Phase Ib Study of the Oral Proteasome Inhibitor Ixazomib (MLN9708) and Fulvestrant in Advanced ER+ Breast Cancer Progressing on Fulvestrant

Abstract

is a selective estrogen receptor (ER)downregulating anti-estrogen that blocks ER transcriptional activity and is approved for ER+ breast cancer. • Fulvestrant also induces accumulation of insoluble ER and activates an unfolded protein response; proteasome inhibitors have been shown to enhance these effects in preclinical models.

Complete pathological response of hormone receptor positive invasive breast cancer in a patient with multiple myeloma treated with ixazomib

“…Although a limited number of patients were recruited, this clinical trial has shown that IX may be a valuable therapy in such context. 15…”

Inhibitory effort of MLN2238 on basal-like breast cancer: An investigation based on the gene set enrichment analysis

“…Then, the cells were stained with 50 μg/ml PI (Sigma Chemicals, St. Louis, MO, USA) after being incubated with 100 μg/ml RNase for 30 min (Sigma Chemicals, St. Louis, MO, USA). And finally, FACSC-Calibur (BD Biosciences, Franklin Lakes, NJ, USA) and FCS express software (DeNovo Software, Los Angeles, CA, USA) were used to analyze DNA contents by flow cytometry (17).…”

“…The research showed that the structure of MLN2238 is different from bortezomib (15). MLN2238 (ixazomib) has been given great promise because of the proven clinical effects of bortezomib which was another proteasome inhibitor (16,17). Moreover, the disassociation half-life of ixazomib was six-fold faster than bortezomib which made ixazomib fast dissociate from red blood cells and rapidly entered into the tumor cells (18).…”