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Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Lenalidomide: the emerging role of a novel targeted agent in malignancies
Sujith Kalmadi1, Rachid Baz, Anuj Mahindra
1Taussig Cancer Center, Cleveland Clinic, Cleveland, Ohio 44195, USA. kalmads@ccf.org
Abstract:
Lenalidomide is an immunomodulatory drug that was developed by modification of the first-generation immunomodulatory drug thalidomide in a drug discovery program. Lenalidomide more potently regulates cellular immune and cytokine responses, while lacking the side-effect profile of thalidomide. The promising activity seen in multiple myeloma and myelodysplastic syndrome has led to its approval by the U.S. Food and Drug Administration in these conditions. The clinical results that we have seen so far, which demonstrate significant efficacy with a tolerable toxicity profile, provide a strong basis for the use of lenalidomide in other malignancies. Combination therapy with lenalidomide could enhance this agent's antineoplastic role; this is likely the position it will occupy in the armamentarium against cancer.
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