Selinexor is bis(trifluoromethyl)phenyl-triazole-based antineoplastic small molecule (Figure 7). It was first approved in 2019 by the U.S. FDA and is being prescribed with dexamethasone for refractory or relapsed multiple myeloma. Selinexor is an orally bioavailable, selective inhibitor of chromosome region maintenance 1 (CRM1) protein (also known as exportin 1 (XPO1)). CRM1 is the main export factor that shuttles nuclear proteins to the cytoplasm and is typically overexpressed in cancer cells. Its selective inhibition can assist in restoring the endogenous tumor-suppressing processes so as to eliminate cancer cells. Specifically, selinexor selectively and irreversibly modifies the essential Cys528 residue in CRM1, and thus, it blocks CRM1-mediated nuclear export of cargo proteins such as tumor suppressor proteins (p21, p53, pRB, BRCA1/2, FOXO, and others) from the cell nucleus to the cytoplasm. This leads to the accumulation of tumor suppressor proteins in the nucleus. It also results in decreased levels of oncoproteins, cell cycle arrest, and apoptosis of cancer cells without affecting the normal cells [119,120,121].