On February 23, 2021 Day One Biopharmaceuticals, a clinical-stage biopharmaceutical company focused on accelerating new, promising targeted therapies for children and adults with cancer, reported that it has entered into a global licensing agreement with Merck KGaA, Darmstadt, Germany, for an exclusive license to develop and commercialize pimasertib as well as a second compound, MSC2015103B (Press release, Day One, FEB 23, 2021, View Source [SID1234575482]). Pimasertib and MSC2015103B are oral, highly-selective small molecule allosteric inhibitors of MEK 1/2, a key enzyme in the MAPK signaling pathway. Dysregulation of the MAPK pathway has been shown to occur in many cancers.
Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:
Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing
Schedule Your 30 min Free Demo!
Pimasertib has been studied in more than 10 Phase 1/2 clinical trials in approximately 900 patients with various tumor types. Day One plans to initiate a Phase 1/2 study to evaluate the safety, tolerability, and preliminary efficacy of combining pimasertib with DAY101, the Company’s potential first-in-class, oral, brain-penetrant, highly selective type II pan-RAF kinase inhibitor, in patients ≥12 years of age with recurrent, progressive, or refractory solid tumors with MAPK pathway aberrations.
"Day One is purpose-built to accelerate innovative targeted therapies designed to help both children and adults with cancer," said Jeremy Bender, Ph.D., chief executive officer of Day One. "This license agreement with Merck KGaA, Darmstadt, Germany, exemplifies our core strategy to identify investigational potential treatment options such as pimasertib and leverage our expertise to rapidly advance them in patients who we believe will benefit the most. We are excited that a leading pharmaceutical company like Merck KGaA, Darmstadt, Germany recognizes the importance of our mission and look forward to the advancement of pimasertib in combination with our pan-RAF kinase inhibitor, DAY101."
"There is strong scientific and clinical rationale for targeting multiple nodes of the MAPK signaling pathway to drive deeper and more durable tumor responses," said Samuel Blackman, M.D., Ph.D., co-founder and chief medical officer of Day One. "DAY101 demonstrated encouraging single agent anti-tumor activity in pediatric low-grade glioma, and we believe the combination of pimasertib and DAY101 will be well-suited for adult patients with solid tumors given their greater heterogeneity. Further, data have shown DAY101 to selectively inhibit both RAF monomers and dimers which may broaden its potential clinical application in combination with MEK inhibition in solid tumors driven by non-BRAF V600 mutations and RAF fusions. We look forward to initiating a Phase 1/2 combination study later this year."
Under the terms of the agreement, Day One will make an upfront payment to Merck KGaA, Darmstadt, Germany plus additional regulatory, approval and sales-based milestone payments. Merck KGaA, Darmstadt, Germany will also receive royalties on potential net sales of pimasertib and MSC2015103B. Specific financial details are not disclosed.
About Pimasertib
Pimasertib is designed as a highly selective, oral, small molecule inhibitor of mitogen‐activated protein kinase kinases 1 and 2 (MEK1/2), of the MAPK signaling pathway. Dysregulation of the MAPK pathway has been shown to occur in many cancers. Pimasertib has been studied in more than 10 Phase 1/2 clinical trials in approximately 900 patients with various tumor types and has demonstrated a safety and efficacy profile comparable to other MEK inhibitors.