| Hazard Information | Back Directory | [Uses]
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL)[1][2]. | [in vivo]
Golcadomide (1 mg/kg) monotherapy results in modest tumor growth inhibition, whereas the combination of Golcadomide (1 mg/kg) and rituximab (10 mg/kg) results in tumor regression in 100% of animals in the WSU-DLCL2 model and the FL xenograft model. | [IC 50]
Cereblon | [References]
[1] J.-M. Michot, et al. A PHASE 1, MULTICENTER, OPEN-LABEL STUDY OF CC-99282 ALONE AND IN COMBINATION WITH RITUXIMAB IN PATIENTS WITH RELAPSED OR REFRACTORY NON-HODGKIN LYMPHOMAS. Hematological Oncology. Volume 39, Issue S2, Jun. 2021.
[2] Carrancio S, et al. CC-99282 is a novel cereblon (CRBN) E3 ligase modulator (CELMoD) agent with enhanced tumoricidal activity in preclinical models of lymphoma[J]. Blood, 2021, 138: 1200. |
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