Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer: Dr. Stefan Peukert

Seminar series
Organic Colloquium
When
Thu, Apr 11 2:00pm to 3:00pm
Where
Molecular Sciences 3440
Speaker Dr. Stefan Peukert
Novartis Institute of BioMedical Research (Cambridge) Global Discovery Chemistry
Global Discovery Chemistry
Description

Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer

Abstract: The estrogen receptor (ER) is a nuclear hormone receptor that regulates a variety of genes which promote both cell proliferation and cell cycle progression. In the clinical setting ER positive breast cancer accounts for approximately 2/3 of all breast cancer diagnoses. Anti-estrogen therapies, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AI), are the core treatment modalities in patients with ER positive breast cancer. Although a large proportion of patients respond positive to endocrine therapy, resistance to these drug treatments remains an impediment to durable clinical response. Selective estrogen receptor degraders (SERDs) that remove the receptor have been shown to be effective in this setting. We describe the discovery of LSZ102, a potent, orally available SERD found to inhibit ER mediated transcription and proliferation in a cell culture model of ER positive breast cancer Activity in mouse models of ER positive breast cancer, pharmacokinetic properties in preclinical species and early clinical data from an ongoing Phase I trial in patients are presented.

 

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