A Review of Small Molecules and Their Therapeutic Targets

Publication date: Available online 18 June 2018Source: Clinical Lymphoma Myeloma and LeukemiaAuthor(s): Hanley N. AbramsonAbstractTreatment of multiple myeloma (MM), a neoplasm of plasma cells, formerly dependent on alkylating drugs, corticosteroids, and autologous stem cell transplantation (ASCT), has changed dramatically in the past 20 years as three new classes of small molecule drugs (arbitrarily defined as having molecular weights of less than 900 kDa) - immunomodulators (IMiDs), proteasome inhibitors (PIs), and histone deacetylase (HDAC) blockers - have been introduced for the disease. Therapeutic options for MM expanded further in 2015 when two new monoclonal antibodies (daratumumab and elotuzumab) were approved by the FDA for MM. Although MM remains incurable, the cumulative effect of these advances has resulted in a near-doubling of the five-year survival rate since the late 1980’s. In spite of these advances, therapy of MM continues to pose substantial challenges as resistance to therapy frequently develops and relapse and recurrence are all too common. This review focuses on the pipeline for new small molecules in various stages of development, as well as on their associated cellular targets. In addition to newer versions of alkylators, IMiDs, PIs, and HDAC inhibitors, this review considers the prospects for adding new classes of small molecules to the MM armamentarium, which offer the potential for oral efficacy, relative simplicity of preparation, and prospects...
Source: Clinical Lymphoma Myeloma and Leukemia - Category: Cancer & Oncology Source Type: research