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

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 with proves its suitability.

Keywords

PET/CT PSMA prostate cancer radiation dosimetry radiation dosage

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