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A 3\u2009+\u20093 dose-escalation design was utilized with a starting dose of 50\u00a0mg daily for 3\u00a0weeks on and 1\u00a0week off treatment in 28-day cycles. Patients received escalating doses of FCN-437c monotherapy (50, 100, 200, 300, and 450\u00a0mg). <jats:italic>Results\u00a0<\/jats:italic>Seventeen patients received FCN-437c 50\u00a0mg (<jats:italic>n<\/jats:italic>\u2009=\u20093), 100\u00a0mg (<jats:italic>n<\/jats:italic>\u2009=\u20093), 200\u00a0mg (<jats:italic>n<\/jats:italic>\u2009=\u20093), 300\u00a0mg (<jats:italic>n<\/jats:italic>\u2009=\u20096), and 450\u00a0mg (<jats:italic>n<\/jats:italic>\u2009=\u20092). Two patients who received the 450-mg dose experienced dose-limiting toxicities (DLTs; grade 4 thrombocytopenia and neutropenia); no DLT was observed at any other dose level. Frequently reported treatment-emergent adverse events (TEAEs) of any grade were hematological: leukopenia (94.1%), neutropenia (88.2%), anemia (64.7%), and thrombocytopenia (47.1%). Grade 3\u20134 TEAEs included neutropenia (64.7%) and leukopenia (47.1%). Exposure of FCN-437c increased almost proportionally to doses ranging from 50 to 200\u00a0mg. At doses from 200 to 450\u00a0mg, there appeared to be a trend of saturation. The MTD was determined to be 300\u00a0mg. Of 15 patients with measurable disease, nine (60.0%) patients experienced stable disease; no complete or partial responses were observed. <jats:italic>Conclusions\u00a0<\/jats:italic>These results established an acceptable safety profile for FCN-437c in patients with advanced BC, and there were no unexpected signals relative to other CDK4\/6 inhibitors. 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The study was approved by the Ethics Committee of Fudan University Shanghai Cancer Center (No. 1806186\u20138-1808), Cancer Hospital of the University of Chinese Academy of Sciences (No. IRB-[2019]619), and Sir Run Run Shaw Hospital (No. 20190927\u201314).","order":2,"name":"Ethics","group":{"name":"EthicsHeading","label":"Ethics approval"}},{"value":"Informed consent was obtained from all individuals who participated in the study.","order":3,"name":"Ethics","group":{"name":"EthicsHeading","label":"Consent to participate"}},{"value":"The study was initiated, funded, and sponsored by Avanc Pharmaceutical Co., Ltd. Jian Zhang, Xiaojia Wang, Xian Wang, and Xichun Hu declare no potential conflicts of interest. Aimin Hui is a full-time employee of Fosun Pharma USA Inc. Zhuli Wu, Changjiang Xu, Yuchen Yang, and Wenjing Zhang are full-time employees of Beijing Fosun Pharmaceutical Research and Development Co., Ltd. Ling Tian is a full-time employee of Avanc Pharmaceutical Co., Ltd.","order":4,"name":"Ethics","group":{"name":"EthicsHeading","label":"Conflicts of interest\/competing interests"}}]}}