Safety and Tolerability Study of 68Ga/177Lu-BRP-020063 in Advanced Solid Tumors

A Study Evaluating the Safety, Pharmacokinetics, and Radiation Dosimetry of 68Ga/177Lu-BRP-020063 in Patients With Advanced Metastatic Solid Tumors.

This study is an open-label, single-arm, interventional clinical trial designed to investigate the safety of ⁶⁸Ga/¹⁷⁷Lu-BRP-020063 in patients with advanced metastatic solid tumors; to evaluate the pharmacokinetics, biodistribution, and radiation dosimetry of ¹⁷⁷Lu-BRP-020063 in patients with metastatic solid tumors; and to preliminarily explore its therapeutic efficacy. The study plans to enroll 10 patients to receive ⁶⁸Ga-BRP-020063 PET/CT imaging, among whom 5 patients positive for ⁶⁸Ga-BRP-020063 will be selected to receive a low dose of ¹⁷⁷Lu-BRP-020063. The results of this study will provide a basis for the design of subsequent studies involving higher doses of ¹⁷⁷Lu-BRP-020063.

Study Overview

• Status: Not yet recruiting
• Conditions: Urothelial Carcinoma (UC)
• Intervention / Treatment: Drug: ⁶⁸Ga/¹⁷⁷Lu-BRP-020063

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

Contacts and Locations

• Study Contact: Name: Yan Xing, Dr.; Phone Number: +862163246311; Email: xy.1@163.com

Participation Criteria

Eligibility Criteria

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

Description

Inclusion Criteria:

1. Age ≥ 18 years, regardless of gender;
2. Patients with a confirmed diagnosis of advanced metastatic solid tumor (preferably urothelial carcinoma, followed by breast cancer);
3. Willing to provide archived or freshly biopsied tumor tissue specimens (recommended within the past 2 years);
4. Performance status (ECOG) score of 0-1;

5. Adequate organ function:

   • Complete Blood Count: White blood cell count ≥ 3.0 × 10⁹/L, neutrophil count ≥ 1.5 × 10⁹/L, hemoglobin ≥ 90 g/L, platelet count ≥ 75 × 10⁹/L;
   • Liver function: Total bilirubin ≤ 2.5 × ULN, alanine aminotransferase ≤ 3 × ULN, aspartate aminotransferase ≤ 3 × ULN;
   • Renal function: Creatinine clearance ≥ 50 mL/min (Cockcroft-Gault formula);
   • Coagulation function: Prothrombin time ≤ 1.5 × ULN, activated partial thromboplastin time ≤ 1.5 × ULN, international normalized ratio ≤ 1.5 × ULN;
6. Subjects of childbearing potential must voluntarily adopt effective contraception during the treatment period and for 6 months after the last dose of the investigational drug (for females);
7. Willing to participate in this trial and sign an informed consent form.

Exclusion Criteria:

1. Previous treatment with Nectin-4-targeted drugs (including clinical trials);
2. Inability to complete PET/CT or SPECT/CT examinations (including inability to lie flat, claustrophobia, radiophobia, etc.);
3. Participation in drug or device clinical studies within 4 weeks prior to the first dose;

4. Presence of severe or uncontrolled underlying diseases, including but not limited to:

   1. NYHA Class II or higher congestive heart failure, or severe arrhythmia requiring medication;
   2. Severe cardiovascular/cerebrovascular or valvular diseases;
   3. Poorly controlled diabetes or hypertension;
5. Inability to tolerate intravenous administration or difficulty with venipuncture (e.g., history of needle or blood phobia);
6. Active infection within 4 weeks prior to the first dose;
7. Women who are planning pregnancy, currently pregnant, or breastfeeding;
8. Allergy to radioactive rays or other severe allergic history;
9. History of neurological metastasis with associated symptoms;
10. Concurrent other malignancies;
11. Undergone general anesthesia surgery within 4 weeks prior to the first dose;
12. Other conditions deemed by the investigator as unsuitable for inclusion in the 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: ⁶⁸Ga/¹⁷⁷Lu-BRP-020063 Treatment Arm

Drug: ⁶⁸Ga/¹⁷⁷Lu-BRP-020063; 68Ga-BRP-020063 Injection (Diagnostic Phase): All subjects will receive a single administration of 68Ga-BRP-020063 injection. The dose of 5 mCi (185 MBq), within an acceptable range of 3-7 mCi (111-259 MBq), will be delivered via rapid consecutive intravenous bolus injection in a volume not exceeding 10 mL, followed by a saline flush. 177Lu-BRP-020063 Injection (Therapeutic Phase): Five subjects who show positive results on the 68Ga-BRP-020063 PET/CT scan will be selected to receive a single administration of 177Lu-BRP-020063 injection. A dose of 40 mCi (1.48 GBq), within an acceptable range of 30-50 mCi (1.11-1.85 GBq), will be administered via intravenous infusion over approximately 20 minutes using an infusion pump, followed by a saline flush.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Adeverse Events	From enrolment to 4 weeks after the first dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
PK Parameters	AUC(0-∞)	From administration up to 168 hours post-dose
Biodistribution	Perform whole-body SPECT/CT to determine radioactivity (%ID) in major organs over time for biodistribution assessment.	From administration up to 168 hours post-dose
Radiation Dosimetry		from administration up to 168 hours post-dose

Other Outcome Measures

Outcome Measure	Time Frame
ORR	be assessed at 6-week or 8-week intervals from the start of treatment until disease progression to up to 1 year.
DCR	be assessed at 6-week or 8-week intervals from the start of treatment until disease progression to up to 1 year.

Collaborators and Investigators

• Sponsor: Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine

Study record dates

Study Major Dates

• Study Start (Estimated): March 2, 2026
• Primary Completion (Estimated): August 31, 2026
• Study Completion (Estimated): August 31, 2026

Study Registration Dates

• First Submitted: February 11, 2026
• First Submitted That Met QC Criteria: February 23, 2026
• First Posted (Actual): February 27, 2026

Study Record Updates

• Last Update Posted (Actual): February 27, 2026
• Last Update Submitted That Met QC Criteria: February 23, 2026
• Last Verified: February 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Neoplasms; Neoplasms by Histologic Type; Neoplasms, Glandular and Epithelial; Carcinoma; Carcinoma, Transitional Cell
• Other Study ID Numbers: IIT-2026-030

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