NXP900 is a SRC/YES1 Kinase Inhibitor with a Novel and Differentiated Mechanism of Action.

FORT LEE, NJ, USA I September 14, 2021 I Nuvectis Pharma, Inc., a biopharmaceutical company focused on the development of innovative precision medicines for the treatment of serious conditions of unmet medical need in oncology, announced today that it has licensed exclusive worldwide rights to develop and commercialize a novel, oral, small molecule, SRC/YES1 inhibitor from the University of Edinburgh in Scotland. The compound, which has been designated NXP900, was discovered at the Cancer Research UK Edinburgh Centre of the University of Edinburgh’s Institute of Genetics and Cancer and is expected to commence IND-enabling studies in 4Q2021.

The pro-oncogenic effects of SRC kinase-mediated signaling in various solid tumor types, including breast, colon, prostate, pancreatic and ovarian cancers are well documented. In addition, amplification of the YES1 gene has also been reported in various solid tumors, including lung, head and neck, esophageal and sarcoma, and has also been described as a mechanism of acquired resistance to treatment with EGFR inhibitors that develops in a substantial percentage of patients with EGFR-mutated lung adenocarcinomas.

NXP900 has a unique mechanism of action in that it inhibits both the catalytic and scaffolding functions of the SRC kinase, thereby providing a complete shutdown of the signaling pathway, in contrast to the currently approved and in-development multi-kinase inhibitors that target SRC but only inhibit its catalytic function. We believe that another key differentiating factor is that NXP900 does not inhibit the ABL kinase, with in vivo data indicating no treatment-related immunosuppression, a potential advantage in the setting of solid tumors. In vitro, NXP900 inhibited the activity of SRC and YES1 kinases at sub-nanomolar concentrations. In vivo, treatment with NXP900 inhibited primary and metastatic tumor growth in xenograft models of breast cancer and demonstrated on-target pharmacodynamic effects. Data supporting NXP900’s unique mechanism of action has been recently published in the journal Cancer Research (“A novel mode of inhibiting SRC improves drug efficacy and tolerability”, 10.1158/0008-5472.CAN-21-0613). Taken together, we believe that NXP900 has the potential to become the first SRC/YES1 inhibitor for treatment of solid tumors.

Neil Carragher, Professor of Drug Discovery and Director of Translation, University of Edinburgh, said: “We believe that NXP900’s selectivity and demonstrated potency in several animal models of cancers potentially provide a broad range of development options, both as single agent and in combination with approved drugs. We are excited to be working with Nuvectis to rapidly move NXP900 into the IND-enabling studies with the hope of commencing clinical trials for NXP900 shortly thereafter.”

Asier Unciti-Broceta, Professor of Medicinal Chemistry and Head of the Innovative Therapeutics Lab, University of Edinburgh, said: “We are delighted to have partnered NXP900 with Nuvectis upon completion of the discovery program at the Institute of Genetics and Cancer. We are confident that Nuvectis’ skills and expertise in drug development bode well for the successful and rapid development of NXP900 and ultimately hope it becomes a much-needed new option that benefits patients with SRC/YES1 driven cancers.”

“We are thrilled to partner with the Institute of Genetics and Cancer at the University of Edinburgh to advance the development of NXP900, which has demonstrated outstanding preclinical activity to date. We also thank Edinburgh Innovations, the commercialization service of the university, for facilitating this licensing,” said Ron Bentsur, Co-Founder, Chairman and Chief Executive Officer of Nuvectis, who added, “We believe that with our two pipeline products, we are now one step closer to creating a diversified precision-medicine oncology-focused company with the goal of helping more people in their fight against hard-to-treat cancers.”

About Nuvectis Pharma

Nuvectis Pharma, Inc. is a biopharmaceutical company focused on the development of innovative precision medicines for serious conditions of unmet medical need in oncology. Nuvectis was founded in 2020 and is led by a team of industry veterans with broad and extensive drug development experience, and a proven track record of clinical and regulatory success. Nuvectis recently announced the completion of a $15 million Series A Preferred Stock financing with institutional and private investors, along with the in-licensing of exclusive worldwide rights to NXP800, an oral small molecule inhibitor of the HSF1 pathway from the Institute of Cancer Research (ICR). A Phase 1 trial of NXP800 in patients with advanced solid tumors is set to begin in 4Q2021. Nuvectis is also developing NXP900, a SRC/YES1 inhibitor, which is expected to begin IND-enabling studies in 4Q2021.

For more information, please visit www.nuvectis.com.

About the University of Edinburgh

The University of Edinburgh is consistently ranked in the world top 50 universities and is placed 16th in the 2022 QS World University Rankings. Through its cutting-edge research, expertise, facilities and technologies the University of Edinburgh works closely with industry, the business community and government partners to develop innovative ideas into products, processes and services that positively impact society and the economy at national and global levels.

For more information visit www.ed.ac.uk.

About Edinburgh Innovations

Edinburgh Innovations is the University of Edinburgh’s commercialization service. EI leads the University’s activities in industry engagement and business development, enterprise support for students and staff, and the identification, management and commercialization of university intellectual property. https://edinburgh-innovations.ed.ac.uk.

SOURCE: Nuvectis Pharma