ACE inhibitor (Servier)

ROCKVILLE, Md., March 13, 2024 /PRNewswire/ -- Expert Systems, a leader in AI-enabled drug discovery, proudly announces a significant milestone in partnership with Eilean Therapeutics LLC: the start of Phase 1 trial of balamenib (ZE63-0302), a highly selective inhibitor of the menin–KMT2A binding interaction, under the Clinical Trial Notification (CTN) scheme of the Australian Therapeutics Goods Administration (TGA). "Balamenib has a highly differentiated pre-clinical pro indicates important advantages over molecules in the same class in safety, tolerability and feasibility of outpatient treatment," commented Bill Farley, CBO at Expert Systems. "We are proud that our comprehensive hybrid AI-based platform has helped accelerate the development of a new promising & safe treatment for AML." Supported by Orbimed, Torrey Pines Investment, and Dr. John C. Byrd, Eilean Therapeutics is committed to leading the development of innovative therapies that significantly enhance treatment outcomes in both hematologic and solid malignancies. This effort is bolstered by leveraging Expert Systems' cutting-edge AI platform to speed up the discovery and development process. About Balamenib Balamenib (ZE63-0302) is an oral small molecule inhibitor of the menin-KMT2A interaction. In vitro studies with KMT2Ar specific cell lines and in vivo studies using xenograft models demonstrated that balamenib is a potent menin inhibitor when administered both as a stand-alone agent or in combination with other compounds used for the treatment of r/rAML, in particular with eiletoclax (ZE50-0134), and lomonitinib (ZE46-0134), Eilean Therapeutics' BCL-2 selective inhibitor and pan FLT3/IRAK4 inhibitor, respectively. Balamenib demonstrates improved safety compared to other molecules in the same class, with an absence of QTc prolongation and is neither a substrate nor inducer of cytochrome P450 3A4 metabolism. Furthermore, balamenib shows significantly reduced susceptibility to "hot spot" menin mutations currently being encountered in the clinic with other menin inhibitors. About Expert Systems, Inc. Expert Systems, Inc., an advanced accelerator platform, is equipped with a comprehensive, hybrid AI-based system that covers the entire spectrum of preclinical drug discovery and early development phases. This includes target identification, virtual screening, non-clinical and clinical pharmacology, chemical liability assessment, and toxicology. Utilizing a unique combination of proprietary and public databases, Expert Systems employs specialized software tools to evaluate the intellectual property landscape and construct a competitive drug intelligence strategy to de-risk candidate selection for rapid transition from in silico to first-in-human trials. Expert Systems has been pivotal in establishing seed and Series A companies, organizing and managing over 30 research and development programs across various financial investors and strategic partners in North America, Europe, and Australia. To learn more, visit About Eilean Therapeutics Eilean Therapeutics LLC is a cutting-edge biopharmaceutical company, established through a collaboration between Orbimed, Torrey Pines Investment, and Dr. John C. Byrd, dedicated to the identification of both best-in-class and first-in-class small molecule inhibitors targeting escape mutations in both hematologic and solid cancers. The company harnesses the Expert Systems Inc. hybrid AI platform alongside its key partners' exclusive data, chem-bio platforms, knowledge, and expertise. This enables Eilean Therapeutics to select molecular mechanisms of pathology with high clinical relevance, precisely designing and expediting the discovery and development processes for leading-edge therapies. Eilean Therapeutics is committed to leveraging its unique capabilities and platform to create novel, groundbreaking medicines for patients with hematologic and solid malignancies, marking a new era in targeted cancer therapy. For more information, visit Bill Farley CBO bfarley@expertsystems.inc

The National Institute for Health and Care Excellence (NICE) has recommended STADA and Calliditas Therapeutics’ targeted-release Kinpeygo (budesonide) to treat a subset of patients with IgA nephropathy (IgAN), a rare kidney disease. Affecting approximately 14,000 people in England, IgAN occurs when IgA accumulates in the kidneys, causing inflammation and scarring, which can lead to kidney failure. Patients can experience a broad range of symptoms, including bone and joint pain, fatigue and muscle weakness, and as the condition progresses, chronic kidney disease and associated infections can lead to hospitalisation. Kinpeygo has been specifically recommended for use on the NHS in England and Wales as an option for treating primary IgAN when there is a risk of rapid disease progression in adults with a urine protein-to-creatinine ratio of 1.5g/g or more. NICE also outlined that the drug must be used as an add-on to optimised standard care, including the highest tolerated licensed dose of angiotensin-converting enzyme (ACE) inhibitors or angiotensin-receptor blockers (ARBs), unless these are contraindicated. STADA, which holds the commercial rights for the drug in the UK, European Economic Area member states and Switzerland, said it intends to supply and make the drug available to patients in the UK in spring 2024. The submission was supported by positive results from the NeflgArd randomised, double-blind trial comparing targeted-release Kinpeygo plus standard care, including maximally tolerated RASi therapy with an ACE-inhibitor or ARB, to standard care plus placebo. In its guidance, NICE outlined that the clinical trial evidence suggests that targeted-release Kinpeygo plus standard care is more effective than standard care alone, noting that "targeted-release [Kinpeygo] showed benefit on urine protein-to-creatinine ratio and estimated glomerular filtration". The agency added that, as Kinpeygo is now the first licensed treatment that specifically treats IgAN, it increases "the likelihood that people may avoid or delay the need for dialysis or a kidney transplant". Paul Burden, vice president of STADA UK, said: “Supported by this positive NICE appraisal, we look forward to bringing the UK’s first approved treatment to patients with primary IgAN, a progressive, rare kidney disease, within the next few months.”