An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial

Abstract Background Bireociclib (XZP‐3287) is a novel selective cyclin‐dependent kinase 4 and 6 (CDK4/6) inhibitor, with a favorable safety profile demonstrated in preclinical and phase I studies. BRIGHT‐1 aimed to further explore the efficacy and safety of bireociclib monotherapy in patients with l...

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Main Authors: Jiayu Wang, Qingyuan Zhang, Tao Sun, Huiping Li, Ying Cheng, Zhongsheng Tong, Huihui Li, Wei Li, Jingfen Wang, Yuee Teng, Xinhong Wu, Jing Cheng, Zhendong Chen, Zhengqiu Zhu, Li Wang, Mingming Liu, Xianghui Duan, Lingmei Xu, Binghe Xu
Format: Article
Language:English
Published: Wiley 2025-06-01
Series:Cancer Communications
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Online Access:https://doi.org/10.1002/cac2.70009
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author Jiayu Wang
Qingyuan Zhang
Tao Sun
Huiping Li
Ying Cheng
Zhongsheng Tong
Huihui Li
Wei Li
Jingfen Wang
Yuee Teng
Xinhong Wu
Jing Cheng
Zhendong Chen
Zhengqiu Zhu
Li Wang
Mingming Liu
Xianghui Duan
Lingmei Xu
Binghe Xu
author_facet Jiayu Wang
Qingyuan Zhang
Tao Sun
Huiping Li
Ying Cheng
Zhongsheng Tong
Huihui Li
Wei Li
Jingfen Wang
Yuee Teng
Xinhong Wu
Jing Cheng
Zhendong Chen
Zhengqiu Zhu
Li Wang
Mingming Liu
Xianghui Duan
Lingmei Xu
Binghe Xu
author_sort Jiayu Wang
collection DOAJ
description Abstract Background Bireociclib (XZP‐3287) is a novel selective cyclin‐dependent kinase 4 and 6 (CDK4/6) inhibitor, with a favorable safety profile demonstrated in preclinical and phase I studies. BRIGHT‐1 aimed to further explore the efficacy and safety of bireociclib monotherapy in patients with locally advanced, recurrent or metastatic, hormone receptor‐positive and human epidermal growth factor receptor 2‐negative (HR+/HER2−) breast cancer who had progressed on or after prior chemotherapy and endocrine therapy in advanced settings, without previous exposure to CDK4/6 inhibitors. Methods In this open‐label phase II trial, eligible patients received bireociclib 480 mg twice daily (BID) until disease progression or intolerable toxicities. The primary endpoint was the confirmed objective response rate (ORR) assessed by an independent review committee (IRC). The secondary endpoints included progression‐free survival (PFS), investigator‐assessed ORR, disease control rate (DCR), clinical benefit rate (CBR), duration of response (DoR), overall survival (OS), safety and the pharmacokinetic properties of bireociclib. Results A total of 131 patients were enrolled. At data cutoff (July 31, 2023), the IRC‐assessed ORR was 29.8% (95% confidence interval [CI], 22.1% to 38.4%), with a DCR of 73.3% (95% CI, 64.8% to 80.6%), CBR of 42.0% (95% CI, 33.4% to 50.9%) and a median DoR of 15.2 months (95% CI, 9.5 months to not reached). The median PFS was 11.0 months (95% CI, 7.3 months to 12.9 months) assessed by the IRC, and the median OS was 29.0 months (95% CI, 24.9 months to not reached). The most frequently reported treatment‐emergent adverse events (TEAEs) of any grade were diarrhea (93.1%), neutrophil count decreased (87.0%), white blood cell decreased (86.3%), vomiting (78.6%), anemia (72.5%), and platelet count decreased (72.5%). The grade ≥3 TEAEs occurred in 109 (83.2%) patients. The most common grade ≥3 TEAEs were neutrophil count decreased (43.5%), white blood cell decreased (32.8%), hypokalemia (20.6%), and diarrhea (19.1%). Conclusions Bireociclib monotherapy at 480 mg BID exhibited promising and sustained clinical activity, with no unexpected and acceptable toxicity in patients with recurrent or metastatic HR+/HER2− breast cancer who had progressed on or after previous therapy. Trial registration Clinicaltrials.gov ID, NCT04539496.
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spelling doaj-art-e2134f856cb041a0b3cd055c60dd48732025-08-20T02:20:51ZengWileyCancer Communications2523-35482025-06-0145664065310.1002/cac2.70009An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trialJiayu Wang0Qingyuan Zhang1Tao Sun2Huiping Li3Ying Cheng4Zhongsheng Tong5Huihui Li6Wei Li7Jingfen Wang8Yuee Teng9Xinhong Wu10Jing Cheng11Zhendong Chen12Zhengqiu Zhu13Li Wang14Mingming Liu15Xianghui Duan16Lingmei Xu17Binghe Xu18Department of Medical Oncology and State Key Laboratory of Molecular OncologyNational Cancer Center/Cancer HospitalChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijingP. R. ChinaDepartment of Breast & LymphomaHarbin Medical University Cancer HospitalHarbinHeilongjiangP. R. ChinaDepartment of Breast MedicineInstitute of OncologyCancer Hospital of Dalian University of TechnologyLiaoning Cancer HospitalShenyangLiaoningP. R. ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education)Department of Breast OncologyPeking University Cancer Hospital and InstituteBeijingP. R. ChinaDepartment of Thoracic Medical OncologyJilin Provincial Cancer HospitalChangchunJilinP. R. ChinaDepartment of Breast OncologyTianjin Medical University Cancer Institute and HospitalTianjinP. R. ChinaDepartment of Breast Medical OncologyShandong Cancer Hospital Affiliated to Shandong UniversityJinanShandongP. R. ChinaCancer CenterThe First Bethune Hospital of Jilin UniversityChangchunP. R. ChinaDepartment of Breast Medical OncologyLinyi Cancer HospitalLinyi Shandong P. R. ChinaDepartment of Breast Internal MedicineThe First Hospital of China Medical UniversityShenyangLiaoningP. R. ChinaDepartment of Breast SurgeryHubei Cancer HospitalTongji Medical CollegeHuazhong University of Science and TechnologyHubei Provincial Clinical Research Center for Breast Cancer, and Wuhan Clinical Research Center for Breast CancerWuhanHubeiP. R. ChinaCancer CenterUnion HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhanHubeiP. R. ChinaDepartment of OncologyThe Second Hospital of Anhui Medical UniversityHefeiAnhuiP. R. ChinaDepartment of OncologyThe Affiliated Hospital of Xuzhou Medical UniversityXuzhouJiangsuP. R. ChinaClinical Science DepartmentXuanzhu Biopharmaceutical Co., Ltd.BeijingP. R. ChinaClinical Science DepartmentXuanzhu Biopharmaceutical Co., Ltd.BeijingP. R. ChinaClinical Science DepartmentXuanzhu Biopharmaceutical Co., Ltd.BeijingP. R. ChinaClinical Science DepartmentXuanzhu Biopharmaceutical Co., Ltd.BeijingP. R. ChinaDepartment of Medical Oncology and State Key Laboratory of Molecular OncologyNational Cancer Center/Cancer HospitalChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijingP. R. ChinaAbstract Background Bireociclib (XZP‐3287) is a novel selective cyclin‐dependent kinase 4 and 6 (CDK4/6) inhibitor, with a favorable safety profile demonstrated in preclinical and phase I studies. BRIGHT‐1 aimed to further explore the efficacy and safety of bireociclib monotherapy in patients with locally advanced, recurrent or metastatic, hormone receptor‐positive and human epidermal growth factor receptor 2‐negative (HR+/HER2−) breast cancer who had progressed on or after prior chemotherapy and endocrine therapy in advanced settings, without previous exposure to CDK4/6 inhibitors. Methods In this open‐label phase II trial, eligible patients received bireociclib 480 mg twice daily (BID) until disease progression or intolerable toxicities. The primary endpoint was the confirmed objective response rate (ORR) assessed by an independent review committee (IRC). The secondary endpoints included progression‐free survival (PFS), investigator‐assessed ORR, disease control rate (DCR), clinical benefit rate (CBR), duration of response (DoR), overall survival (OS), safety and the pharmacokinetic properties of bireociclib. Results A total of 131 patients were enrolled. At data cutoff (July 31, 2023), the IRC‐assessed ORR was 29.8% (95% confidence interval [CI], 22.1% to 38.4%), with a DCR of 73.3% (95% CI, 64.8% to 80.6%), CBR of 42.0% (95% CI, 33.4% to 50.9%) and a median DoR of 15.2 months (95% CI, 9.5 months to not reached). The median PFS was 11.0 months (95% CI, 7.3 months to 12.9 months) assessed by the IRC, and the median OS was 29.0 months (95% CI, 24.9 months to not reached). The most frequently reported treatment‐emergent adverse events (TEAEs) of any grade were diarrhea (93.1%), neutrophil count decreased (87.0%), white blood cell decreased (86.3%), vomiting (78.6%), anemia (72.5%), and platelet count decreased (72.5%). The grade ≥3 TEAEs occurred in 109 (83.2%) patients. The most common grade ≥3 TEAEs were neutrophil count decreased (43.5%), white blood cell decreased (32.8%), hypokalemia (20.6%), and diarrhea (19.1%). Conclusions Bireociclib monotherapy at 480 mg BID exhibited promising and sustained clinical activity, with no unexpected and acceptable toxicity in patients with recurrent or metastatic HR+/HER2− breast cancer who had progressed on or after previous therapy. Trial registration Clinicaltrials.gov ID, NCT04539496.https://doi.org/10.1002/cac2.70009advanced breast cancerbireociclibCDK4/6 inhibitorendocrine therapyHER2−HR+
spellingShingle Jiayu Wang
Qingyuan Zhang
Tao Sun
Huiping Li
Ying Cheng
Zhongsheng Tong
Huihui Li
Wei Li
Jingfen Wang
Yuee Teng
Xinhong Wu
Jing Cheng
Zhendong Chen
Zhengqiu Zhu
Li Wang
Mingming Liu
Xianghui Duan
Lingmei Xu
Binghe Xu
An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial
Cancer Communications
advanced breast cancer
bireociclib
CDK4/6 inhibitor
endocrine therapy
HER2−
HR+
title An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial
title_full An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial
title_fullStr An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial
title_full_unstemmed An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial
title_short An open‐label, single‐arm, multicenter, phase II trial of bireociclib as monotherapy for heavily pretreated HR‐positive, HER2‐negative advanced breast cancer patients: BRIGHT‐1 trial
title_sort open label single arm multicenter phase ii trial of bireociclib as monotherapy for heavily pretreated hr positive her2 negative advanced breast cancer patients bright 1 trial
topic advanced breast cancer
bireociclib
CDK4/6 inhibitor
endocrine therapy
HER2−
HR+
url https://doi.org/10.1002/cac2.70009
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