Safety, Tolerability and Preliminary Efficacy of 161Tb-LNC1011 (PSMA Radioligand) in Patients With Metastatic Castration-Resistant Prostate Cancer (mCRPC)

NCT07381582 | Not Yet Recruiting Early Phase 1 DMC

• 1 other identifier: PUMCH-MCH-161Tb-LNC1011
• Study Type: interventional
• Target: 15
• Locations: 1 country
• Sites: 2

Brief Summary

This is a prospective, open-label, single-center, dose-escalation study using a standard 3+3 design to assess the safety, tolerability, biodistribution/dosimetry and preliminary efficacy of the albumin-binding PSMA radioligand 161Tb-LNC1011 in patients with metastatic castration-resistant prostate cancer (mCRPC). Patients will receive intravenous 161Tb-LNC1011 starting at 50 mCi with planned dose-level escalations to 80, 130 and 200 mCi (±10%). Early dose levels (50 mCi) receive 1 cycle; later levels receive up to 4 cycles every 6 weeks based on safety and disease status. Primary endpoints include dose-limiting toxicities (DLTs), adverse events (AEs) graded by CTCAE v5.0, and determination of maximum tolerated dose (MTD). Secondary endpoints include organ/tumor absorbed doses, PSA responses (PSA50/PSA90), disease control, time to PSA progression and radiographic progression-free survival per PCWG3.

Conditions

Prostate Cancer

Keywords

Terbium-161; PSMA; Radionuclide therapy; Metastatic castration-resistant prostate cancer

Outcome Measures

Primary Outcomes (3)

• Incidence of Dose-Limiting Toxicities (DLTs)

  Proportion of participants with DLTs per CTCAE v5.0 during the DLT window.

  First 6 weeks after each initial dose at a given dose level

• Maximum Tolerated Dose (MTD)

  Highest dose level at which ≤1/6 participants experience a DLT.

  At completion of dose escalation (approximately 12-18 months after study start)

• Treatment-Emergent Adverse Events (TEAEs)

  Number and grade of AEs/SAEs per CTCAE v5.0.

  From first dose through 28 days after last dose (extended if related)

Secondary Outcomes (2)

• Organ and Tumor Absorbed Doses (Dosimetry)

  Within first cycle (Day 0 to Day 7 imaging)

• PSA50 and PSA90 Response Rates

  Every 6 weeks during treatment and at end of treatment (up to approximately 24 weeks)

Study Arms (1)

Dose-Escalation Cohort (3+3): 161Tb-LNC1011

EXPERIMENTAL

Single-group, open-label, sequential dose escalation of 161Tb-LNC1011 (IV). Planned dose levels: 50, 80, 130, 200 mCi (±10%). At 50 mCi: 1 cycle; higher levels: up to 4 cycles every 6 weeks, contingent on safety and disease status. DLT window: 6 weeks post-dose; MTD per standard 3+3 rules (≥2/6 DLTs defines exceeding dose). Retreatment requires hematologic recovery to CTCAE ≤ Grade 1 or baseline. Post-dose SPECT/CT at \~30 min, 2 h, 8 h, 24 h, Day 2, Day 7 for dosimetry; disease assessments with 68Ga-PSMA-11 PET/CT and labs per schedule.

Drug: 161Tb-LNC1011

Interventions

161Tb-LNC1011 DRUG

Intravenous administration; planned dose levels: 50, 80, 130, 200 mCi (±10%); cycle interval q6 weeks; up to 1 cycle at 50 mCi and up to 4 cycles at later dose levels as permitted by safety and disease status.

Dose-Escalation Cohort (3+3): 161Tb-LNC1011

Eligibility Criteria

• Age: 18 Years+
• Sex: male
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male, ≥18 years.
• Pathologically confirmed mCRPC per PCWG3.
• Ga-PSMA-11 PET/CT positive.
• Prior exposure to at least one novel androgen-axis drug (e.g., enzalutamide and/or abiraterone) or at least one taxane regimen, or intolerance/refusal to taxane chemotherapy.
• ECOG 0-2; life expectancy ≥6 months.
• Adequate organ function: ALT/AST ≤3× ULN; BUN/Cr ≤1.5× ULN; WBC ≥3.5×10\^9/L; PLT ≥100×10\^9/L; Hb ≥90 g/L.
• Signed informed consent and willingness to comply with study procedures.

You may not qualify if:

• Major trauma/surgery within 4 weeks prior to study treatment.
• Active severe systemic or localized infection or other serious comorbidity.
• Immunodeficiency or recent use of immunosuppressants/immunoenhancers, recent vaccines.
• Autoimmune diseases (e.g., rheumatoid arthritis) requiring active management.
• Uncontrolled arrhythmias (incl. Afib), heart failure NYHA \> II, uncontrolled hypertension.
• Known allergy to components of investigational product.
• Positive syphilis, HBV/HCV/HIV.
• Inadequate contraception in patients of reproductive potential.
• Psychiatric illness compromising compliance.
• Unable to undergo SPECT/CT or to retain urine for 30 minutes.
• Any condition deemed unsuitable by the investigator.

Sponsors & Collaborators

• Mianyang Central Hospital: collaborator
• Peking Union Medical College Hospital: lead

Study Sites (2)

Peking Union Medical College Hospital

Beijing, Beijing Municipality, 100730, China

Location

Mianyang Central Hospital

Mianyang, Sichuan, China

Location

MeSH Terms

Conditions

Prostatic Neoplasms

Condition Hierarchy (Ancestors)

Genital Neoplasms, Male; Urogenital Neoplasms; Neoplasms by Site; Neoplasms; Genital Diseases, Male; Genital Diseases; Urogenital Diseases; Prostatic Diseases; Male Urogenital Diseases

Central Study Contacts

Zhaohui Zhu, MD

CONTACT

86-13611093752; 13611093752@163.com

Zhengguo Chen, MD

CONTACT

86-13908119175

Study Design

• Study Type: interventional
• Phase: early phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Model Details: Intravenous administration; planned dose levels: 50, 80, 130, 200 mCi (±10%); cycle interval q6 weeks; up to 1 cycle at 50 mCi and up to 4 cycles at later dose levels as permitted by safety and disease status.

Study Record Dates

• First Submitted: November 23, 2025
• First Posted: February 2, 2026
• Study Start: January 1, 2026
• Primary Completion (Estimated): October 31, 2027
• Study Completion (Estimated): December 31, 2027
• Last Updated: February 2, 2026

Record last verified: 2025-11

Locations

CN (2)