Aromatase Inhibitor Breast Cancer Therapeutics with Reduced Potential for Side Effects

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2016-CUSH-67271
Aromatase is an enzyme that catalyzes the conversion of androgens to estrogens, which is a crucial step in the biosynthesis of estrogens in the human body. Hormone-receptor-positive breast cancer cells are stimulated by estrogen; therefore, aromatase inhibitors (AI) have been widely used for treatment of this cancer in postmenopausal women. Despite the efficacy of AIs, these drugs have a variety of side effects including joint pain and susceptibility to bone fracture. More than 10 percent of patients discontinue AI therapy after six months due to musculoskeletal toxicity.

To combat these side effects, researchers at Purdue University have developed a compound with dual activity as an aromatase inhibitor and selective estrogen receptor modulator. The compound's activity as a selective estrogen receptor modulator promises a way to avoid the undesired side effects. The compound's display binding to both aromatase and estrogen receptors and modulate estrogen receptor activity in vitro.

Advantages:
-Fewer potential side effects than current aromatase inhibitors
-Modulates estrogen receptors

Potential Applications:
-Breast cancer treatment

Related Publications:
Lv, Wei, et al. Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen
Receptors. Journal of Medicinal Chemistry. 2016, 59, pp 157-170.
DOI: 10.1021/acs.jmedchem.5b01677.
Nov 22, 2016
Utility Patent
United States
9,845,295
Dec 19, 2017

Nov 24, 2015
Provisional-Patent
United States
(None)
(None)
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