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Next-generation relatives of lenalidomide that make the cell's disposal machinery destroy the myeloma proteins Ikaros and Aiolos more completely, working after older drugs fail.
Thalidomide, lenalidomide and pomalidomide act by binding cereblon and redirecting it to degrade Ikaros and Aiolos. Cereblon E3 ligase modulators (iberdomide, mezigdomide) bind cereblon more tightly and degrade these targets faster and more deeply, producing responses in myeloma refractory to lenalidomide and pomalidomide in phase 1 and 2 trials; phase 3 trials with dexamethasone and antibodies are under way. Neutropenia is the main toxicity.
Molecular glues bind cereblon and reshape its surface so that transcription factors Ikaros and Aiolos are ubiquitinated and degraded, killing plasma cells and stimulating T cells.
Iberdomide is a far more potent successor to lenalidomide, now in phase 3 as post-transplant maintenance and in relapsed disease.
Mezigdomide is the most potent oral cereblon modulator, producing responses in about 40% of triple-class-refractory myeloma with dexamethasone alone.
Query for this technology: (TITLE:"Cereblon E3 ligase modulators" OR ABSTRACT:"Cereblon E3 ligase modulators" OR TITLE:"CELMoDs" OR ABSTRACT:"CELMoDs") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Cereblon E3 ligase modulators (CELMoDs), not a curated reading list.
Shares Iberdomide, Mezigdomide, Multiple myeloma.
Shares A Study to Determine Dose, Safety, Tolerability and Efficacy of CC-220 Monotherapy, and in Combination With Other Treatments in Subjects With Multiple, A Study to Evaluate Mezigdomide in Combination With Carfilzomib and Dexamethasone (MeziKD) Versus Carfilzomib and Dexamethasone (Kd) in Participants W, A Study to Determine the Recommended Dose and Regimen and to Evaluate the Safety and Preliminary Efficacy of CC-92480 in Combination With Standard Tre, Relapsed or refractory multiple myeloma.
Shares Iberdomide, Mezigdomide, IKZF1 (Ikaros), IKZF3 (Aiolos).
Shares IKZF1 (Ikaros), IKZF3 (Aiolos), IRF4.
Shares Cereblon (CRBN), A Study to Evaluate Mezigdomide, Bortezomib and Dexamethasone (MEZIVd) Versus Pomalidomide, Bortezomib and Dexamethasone (PVd) in Participants With Re, IKZF1 (Ikaros), IKZF3 (Aiolos).
Shares Molecular glue discovery platforms, Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares A Study to Compare Iberdomide Maintenance Versus Lenalidomide Maintenance Therapy Following Autologous Stem Cell Transplant in Participants With Newly, A Study to Determine Dose, Safety, Tolerability and Efficacy of CC-220 Monotherapy, and in Combination With Other Treatments in Subjects With Multiple, A Study to Determine the Recommended Dose and Schedule, and Evaluate the Safety and Preliminary Efficacy of Mezigdomide in Combination With Elranatama, A Study to Evaluate Mezigdomide in Combination With Carfilzomib and Dexamethasone (MeziKD) Versus Carfilzomib and Dexamethasone (Kd) in Participants W.
Shares Iberdomide, Multiple myeloma.