Ontology highlight
ABSTRACT:
SUBMITTER: Lu Y
PROVIDER: S-EPMC7261373 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Lu Yunlong Y Gutgesell Lauren M LM Xiong Rui R Zhao Jiong J Li Yangfeng Y Rosales Carlo I CI Hollas Michael M Shen Zhengnan Z Gordon-Blake Jesse J Dye Katherine K Wang Yueting Y Lee Sue S Chen Hu H He Donghong D Dubrovyskyii Oleksii O Zhao Huiping H Huang Fei F Lasek Amy W AW Tonetti Debra A DA Thatcher Gregory R J GRJ
Journal of medicinal chemistry 20191210 24
The clinical steroidal selective estrogen receptor (ER) degrader (SERD), fulvestrant, is effective in metastatic breast cancer, but limited by poor pharmacokinetics, prompting the development of orally bioavailable, nonsteroidal SERDs, currently in clinical trials. These trials address local breast cancer as well as peripheral metastases, but patients with brain metastases are generally excluded because of the lack of blood-brain barrier penetration. A novel family of benzothiophene SERDs with a ...[more]