This is a single-arm, open-label, Phase I/II clinical study designed to evaluate the safety, tolerability, pharmacokinetics, dosimetry, pharmacodynamics, and preliminary efficacy of Gallium \[68Ga\] PSMA-0057 Injection and Lutetium \[177Lu\] PSMA-0057 Injection as an integrated theranostic regimen in patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). The study consists of a Phase I dose-escalation phase to determine the maximum tolerated dose (MTD) and/or recommended Phase II dose (RP2D) of 177Lu-PSMA-0057, followed by a Phase II dose-expansion phase to further evaluate preliminary antitumor efficacy and confirm safety and pharmacologic profiles. Eligible participants will receive 68Ga-PSMA-0057 for PET imaging and 177Lu-PSMA-0057 for radioligand therapy. Key objectives include characterization of safety, tolerability, pharmacokinetics, dosimetry, pharmacodynamics, and preliminary therapeutic activity.
Able to communicate well with investigators, understand the study purpose and requirements, voluntarily participate, and sign written informed consent.
Male, ≥18 years at screening.
Histologically or cytologically confirmed prostate cancer (excluding neuroendocrine prostate cancer and small cell prostate cancer), previously treated with at least one novel hormonal agent and 1-2 taxane-based regimens, or deemed intolerant to taxanes.
Serum/plasma testosterone at castrate level (<50 ng/dL or <1.7 nmol/L).
History of hypersensitivity to any study drug component or excipients, or history of specific allergic disease requiring systemic therapy, or other serious allergic reactions.
Prior PSMA-targeted radioligand therapy, or treatment with radionuclides such as Sr-89, Sm-153, Re-186, Re-188, Ra-223, or hemibody radiation within 6 months prior to consent.
Use of any investigational drug or device within 30 days before consent.
Systemic anticancer therapy within 28 days or 5 half-lives prior to consent (whichever is longer), including chemotherapy, radiotherapy, immunotherapy, targeted therapy, systemic immunomodulatory drugs, or antitumor traditional Chinese medicines/formulations within 2 weeks before first dose.
Sequential
68Ga-PSMA-0057
Drug68Ga-PSMA-0057 IV administered as imaging agent for PET/CT.
177Lu-PSMA-0057
Drug177Lu-PSMA-0057 radiopharmaceutical solution for injection.
Incidence of adverse events [68Ga-PSMA-0057]
Number of participants with adverse events as assessed by NCI-CTCAE v5.0
Incidence of adverse events [177Lu-PSMA-0057]
Number of participants with adverse events as assessed by NCI-CTCAE v5.0
Incidence of dose limiting toxicities [177Lu-PSMA-0057]
Number of participants with dose limiting toxicities
Preliminary efficacy: PSA50 response rate (Phase II)
Proportion of patients achieving ≥50% reduction in prostate-specific antigen (PSA) from baseline.
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