Rigosertib is primarily investigated for its potential in cancer treatment, particularly in targeting resistant and aggressive forms of malignancies. It functions as a mitotic inhibitor by disrupting the interaction between the Ras protein and its effector pathways, which are often dysregulated in cancer cells. This mechanism leads to cell cycle arrest and apoptosis in tumor cells. It has shown promise in clinical trials for myelodysplastic syndromes (MDS), especially in patients who are refractory to hypomethylating agents. Rigosertib’s ability to induce oxidative stress and interfere with microtubule formation enhances its anti-proliferative effects across various solid tumors and hematologic cancers. Due to its unique mode of action, rigosertib is also being explored in combination therapies with other anticancer agents to overcome drug resistance and improve treatment outcomes. Its development represents a strategy to target cancers with Ras pathway mutations, which are traditionally difficult to treat with conventional therapies.