Eisai to Present E7386, co-created by PRISM BioLab and Eisai, at the ESMO (European Society for Medical Oncology) Annual Meeting

Abstract Released for E7386, Created Through Collaborative Research Between Eisai and PRISM

TOKYO, Sept. 8, 2024 /PRNewswire/ -- PRISM BioLab, Co. Ltd. ("PRISM"), a leading discovery and development biotechnology company designing small molecule inhibitors of protein-protein interaction (PPI) targets, today announced that the interim analysis of a combination study of E7386(*1), created through collaboration research with Eisai Co., Ltd. ("Eisai"), and Lenvatinib mesylate ( "lenvatinib") (*2) will be presented by Eisai at the European Society for Medical Oncology (ESMO) Congress 2024, held in Barcelona, Spain from September 13 to 17, 2024. The abstract of the study has been released today.

To determine the recommended dose of E7386 in combination with Lenvatinib in the open-label Phase Ib study(NCT0400879(*3)), expansion cohort of advanced endometrial cancer patients progressed following platinum-based chemotherapy and anti-PD-(L)1 immunotherapy have been implemented by Eisai. By data cutoff (Mar 7, 2024) in 16 patients,  31% (5 patients) showed the confirmed partial response (decrease of tumor size > 30%),  and 31% (5 patients) showed the stable disease (tumor size -30% to +20%).

These results confirmed promising preliminary antitumor activity of E7386 + Lenvatinib with a manageable safety profile. To complete the study, enrollment to the expansion part is ongoing.

(*1) E7386

E7386 is an orally available small molecule CBP/ β-catenin inhibitor that inhibits protein-protein interactions between the transcription factor CBP and β-catenin, and regulates the Wnt signaling. E7386 achieved clinical POC (Proof of concept) in October 2021 and following clinical studies are ongoing including phase I for solid tumors as monotherapy, Phase Ib for solid tumors in combination with tyrosine kinase inhibitor Lenvatinib, Phase Ib/II for solid tumors in combination with pembrolizumab, the anti-PD-1 antibody from Merck & Co., Inc., Rahway, NJ, USA.

(*2) Lenvatinib

Lenvatinib is a multi-kinase inhibitor, discovered by Eisai and being co-developed and co-commercialized under a collaboration agreement with Merck & Co., Inc., Rahway, NJ, USA, which inhibits vascular endothelial growth factor receptors (VEGFRs),VEGFR1, VEGR2, VEGFR3 and fibroblast growth factor receptors (FGFRs), FGFR1, FGFR2, FGFR3, FGFR4, and other receptor tyrosine kinases, PDGFR-alpha, KIT, RET. Lenvatinib have been approved for thyroid cancer, hepatocellular carcinoma, thymic caner and renal cell carcinoma (in combination with Everolimus or pembrolizumab, the anti-PD-1 antibody from Merck & Co., Inc., Rahway, NJ, USA.). Lenvatinib is also approved for endometrium cancer in combination with pembrolizumab

(*3) NCT04008797

NCT04008797 is an open-label Phase Ib study of E7386 in combination with other anticancer drug, Lenvatinib for the patients with solid tumors. The study has been implemented by Eisai in Japan, Korea, Taiwan, US, and France determine the safety and the recommended phase 2 dose (RP2D) and also to see the pharmacokinetics and efficacy of E7386 + Lenvatinib. Enrolment of each cohort of hepatic, colon, endometrial cancers are ongoing.

About PRISM BioLab

PRISM BioLab is a discovery and development biotechnology company utilizing proprietary PepMetics® technology to discover orally available small molecule inhibitors of protein-protein interaction (PPI) targets and transform lives of patients suffering from cancer, autoimmune, fibrosis and other diseases. PepMetics® are a unique class of small molecules that mimic three-dimensional structures of alpha-helix and beta-turn, the peptide structures commonly found in intracellular PPI interphases and receptor-ligand interactions. By combining proprietary chemistry, know-how around PPI targets and AI-supported design, PepMetics® technology can deliver inhibitors of challenging PPI targets. The technology holds promise to expand the field of drug discovery by turning previously undruggable PPIs into targets readily druggable with small molecules and by generating oral small molecule alternatives for injectable biologics.

PRISM BioLab is collaborating on new PPI targets with global and Japanese pharmaceutical companies. PepMetics® targeting CBP/beta-catenin PPIs licensed to Eisai Co., Ltd.  and Ohara Pharmaceuticals Co., Ltd. are in clinical development for cancer and liver disease, respectively.

www.prismbiolab.com

SOURCE PRISM BioLab Co., Ltd.