LOMOND THERAPEUTICS REPORTS RESULTS FROM ONGOING CLINICAL STUDIES OF LONITOCLAX, A SELECTIVE BCL-2 INHIBITOR WITH BEST-IN-CLASS SELECTIVITY VERSUS BCL-XL AND NO CYP 3A4 LIABILITY

DOVER, Del., Dec. 9, 2024 /PRNewswire/ -- Lomond Therapeutics, a spin-out of Eilean Therapeutics LLC, a precision oncology-focused discovery and development platform, today announced results from single ascending dose Phase 1 clinical studies of oral once-daily lonitoclax. In this series of healthy volunteer studies, no significant safety signals were observed at exposures where robust inhibition of BCL-2 was achieved, as measured via ex vivo activation of caspase in CLL primary cells. Furthermore, administration of itraconazole, a strong inhibitor of cytochrome P450 3A4 metabolism, did not significantly alter lonitoclax exposures. These results emphasize important advantages over venetoclax and venetoclax-like molecules in safety, tolerability, and feasibility of outpatient treatment, enabling lonitoclax to be used to safely treat CLL and AML patients.

"The positive PK, PD, and safety findings from our Phase 1 trial mark the first clinical data that underscores the differentiated profile and promising potential of lonitoclax compared to venetoclax and venetoclax-like molecules for AML, CLL, and potentially other oncology indications patients," said Dr. Iain Dukes, Chief Executive Officer of Lomond Therapeutics. "We are excited to embark on the next phase of development for lonitoclax with an ongoing CLL study."

About Lonitoclax
Lonitoclax is a next generation BCL-2 inhibitor that has demonstrated best-in-class molecular pharmacology with the highest selectivity against BCL2, a key pro-survival protein that is overexpressed in many cancers. To mitigate the hematologic and immune toxicities observed with venetoclax, lonitoclax was designed with a unique binding mode to improve selectivity for Bcl-2 over Bcl-xL. In addition, a shorter half-life and reduced P4503A4 inhibition properties were built into the molecule to mitigate tumor lysis syndrome and drug accumulation risk, respectively. Lonitoclax has demonstrated monotherapy activity in pre-clinical models, as well as synergistic activity when combined with azacitidine, FLT3 inhibitors, and menin inhibitors in AML xenograft models. Unlike venetoclax, lonitoclax had minimal immunosuppressive activity on B cells, CD8 T cells, and NK cells in preclinical models. 

About Lomond Therapeutics
Lomond Therapeutics is a biopharmaceutical company, focused on the development of best-in-class and first-in-class small molecule inhibitors that target escape mutations in hematologic and solid cancers.  The pre-clinical work with this molecule was done in collaboration with the Leukemia Drug Development Laboratory at the University of Cincinnati led by Dr. John Byrd and Dr. Erin Hertlein. The company is utilizing a proprietary hybrid AI platform of the Expert Systems Accelerator, leveraging its key partners' proprietary data, chem-bio platforms, knowledge and expertise to choose highly valuable molecular mechanisms of pathology to precisely design and accelerate the execution of discovery and development of best-in-class and first-in-class therapies. Lomond Therapeutics' goal is to utilize its capabilities and platform to become a leader in developing novel breakthrough medicines to treat hematologic and solid malignancies. For more information visit www.lomondther.com

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SOURCE Lomond Therapeutics