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Insilico Medicine expands synthetic lethality portfolio with the nomination of a preclinical candidate targeting MAT2A for the treatment of MTAP-deleted cancers

NEW YORK, May 6, 2022 /PRNewswire=KYODO JBN/ --

Insilico Medicine ("Insilico"), a clinical-stage end-to-end artificial

intelligence (AI)-driven drug discovery company, today announced that the

company has nominated a preclinical candidate (PCC) targeting methionine

adenosyltransferase 2A (MAT2A) from AI-designed molecules for the treatment of

methylthioadenosine phosphorylase (MTAP)-deleted cancers. The MAT2A program is

part of Insilico's growing portfolio of synthetic lethality assets in

development.

MTAP deletion is one of the most common gene deletions seen in cancers

including lung, bladder, and pancreatic cancers, and is associated with poor

prognosis. MAT2A is defined as a synthetic lethality target in MTAP-deleted

cancers and plays an essential role in producing S-adenosylmethionine (SAM), a

molecule involved in cell function and survival. Inhibitors of MAT2A lead to a

selective anti-proliferative effect on MTAP-deleted cancer cells by reducing

the level of SAM to affect PRMT5-Dependent mRNA splicing and inducing DNA

damage.

Insilico's PCC is a potent and selective MAT2A inhibitor. It demonstrated

excellent drug-likeness with good solubility and permeability, good efficacy at

low doses in animal models, and a favorable safety profile in preclinical

studies.

"Powered by AI, the MAT2A program team was able to discover the PCC molecule

with high selectivity of MTAP-deleted cancer cells over wide-type cells, which

we believe provides key differentiation compared to reported MAT2A inhibitors,"

said Feng Ren, Ph.D., Chief Scientific Officer of Insilico Medicine. "This is

the second PCC in our growing synthetic lethality pipeline, and we are

progressing the molecule in IND-enabling studies towards clinical trials for

the treatment of MATP-deleted cancers."

Insilico has built a strong portfolio of synthetic lethality assets supported

by scientists with deep drug discovery expertise and its AI-driven small

molecule design and generation engine, Chemistry42. The company announced its

first synthetic lethality preclinical candidate, which targets USP1 for tumors

with homologous recombination deficiency, in mid-April

(

https://en.prnasia.com/releases/apac/insilico-medicine-announces-advancement-of-its-preclinical-candidate-for-usp1-synthetic-lethality-target-to-ind-enabling-studies-for-various-oncological-disorders-357994.shtml

). Continuing this success, Insilico delivered the preclinical candidate for

the MAT2A program approximately 12 months after its initiation.

"This PCC continues the expansion of our synthetic lethality portfolio, driven

by our end-to-end AI drug discovery platform," said Insilico founder and CEO

Alex Zhavoronkov, PhD. "With this latest discovery, we continue to utilize the

power of AI to treat the most aggressive cancers with the highest unmet needs."

Insilico is developing a growing portfolio in frontier areas. Since February

2021, it has delivered 7 PCCs, including AI-discovered therapeutics of novel

targets with novel structures and AI-designed therapeutics of known targets

with desired properties. It also successfully completed a Phase 0 microdose

trial and entered a Phase I clinical trial

(

https://en.prnasia.com/releases/apac/insilico-announces-successful-completion-of-phase-0-microdose-trial-and-initiates-phase-i-clinical-trial-for-its-first-ai-discovered-anti-fibrotic-product-candidate-with-novel-target-352573.shtml

)for its lead fibrosis program, and is currently conducting a Phase I clinical

trial

(

https://en.prnasia.com/releases/apac/insilico-announces-successful-completion-of-phase-0-microdose-trial-and-initiates-phase-i-clinical-trial-for-its-first-ai-discovered-anti-fibrotic-product-candidate-with-novel-target-352573.shtml

)in healthy volunteers.

About Insilico Medicine

Insilico Medicine, a clinical stage end-to-end artificial intelligence

(AI)-driven drug discovery company, is connecting biology, chemistry, and

clinical trials analysis using next-generation AI systems. The company has

developed AI platforms that utilize deep generative models, reinforcement

learning, transformers, and other modern machine learning techniques to

discover novel targets and to design novel molecular structures with desired

properties. Insilico Medicine is delivering breakthrough solutions to discover

and develop innovative drugs for cancer, fibrosis, immunity, central nervous

system (CNS) diseases and aging-related diseases.

Source: Insilico Medicine