GT Apeiron Announces Development Candidate Nomination of Brain Penetrant PRMT5 Inhibitor, GTA182, for the Potential Treatment of MTAP-Deleted Solid Cancers
- Potentially best-in-class MTA-cooperative PRMT5 inhibitor -
- Demonstrates efficacy in pre-clinical models of glioblastoma and non-CNS tumor models with MTAP deletion -
- Apeiron plans to file Investigational New Drug (IND) application for GT182 in mid-2024 -
SAN FRANCISCO & SHANGHAI, October 17, 2023 -- GT Apeiron Therapeutics (‘Apeiron’), a biopharmaceutical company harnessing the power of artificial intelligence to develop targeted precision therapies for unmet medical needs, today announced the development candidate nomination of GTA182, a brain penetrant protein arginine methyltransferase 5 (PRMT5) inhibitor that exhibits methylthioadenosine (MTA) cooperativity resulting in high selectivity for MTAP-deleted cancer cells while sparing MTAP-expressing non-cancer cells. This selectivity is expected to provide a more effective and safer treatment option for patients with MTAP-deleted cancers.
“GTA182’s high selectivity for MTAP deleted cancers and its ability to cross the blood brain barrier make it a best-in-class candidate for advancement into clinical development for the potential treatment of CNS tumors as well as non-CNS indications,” said Fred Aswad, J.D., Ph.D., Senior Vice President of Biology and Translational Science. “Approximately 10% of solid tumors harbor MTAP deletions, including glioblastoma, lung, pancreatic, and bladder cancers all of which have limited treatment options and represent a significant unmet need for patients.”
In preclinical studies, Apeiron has demonstrated that GTA182 is a potent and selective PRMT5 inhibitor exhibiting greater than 100-fold selectivity for MTAP deleted tumor cell lines. GTA182 is brain penetrant and has demonstrated tumor growth inhibition and tumor regression in in vivo pre-clinical models of glioblastoma (GBM) as well as non-CNS murine cancer models with MTAP deletions.
Apeiron plans to file an Investigational New Drug (IND) application in mid-2024.
"The nomination of our wholly–owned GTA182 program as a candidate for clinical development represents another significant milestone for Apeiron and our commitment to developing innovative therapies for cancer patients with unmet medical needs," said Mingxi Li, Ph.D., Chief Executive Officer of Apeiron.
About GT Apeiron
GT Apeiron is redefining medical discovery, using artificial intelligence to streamline the drug development process—from target selection to clinical trials. With strategic locations in the San Francisco Bay Area and Shanghai, and significant partnerships in Europe, Apeiron integrates talent and cutting-edge technologies spanning multiple regions. We believe that by pushing the frontiers of biomedical innovation and engaging talent globally we can create breakthrough medicines for the highest unmet medical needs.
For additional information about GTA182, visit www.apeiron-bio.com/gta182
For additional information about Apeiron, visit www.apeiron-bio.com
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