KRLS-017 / Ube Corp, Kirilys - LARVOL DELTA

Targeting CDK7 enhances the antitumor efficacy of enzalutamide in androgen receptor-positive triple-negative breast cancer by inhibiting c-MYC-mediated tumorigenesis. (PubMed, Mol Cancer Ther) - "An enhancement in inhibition of tumor growth and suppression of c-MYC expression was further confirmed when enzalutamide combined with KRLS-017 in an MDA-MB-453 mouse model. Our study suggests that KRLS-017 enhances the antitumor efficacy of enzalutamide by inhibiting c-MYC-mediated tumorigenesis and presents a potential new approach for treating AR+ LAR TNBC."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • AR • CDK7 • MYC

Preclinical evaluation of KRLS-017, a potent, highly selective and reversible CDK7 inhibitor with broad antitumor effect in preclinical models, in preparation for a Phase 1 clinical trial in advanced solid tumor malignancies (AACR 2024) - "Repeat dose 28 day GLP toxicology studies in rat and dog showed adverse effects in highly proliferative bone marrow and gastrointestinal tissues which is consistent with the known mechanism of action for CDK7 and is considered to be monitorable and manageable in the setting of oncology.The clinical development plan for KRLS-017 includes an initial Phase 1 dose escalation study (KRLS-017-101) in patients with refractory solid tumor malignancies to assess pharmacokinetics / pharmacodynamics and to determine an optimal dose level and treatment schedule to test in expansion cohorts. Given the potential of CDK7 inhibitors in the treatment of hormone receptor positive breast cancer, combination work with other agents (such as selective estrogen receptor degraders) is on-going."

Metastases • P1 data • Preclinical • Breast Cancer • Hematological Malignancies • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER

Targeting CDK7 enhances the antitumor efficacy of enzalutamide in androgen receptor-positive triple-negative breast cancer (SABCS 2022) - "Our results suggest that enzalutamide synergizes with UD-017 by inhibiting c- MYC–mediated oncogenic activity. These in vitro data warrant future in vivo studies of the antitumor synergy of enzalutamide plus UD-017 in AR+ LAR TNBC models."

Clinical • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • AR • CDK7 • MYC

Catalys Pacific Launches Kirilys Therapeutics as a Multi-asset Precision Oncology Company (Businesswire) - "Kirilys Therapeutics, Inc...announced...that the Company completed a seed financing led by Lightspeed Venture Partners. The company licensed its lead compound, KRLS-017, from Ube Industries, Ltd., a premier Japanese chemical manufacturer. The company also completed a partnership agreement with D2G Oncology, Inc. which uses genetically defined animal tumor models to reveal relationships between cancer genotypes and drug efficacy. This financing round will enable Kirilys to complete all activities through the IND filing of KRLS-017, as well as preparatory work for the Phase 1 clinical development program."

Financing • Licensing / partnership • Hematological Malignancies • Oncology • Solid Tumor