• Marcel Frenkel

Looking Back at 2021, and Forward to 2022

Updated: 3 days ago

Dear Ten63 Family and Friends, 2021 was a challenging year for all of us. We hope this message finds you and your loved ones safe and well. Despite the challenges of the pandemic, 2021 has been an extremely fruitful year for us at Ten63. Thank you for being with us on this journey to build the future of drug discovery and to cure what are today incurable diseases. It's still early days, but we have built something special. We are excited to share with you this year's incredible achievements and our future plans.

This year, we welcomed some amazing talent: Mason Yost, Dr. Kiran Kanekal, and Dr. Swati Jain. Their contributions have allowed us to build key aspects of our platform such as improved water modelling, pipeline automation, enhanced AI based scoring of drug-likeness, modeling of chemical synthesis, and improvements to our designs and flexibility models. A current review of our team will find that we have brought together the key people required to make our company a success: experienced pharma executives, battle tested early drug discovery experts and innovative and cutting edge pioneers in computer science and AI, all working together to create a new path in therapeutic discovery. I am very proud of the team that we have built, and 2021 saw us achieve some important milestones.

2021 was a big year for the AI drug discovery industry. Both Exscientia and Insilico Medicines brought, for the first time, AI designed drugs to clinical trials. Undoubtedly, this is a watershed moment for the industry. Although these were significant victories, what they demonstrated is that AI can help advance and accelerate molecules against known target families. At Ten63 we are focused on answering a different question: what can AI do to advance the discovery of drugs against previously undruggable targets (>80% of the human genome)? To that end, we chose to validate on c-Myc, an infamously hard target with clear and established medical importance. c-Myc was first discovered in 1979, and by the mid 80s, its importance in cancer had been made clear. Over the next 40 years, over 20k publications have been written about its role as a master regulator of cancer biology. Needless to say, multiple pharma and academic groups have attempted to design Myc inhibitors; over 5M molecules have been screened in an attempt to design an effective inhibitor. It was against this classically undruggable target that we have been able to show our greatest success.

Using BEYOND, our proprietary computational platform, we have designed and experimentally validated a potent Myc inhibitor. When we compared our Myc inhibitor to a set of top literature compounds, we found that our compound was 10x more potent. Moreover, we were very excited to find that these molecules were drug-like and truly novel and could not have been easily found by any other method. A SciFinder search (which searches patents in 27 countries and approximately 8000 journals and publications) showed that our molecules were not only in no way related to previously reported Myc inhibitors, but also not related to any other molecule ever reported. We are finding solutions in totally new chemical space that only we have been able to search.

These initial designs represent just the beginning of what BEYOND can achieve. In the next few years, we expect BEYOND to allow us to drug the ideal pocket for each medical indication within a target. This will result in best-in-class novel therapeutics not only for previously undruggable targets, but also for known targets that may currently be plagued by resistance mutations, toxicity due to lack of specificity, or both.

As we look at the AI drug discovery ecosystem today, we are seeing a clear path for Ten63 to establish a beachhead for the therapeutic development of best and first-in-class drugs. We believe our validation clearly points towards our differentiation, and what we have achieved during 2021 showed that our platform can out-compete other methods, both computational and experimental, on the hardest targets.

In 2022, Ten63 is focused on raising our Series A, with the objective of developing our internal pipeline of drug discovery targets into the clinic and continuing to advance BEYOND. Our pipeline selection currently focuses on highly validated, previously undruggable targets. However, as we grow our pipeline, we will pick targets based on our ability to predict cellular susceptibility in a disease evolution-aware model. Our objective is to look at disease from a 4D perspective, understand how disease will evolve during treatment and design our pipeline and therapeutics to overcome resistance mechanisms in order to change the paradigm of treatment for currently incurable diseases.

We believe that our ability to unlock the undruggable genome, combined with our unique ability to select targets and design drugs in a 4D-aware fashion, will make Ten63 the future in developing cutting edge therapeutics.

Thank you for your support and interest. Happy Holidays, and we look forward to an even more fruitful 2022!

Marcel Frenkel, PhD

CEO at Ten63 Therapeutics

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