Nerviano, 13 May 2022
MPS1, also known as monopolar spindle 1, is a protein kinase which is over-expressed and hyperactivated in different tumors and which plays a critical role in the control of mitosis (cell division) by regulating a process called the Spindle Assembly Checkpoint. NMS Srl started the MPS1 inhibitor program, which resulted in the identification of the innovative and proprietary clinical candidate NMS-01940153E, a molecule with potential for being a first-in-class drug against this target.
NMS-01940153E is a potent and selective inhibitor of MPS1, possessing potent antiproliferative activity against cell lines derived from different tumor types, including breast cancer, colon carcinoma and hepatocellular carcinoma, with a distinct activity profile and different mechanism of action when compared to other mitotic inhibitors currently approved or in the clinic. Tumor growth inhibition observed in preclinical models, associated with a favorable pharmacokinetic and toxicological profile confirmed the selection of NMS-01940153E as a promising Product Candidate for clinical development.
The publication by Schöffski et al reports the results of the FIH study where thirty-eight patients were treated with NMS-01940153E by intravenous administration once a week, for 3 consecutive weeks in repeated 28-day cycles to explore safety, pK and early signs of efficacy.
Based on the positive findings of this first study, NMS is currently developing NMS-01940153E in a phase I/II clinical trial in the setting of hepatocellular carcinoma (HCC). Lisa Mahnke, CMO Consultant of NMS stated: “NMS is pleased to continue development of NMS-01940153E in a relevant dosing range in hepatocellular carcinoma for patients with high unmet medical need.” This trial (EUDRACT 2020-001002-26) is currently being conducted by NMS at centers of excellence for HCC both in Italy and in Spain.
20220513-NMS Srl MPS1 FIH Study Published-Final