Pharmacokinetics and Dosimetry of [68Ga]Ga-PSMA-11 in Chinese Participants with Progressive Metastatic Castration-Resistant Prostate Cancer: A Phase 2 Study

Wei Fan; Yonghong Li; Hongcheng Shi; Jianming Guo; Rui Huang; Qiang Dong; Zhi Yang; Yong Yang; Xinlu Wang; Di Gu; Dingwei Ye; Feng Wang; Jing Wang; Danfeng Xu; Zhiqiang Jiang; Haifu Li; Jialu Li; Runqin Li; Li Huo; Zhigang Ji

doi:10.1177/10849785251415122

Pharmacokinetics and Dosimetry of [⁶⁸Ga]Ga-PSMA-11 in Chinese Participants with Progressive Metastatic Castration-Resistant Prostate Cancer: A Phase 2 Study

Cancer Biother Radiopharm. 2026 Feb 14:10849785251415122. doi: 10.1177/10849785251415122. Online ahead of print.

Authors

Wei Fan¹, Yonghong Li², Hongcheng Shi², Jianming Guo³, Rui Huang⁴, Qiang Dong⁵, Zhi Yang⁶, Yong Yang⁷, Xinlu Wang⁸, Di Gu⁹, Dingwei Ye¹⁰, Feng Wang¹¹, Jing Wang¹², Danfeng Xu¹³, Zhiqiang Jiang¹⁴, Haifu Li¹⁵, Jialu Li¹⁶, Runqin Li¹⁷, Li Huo¹⁸, Zhigang Ji¹⁸

Affiliations

¹ Department of Nuclear Medicine, Sun Yat-sen University Cancer Center, Guangzhou, China.
² Department of Urology, Sun Yat-sen University Cancer Center, Guangzhou, China.
³ Department of Urology, Fudan University Zhongshan Hospital, Shanghai, China.
⁴ Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, China.
⁵ Department of Urology, West China Hospital, Sichuan University, Chengdu, China.
⁶ Department of Nuclear Medicine, Peking University Cancer Hospital, Beijing, China.
⁷ Department of Urology, Peking University Cancer Hospital, Beijing, China.
⁸ Department of Nuclear Medicine, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, China.
⁹ Department of Urology, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, China.
¹⁰ Department of Urology, Fudan University Shanghai Cancer Center, Shanghai, China.
¹¹ Department of Nuclear Medicine, Nanjing First Hospital, Nanjing, China.
¹² Department of Nuclear Medicine, Xijing Hospital, Xi'an, China.
¹³ Department of Urology, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
¹⁴ Novartis Biomedical Research, Shanghai, China.
¹⁵ Novartis Development, Beijing, China.
¹⁶ Novartis Development, Shanghai, China.
¹⁷ Novartis Pharmaceuticals Corporation, Shanghai, China.
¹⁸ Peking Union Medical College Hospital, Beijing, China.

PMID: 41689461
DOI: 10.1177/10849785251415122

Abstract

Introduction: [⁶⁸Ga]Ga-prostate-specific membrane antigen (PSMA)-11 positron emission tomography (PET)/computed tomography (CT) imaging has demonstrated clinical value for individuals with prostate cancer (PC). In this phase 2 study, we measured the pharmacokinetics and dosimetry of [⁶⁸Ga]Ga-PSMA-11 in Chinese participants.

Methods: Adult Chinese participants with progressive metastatic castration-resistant PC (mCRPC) received a single intravenous [⁶⁸Ga]Ga-PSMA-11 dose of approximately 150 MBq. Blood samples were collected at 5, 15, 30, 45, 85, 175, and 245 min post injection for pharmacokinetics assessments. Whole-body PET scans and low/ultra-low-dose CT scans were acquired at 30, 60, 120, and 255 min post injection for dosimetry assessments.

Results: Pharmacokinetics and dosimetry assessments were completed in seven participants who received a [⁶⁸Ga]Ga-PSMA-11 dose (range: 108.3-236.7 MBq). In the blood, the geometric mean effective terminal half-life was 1.34 h (geometric coefficient of variation [geo-CV], 182%); geometric mean clearance was 9.80 L/h (geo-CV, 106%). The highest absorbed doses were seen in the kidneys, urinary bladder walls, and lacrimal glands. In the study population, the geometric mean (geo-CV) effective dose of [⁶⁸Ga]Ga-PSMA-11 was 4.2 mSv (32.9%).

Conclusions: The pharmacokinetic and dosimetry profiles of [⁶⁸Ga]Ga-PSMA-11, assessed using a validated method in participants with progressive mCRPC, make it very suitable as an imaging agent.

Keywords: 68Ga-PSMA-11; PET/CT; PSMA; prostate cancer; radiation dosage; radiation dosimetry.