Insilico Medicine expands synthetic lethality portfolio with the nomination of a preclinical candidate targeting MAT2A for the treatment
PR95790
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
(
). 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
(
)for its lead fibrosis program, and is currently conducting a Phase I clinical
trial
(
)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
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