Insilico Medicine names preclinical candida

Insilico Medicine (“Insilico”), a clinical-stage, end-to-end, artificial intelligence (AI)-driven drug discovery company, today announced that the company’s drug discovery team has nominated a preclinical candidate targeting KAT6A for ER+/HER2- breast cancer therapies using its end-to-end Pharma.AI platform. The company has now nominated eight preclinical candidates for 2022.

According to statistics published by the International Agency for Research on Cancer (IARC), breast cancer surpassed lung cancer as the most commonly diagnosed cancer and the fifth cause of cancer death worldwide in 2020. ER+/HER2 breast cancer is the most common subtype, and endocrine therapy in combination with CDK4/6 inhibitors is the standard treatment for this population with advanced or metastatic disease. However, the overall reported response rate is less than 50%, indicating a large unmet medical need.

“KAT6A is emerging as an attractive epigenetic target for ER+/HER2- breast cancer, and we are committed to rapidly advancing PCC toward a clinical trial to evaluate its efficacy in the clinic,” said Feng Ren, Ph.D., Co-CEO and Chief Scientific Officer of Insilico Medicine.

KAT6A is a histone (lysine) acetyltransferase (HAT), which plays an important role in cell cycle progression, neural stem cell maintenance, and hematopoietic development. In breast cancer, KAT6A is amplified as part of the 8p11 amplicon in about 10-15% of the population and modulates the level of estrogen receptor (ER) expression. Therefore, targeting the KAT6A oncogene is expected to bring promising therapy for ER+/HER2- breast cancer patients.

The preclinical compound is a selective KAT6A inhibitor generated using Insilico’s AI drug design platform, Chemistry42. It shows strong in vitro inhibitory activity and in vivo efficacy in ER+/HER2- breast cancer models and demonstrated significant efficacy in tumor models derived from patients who had relapsed on multiple prior lines of therapy. There are also favorable ones in vitro ADME properties i in vivo pharmacokinetic profile. Insilico has launched an Investigational New Drug (IND) enabling study of the compound to advance this internally developed program to the clinical stage.

“The nomination of a preclinical candidate targeting KAT6A strengthens our growing oncology pipeline, further validating the strength of our proprietary AI platform,” said Dr. Alex Zhavoronkov, founder and CEO of Insilico Medicine. “We are very happy to see how the Chemistry42 next-generation AI platform, which we are providing to our partners, is accelerating our own drug discovery efforts.”

Powered by its end-to-end Pharma.AI platform, Insilico has delivered eight preclinical AI-discovered therapy candidates a new goal with a new structure and AI-designed therapeutics of known targets with desired properties in the last 12 months, covering multiple disease areas, including immuno-oncology, inflammation and COVID-19. It also entered Phase I clinical trials with its first internally developed fibrosis program in New Zealand and China.

About Insilico Medicine

Insilico Medicine, an end-to-end artificial intelligence (AI)-based clinical-stage drug discovery company, connects biology, chemistry and clinical trial analysis using next-generation AI systems. The company has developed AI platforms that use deep generative models, reinforcement learning, transformers and other modern machine learning techniques to discover new targets and generate new molecular structures with desired properties. Insilico Medicine develops revolutionary solutions for the discovery and development of innovative medicines for cancer, fibrosis, immunity, central nervous system diseases, infectious diseases, autoimmune diseases and diseases related to aging.


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