The drug candidate camizestrant (AZD-9833), recently highlighted by Drug Hunter, is a next-generation orally active and selective estrogen receptor degrader (SERD) now in Phase III trials for ER-positive breast cancer. We have created a set of analogs to this molecule!

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Camizestrant demonstrates robust estrogen receptor (ER) degradation and antiproliferative activity in both ESR1 wild-type and ESR1 mutant breast cancer cell lines, as well as in patient-derived xenograft (PDX) models. Furthermore, its combination with CDK4/6 inhibitors and PI3K/AKT/mTOR-targeted therapy enhances its antitumor efficacy, suggesting its great potential as a basis in endocrine therapy for ER-positive breast cancer. Developing new SERDs is a prominent strategy for addressing endocrine resistance, a significant barrier to cancer treatment.

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