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

Official title

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

Overview

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.

Interventions

• 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 ad

Primary outcome measures

• Adeverse Events [Time frame: From enrolment to 4 weeks after the first dose]

Secondary outcome measures (3)

• PK Parameters [Time frame: From administration up to 168 hours post-dose]
• Biodistribution [Time frame: From administration up to 168 hours post-dose]
• Radiation Dosimetry [Time frame: from administration up to 168 hours post-dose]

Eligibility criteria

Inclusion criteria

• Age ≥ 18 years, regardless of gender;
• Patients with a confirmed diagnosis of advanced metastatic solid tumor (preferably urothelial carcinoma, followed by breast cancer);
• Willing to provide archived or freshly biopsied tumor tissue specimens (recommended within the past 2 years);
• Performance status (ECOG) score of 0-1;
• 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;
• 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);
• Willing to participate in this trial and sign an informed consent form.

Exclusion criteria

• Previous treatment with Nectin-4-targeted drugs (including clinical trials);
• Inability to complete PET/CT or SPECT/CT examinations (including inability to lie flat, claustrophobia, radiophobia, etc.);
• Participation in drug or device clinical studies within 4 weeks prior to the first dose;
• Presence of severe or uncontrolled underlying diseases, including but not limited to:

• NYHA Class II or higher congestive heart failure, or severe arrhythmia requiring medication;
• Severe cardiovascular/cerebrovascular or valvular diseases;
• Poorly controlled diabetes or hypertension;
• Inability to tolerate intravenous administration or difficulty with venipuncture (e.g., history of needle or blood phobia);
• Active infection within 4 weeks prior to the first dose;
• Women who are planning pregnancy, currently pregnant, or breastfeeding;
• Allergy to radioactive rays or other severe allergic history;
• History of neurological metastasis with associated symptoms;
• Concurrent other malignancies;
• Undergone general anesthesia surgery within 4 weeks prior to the first dose;
• Other conditions deemed by the investigator as unsuitable for inclusion in the clinical study.

Criteria are shown verbatim from the registry (in English). Final eligibility is always assessed by the study center.

Healthy volunteers: No

Study design

Allocation

N/A

Model

Single group

Masking

Open label

Primary purpose

Treatment

Study locations

China · 1 center

• Shanghai General Hospital — Shanghai

Identifiers

NCT: NCT07439120 · IIT-2026-030

Primary sources (government registries)

• ClinicalTrials.gov (US NIH)

View this study on ClinicalTrials.gov ↗