Introduction Rigosertib (ON01910.Na), is a targeted therapeutic that inhibits multiple kinases, including PI3K and Plk1. Rigosertib has been found to induce the proliferative arrest and apoptosis of myeloblasts but not of other normal hematopoietic cells. Rigosertib has significant clinical activity as a therapy for patients with high-risk myelodysplastic syndrome (MDS) who are otherwise refractory to DNA methyltransferase (DNMT) inhibitors. Moreover, rigosertib has potential clinical activity in a multitude of solid tumors. Areas covered The objective of this review is to evaluate the mechanism of activity, efficacy and dosing of rigosertib. Furthermore, we discuss the challenge in the clinical development of rigosertib, to identify the specific patients that are most likely to benefit from this therapeutic agent. A PubMed search was performed using the following key words: rigosertib and ON01910.Na. Expert opinion We describe the application of a novel nanoscale proteomic assay, the nanoimmunoassay (NIA), a tractable approach for measuring the activity and predicting the efficacy of rigosertib, in real-time, using limited human clinical specimens. Our strategy suggests a possible paradigm where proteomic analysis during the pre-clinical and clinical development of a therapy can be used to uncover biomarkers for the analysis and prediction of efficacy in human patients.

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