Lasofoxifene treatment of breast cancer

Abstract

The disclosure provides methods for treating estrogen receptor positive (ER⁺) cancer in women with an effective amount of lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The disclosure also includes the detection of the Estrogen Receptor 1 (ESR1) gene mutations that lead to endocrine resistance and treatment of endocrine resistant ER⁺ cancers.

Description

1. CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application Nos. 62 / 502,299, filed May 5, 2017; 62 / 457,759, filed Feb. 10, 2017; and 62 / 406,859, filed Oct. 11, 2016, each of which is incorporated in its entirety by reference.2. SEQUENCE LISTING[0002]The instant application contains a Sequence Listing which has been submitted via EFS-Web and is hereby incorporated by reference in its entirety. Said ASCII copy, created on Oct. 9, 2017, is named 33498US_CRF_sequencelisting.txt, and is 2,118 bytes in size.3. BACKGROUND OF THE INVENTION[0003]Estrogen receptor positive (ER+) breast cancers are a group of breast cancers that express estrogen receptor α (ERα). Approximately 70% of breast cancers are ER+ and are, therefore, treated with endocrine therapy. Endocrine therapy has led to significant improvement in outcome of women with ER+ breast cancer by lowering the level of estrogen or blocking estrogen signaling. However, its effective...

AI Technical Summary

Benefits of technology

[0008]In a second series of experiments, we confirmed that lasofoxifene is able to reduce viability of the breast cancer cel

Problems solved by technology

However, its effectiveness is limited by i

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