AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models.

doi:10.1158/0008-5472.CAN-15-2357

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Article

AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models.

Cancer research - 1 Jun 2016

Weir Hazel M, Bradbury Robert H, Lawson Mandy, Rabow Alfred A, Buttar David, Callis Rowena J, Curwen Jon O, de Almeida Camila, Ballard Peter, Hulse Michael, Donald Craig S, Feron Lyman J L, Karoutchi Galith, MacFaul Philip, Moss Thomas, Norman Richard A, Pearson Stuart E, Tonge Michael, Davies Gareth, Walker Graeme E, Wilson Zena, Rowlinson Rachel, Powell Steve, Sadler Claire, Richmond Graham, Ladd Brendon, Pazolli Ermira, Mazzola Anne Marie, D'Cruz Celina, De Savi Chris

Abstract excerpt

Fulvestrant is an estrogen receptor (ER) antagonist administered to breast cancer patients by monthly intramuscular injection. Given its present limitations of dosing and route of administration, a more flexible orally available compound has been sought to pursue the potential benefits of this drug in patients with advanced metastatic disease. Here we report the identification and characterization of AZD9496, a...

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PMID: 27020862
DOI: 10.1158/0008-5472.CAN-15-2357

Genes

ESR1
CDK4

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