We are exploiting our core Discovery engine to constantly develop new molecular entities with potential for “first in class “ and “best in class”. Our projects target a broad number of solid tumors and haematological indications, with a focus on biomarker selected patient populations. We are developing projects in house into clinical development in order to accelerate the clinical benefit for our patients.
FLT3, CSF1R and KIT play an important role in Acute Myeloid Leukemia (AML). FLT3 is mutated (FLT3+) in ~ 30% of AML and a validated target in AML, where FLT3 inhibitors have been approved for first and second line treatment. However the medical need is still high and the emergence of secondary drug resistance FLT3 mutations creates the need for novel drugs active on these mutations.
NMS-088 is a potent and selective FLT3 inhibitor with strong activity on the F691L resistance mutation to gilteritinib and other FLT3 inhibitors. Based on its activity on CSF1R inhibition it also has potential for treatment of CMML, where this receptor is highly expressed.
MKIA-088-001, a Phase I/II study of NMS-088 as single agent, is ongoing in relapsed/refractory AML and CMML (ClinicalTrials.gov Identifier: NCT03922100).
PARP is an enzyme implicated in the regulation of DNA repair. PARP inhibition has already been proven a successful therapeutic strategy for treatment of patients carrying deleterious germline and/or somatic BRCA mutations, present in a relevant percentage of breast, ovarian, prostate and pancreatic cancers.
NMS-293 is a potent and selective inhibitor of PARP-1 with unique features compared with other PARP inhibitors, such as its selectivity for PARP-1 vs. PARP-2 and lack of DNA trapping effects, which may result in higher tolerability in terms of undesired hematopoietic effects. Due to its high brain penetration it has potential for efficacy against primary brain tumors and CNS metastases.
PARPA-293-001, a Phase I study of NMS-293 as single agent, is ongoing in solid tumors enriched for BRCA mutant tumors
(ClinicalTrials.gov Identifier: NCT04182516).
Primary liver cancer is the sixth most common neoplasm and among the leading cause of cancer-related death worldwide. Hepatocellular carcinoma (HCC) constitutes 80-90% of all primary liver cancers. Its incidence is increasing and will soon surpass one million annual cases worldwide. Most HCC cases are diagnosed at advanced stages where, despite the recent approval of TKIs as well as checkpoint inhibitors, there is a high unmet medical need.
NMS-153 is a highly potent and selective inhibitor of the MPS1 kinase, which is a mitotic regulator frequently overexpressed and activated in cancer, with broad preclinical activity in different tumor settings, including HCC.
MPSA-153-001 is a Phase I/II study of NMS-153 as single agent in HCC open for recruitment.