and we are now rapidly completing IND-enabling studies for our clinical candidate” stated Dr. Yue Xiong, co-founder and Chief Scientific Officer of Cullgen. “In addition to our TRK program, we are also advancing multiple additional cancer degrader programs through pre-clinical studies, as well as utilizing our uSMITE™ platform to discover novel E3 ligands which we are using to develop completely new classes of targeted protein degraders.”

Journal of Medicinal Chemistry is a peer-reviewed science and medical journal published by a division of the American Chemical Society (ACS). The journal publishes innovative studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action.

About Cullgen Inc.

Cullgen is a privately held biopharmaceutical company dedicated to the development of first-in-class new chemical entities (NCEs) for the treatment of diseases lacking effective therapeutic approaches. We are developing our proprietary technology platform, ubiquitin-mediated, small molecule-induced target elimination technology, (uSMITE™), based on recent advances in the science of protein degradation. Typically, drugs are designed to interact with the functional sites of proteins and block their activities. We are developing uSMITE™ to expand the drug design paradigm beyond functional site inhibition, to make it possible to eliminate previously “undruggable” enzymes and proteins by targeted destruction. We also intend to use the uSMITE™ technology to harness the ubiquitin proteasome system, a multi-step biochemical process that controls protein degradation in all cells. From years of research on the proteasome system and key discoveries about its assembly, Cullgen’s founders have already demonstrated that the underlying technology can rapidly generate a large number of highly potent, selective, and bioavailable compounds. Furthermore, this process is significantly more cost effective compared with traditional drug discovery approaches. For more information, visit www.cullgen.com.