Activity of preclinical and phase I clinical trial of a novel androgen receptor antagonist GT0918 in metastatic breast cancer

Purpose To evaluate GT0918, a 2nd-generation AR antagonist, for its AR down-regulation activity among breast cancer patients. Methods The effect of GT0918 on AR protein expression was evaluated in AR expression breast cancer cells and in breast cancer xenograft model. A 3 + 3 phase I dose-escalation...

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Veröffentlicht in:	Breast cancer research and treatment 2021-10, Vol.189 (3), p.725-736
Hauptverfasser:	Li, Huiping, Song, Guohong, Zhou, Qiaoxia, Ran, Ran, Jiang, Hanfang, Zhang, Ruyan, Liu, Yaxin, Zhang, Jiayang, Meng, Luping, Ma, Liandong, Sun, Ye, Wang, Meiyu, Zhou, Qingqing, Yan, Honghua, Zhou, Qianxiang, Dong, Xunwei, Tong, Youzhi
Format:	Artikel
Sprache:	eng
Schlagworte:	Alanine Alanine transaminase Androgen Receptor Antagonists Androgen receptors Animal models Animals Antitumor activity Appetite loss Aspartate Aspartate aminotransferase Asthenia Blood Blood cell count Blood cholesterol Breast cancer Breast Neoplasms - drug therapy Cancer research Cholesterol Clinical Trial Clinical trials Dosage Down-regulation Female Humans Leukocytes (neutrophilic) Low density lipoproteins Medicine Medicine & Public Health Metastases Metastasis Mice NCT NCT04103853 Oncology Oxazoles Patients Pharmacokinetics Product development Receptors, Androgen Thiohydantoins Triglycerides Tumors Xenografts
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