Clinical Evaluation of 177Lu-PSMA-VG01 Injection in Patients With PSMA-Positive Metastatic Castration-Resistant Prostate Cancer （mCRPC）

A Phase 1, Dose-Escalation Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Biodistribution, Radiation Dosimetry and Preliminary Efficacy of 177Lu-PSMA-VG01 Injection in Patients With PSMA-Positive Metastatic Castration-Resistant Prostate Cancer (mCRPC)

This is a phase I clinical trial conducted in participants with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). After confirmation of PSMA positivity, participants receive intravenous administration of 177Lu-PSMA-VG01. The objectives are: to evaluate the biodistribution, radiation dosimetry, safety and tolerability of 177Lu-PSMA-VG01 in participants; and to assess the pharmacokinetics (PK), preliminary anti-tumor activity, and in vivo stability of 177Lu-PSMA-VG01 in participants.

Study Overview

• Status: Recruiting
• Conditions: PSMA-positive Metastatic Castration-resistant Prostate Cancer (mCRPC)
• Intervention / Treatment: Drug: 177Lu-PSMA-VG01

Detailed Description

This is a prospective, single-arm, dose-escalation and open phase I clinical study. 10-24 participants are expected to be enrolled. Participants will sign the informed consent form (ICF) prior to screening.

Only PSMA-positive participants with metastatic castration-resistant prostate cancer (mCRPC) who meet the inclusion criteria and do not meet any exclusion criteria will be enrolled. The successful screened participants will be treated with 177Lu-PSMA-VG01 injection intravenously during the treatment period. Pharmacokinetic (PK) blood samples will be collected, and SPECT/CT imaging will be performed during the clinical study.

Long-term follow-up will last up to 2 years after completion of EOT. Throughout the study period, participants will undergo safety monitoring following drug administration.

• Study Type: Interventional
• Enrollment (Estimated): 10
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Xiaobo Su; Phone Number: 086+0632-2989679; Email: xiaobo.su@vitsgen.com

Study Locations

• China
  • Shanghai Municipality
    • Shanghai, Shanghai Municipality, China, 200032
      • Recruiting
      • Zhong Shan Hospital Fudan University
      • Contact: Hongcheng Shi, Doctor of Medicine; Phone Number: 086+ 021-64041990; Email: shi.hongcheng@zs-hospital.sh.cn

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

1. Male participants aged 18 years (inclusive) to 80 years (exclusive) at the time of signing the informed consent.
2. Histologically or cytologically confirmed prostate cancer with no standard treatment options available, or failure/intolerance to standard therapies, or inability to access standard treatment.
3. During the screening period, imaging examinations (within 4 weeks before administration) showed the presence of ≥1 metastatic lesion.
4. ECOG Performance Status score: 0 to 2.
5. Expected survival time exceeds 6 months.
6. All clinically significant toxicities related to prior anti-tumor therapy (e.g., chemotherapy, radiotherapy, etc., excluding Luteinizing Hormone-Releasing Hormone (LHRH) analog therapy) must have resolved to ≤ Grade 1, except for toxicities deemed safe and manageable by the investigator, such as alopecia, peripheral neuropathy ≤ Grade 2, etc. (CTCAE V6.0).
7. The participant must be fully informed about the study and voluntarily provide written informed consent prior to participation.
8. The participant must be capable of understanding and complying with the requirements of the trial protocol.
9. The participant must use a condom during sexual activity throughout the study period and for 14 weeks after the last dose of study treatment to prevent pregnancy in partners and potential exposure of partners to the investigational product g via semen. Additionally, the participant should refrain from sperm donation during the specified timeframe above.

Exclusion Criteria:

1. Having received anti-tumor therapies such as chemotherapy, biological therapy, targeted therapy, or immunotherapy within 4 weeks prior to the first dose of the investigational product, or planning to receive such therapies during the study period.
2. Having received systemic or local radionuclide therapy within 3 months prior to the first dose.
3. Having received other investigational product treatments not yet approved within 4 weeks prior to the first dose of the investigational product, or within five half-lives of that.
4. Having undergone major organ surgery (excluding needle biopsy) or experienced significant trauma within 4 weeks prior to the first dose of the investigational product, or requiring elective surgery during the trial period.
5. Having been diagnosed with other malignancies within the past 2 years (participants with a prior history of malignancy who have received adequate treatment and have remained disease- and treatment-free for over 3 years prior to enrollment are eligible, as are patients with adequately treated non-melanoma skin cancer or superficial bladder cancer).
6. Having symptomatic spinal cord compression or clinical/imaging findings suggestive of impending spinal cord compression.
7. Known allergy to structural analogs of this product or other excipients.
8. Having a history of immunodeficiency, including a positive HIV test result, other acquired or congenital immunodeficiency diseases, or a history of organ transplantation; a history of severe autoimmune diseases deemed unsuitable for enrollment by the investigator; or requiring immunosuppressive therapy for allogeneic organ transplantation.
9. Having severe infections (requiring intravenous antibiotics, antifungals, or antivirals according to clinical practice guidelines), active hepatitis A, active hepatitis B (HBV DNA ≥2000 IU/mL or 10^4 copies/mL; prophylactic antiviral therapy other than interferon is allowed), active hepatitis C (anti-HCV positive and HCV-RNA above the lower limit of detection), or active syphilis infection.
10. Having uncontrolled third-space fluid accumulations (such as significant pleural effusion, ascites or pericardial effusion) deemed unsuitable for enrollment by the investigator.
11. Having a clear history of neurological or psychiatric disorders, including epilepsy or dementia.
12. Other reasons considered by the investigator to make the participant unsuitable for participation in this clinical study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 177Lu-PSMA-VG01 Injection; Successfully screened participants will be treated with 177Lu-PSMA-VG01 Injection during the treatment period .	Drug: 177Lu-PSMA-VG01; Treatment patients

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Radiation dosimetry	Standard uptake value (SUV), organ accumulation (%ID), absorbed dose (AD), and effective dose (ED) in tumors and target organs	Up to 36 weeks
Dose-Limiting Toxicities (DLT)	Evaluating the safety and tolerability of the 177Lu-PSMA-VG01 injection in participants.	Up to 6 weeks
Maximum Tolerate dose（MTD）	Evaluating the safety and tolerability of the 177Lu-PSMA-VG01 injection in participants.	Up to 6 weeks
AE	Evaluating the safety and tolerability of the 177Lu-PSMA-VG01 injection in participants. All Adverse Events (AEs) occurring during the clinical study period will be monitored.	Up to 36 weeks
Accumulation (%ID)	Evaluation of drug biodistribution in major human organs.	Up to 36 weeks
Area under the plasma concentration-time curve from time zero to the last measurable concentration（AUC₀-last）	Pharmacokinetics (PK) of 177Lu-PSMA-VG01 in plasma	Up to 8 days.
Area under the plasma concentration-time curve from time zero extrapolated to infinite time (AUC0-inf)	Pharmacokinetics (PK) of 177Lu-PSMA-VG01 in plasma	Up to 8 days .
Maximum plasma concentration (Cmax)	Pharmacokinetics (PK) of 177Lu-PSMA-VG01 in plasma	Up to 8 days .

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Objective Response Rate (ORR)		Up to 2 years after completing the End-of-Treatment visit.
radiographic Progression-Free Survival (rPFS)		Up to 2 years after completing the End-of-Treatment visit.
PSA response rate	PSA50 response rate and PSA90 response rate	From baseline to 36 weeks

Collaborators and Investigators

• Sponsor: VitsGen Therapeutics Inc.

Study record dates

Study Major Dates

• Study Start (Estimated): June 16, 2026
• Primary Completion (Estimated): May 6, 2027
• Study Completion (Estimated): May 6, 2029

Study Registration Dates

• First Submitted: May 7, 2026
• First Submitted That Met QC Criteria: June 15, 2026
• First Posted (Actual): June 22, 2026

Study Record Updates

• Last Update Posted (Actual): June 22, 2026
• Last Update Submitted That Met QC Criteria: June 15, 2026
• Last Verified: June 1, 2026

More Information

Terms related to this study

• Other Study ID Numbers: 2026-078R

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No