Merck Enters Collaboration and Option to License Agreement with Nerviano Medical Sciences to Develop Next-Generation PARP1 Selective Inhibitor

Not intended for US-, Canada- or UK-based media

• NMS-293 is a next generation, orally available,      brain-penetrant PARP1 selective inhibitor

• NMS-293 is currently studied in Phase I as      monotherapy for the treatment of patients with BRCA-mutated tumors and in      combination with temozolomide in recurrent glioblastoma

• Next generation PARP1 selective inhibitors could      fill a significant unmet patient need across a wide range of tumors      including those not responsive to currently available PARP inhibitors and      those requiring combination with other agents

DARMSTADT, Germany -- (BUSINESS WIRE) --

Merck, a leading science and technology company, today announced a collaboration agreement with licensing option with Nerviano Medical Sciences S.r.l. (NMS) for the next-generation highly selective and brain-penetrant PARP1 (poly (ADP-ribose) polymerase) inhibitor, NMS-293. NMS-293 has strong potential in combination with a wide variety of DNA-damaging agents, including systemic or targeted chemotherapy (Antibody-Drug Conjugates) or with DNA damage response inhibitors, in numerous tumor types. NMS-293 is in early clinical development for the treatment of patients with BRCA-mutated tumors as a single agent and in combination with temozolomide in recurrent glioblastoma.

“Building on the therapeutic impact that PARP inhibitors have had over the last several years, we believe this new PARP1 program, if successful, could fill a significant unmet need for patients unresponsive to existing PARP inhibitors with an improved hematological adverse event profile,” said Victoria Zazulina, M.D., Head of Development Unit Oncology for the Healthcare business of Merck. “The work of NMS to discover and advance this next generation PARP1 selective inhibitor coupled with our deep expertise in developing therapies which modify DNA damage response mechanisms, creates a strong foundation to further develop this investigational therapy for patients.”

PARP is key in the repair of DNA damage, and PARP inhibitors have been shown to be highly efficacious in the treatment of patients with tumors deficient in homologous recombination repair, such as breast, ovarian, prostate and pancreatic cancers with BRCA-mutations.

Under the current agreement, Merck will make early payments (up-front and option exercise fees) of up to $65 million to NMS. Furthermore, NMS will receive payments for the achievement of certain development, regulatory and commercial milestones and tiered royalties on net sales by Merck. Upon exercise of the option, NMS will grant to Merck the exclusive rights to research, develop, manufacture, and commercialize NMS-293.

During the option period, NMS and Merck will collaborate on the clinical development of NMS-293, with NMS designing, sponsoring, conducting, and funding global clinical trials.

About NMS-293

NMS-293 is an orally available small molecule inhibitor of PARP1 and is currently in early clinical development for the treatment of patients with BRCA mutated tumors as single agent and with recurrent Glioblastoma (GBM), a brain tumor with very high medical need, in combination with temozolomide (TMZ).