Study Evaluating mCRPC Treatment Using PSMA [Lu-177]-PNT2002 Therapy After Second-line Hormonal Treatment

NCT ID: NCT04647526

Last Updated: 2026-01-13

Study Results

Results available

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Basic Information

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Recruitment Status

ACTIVE_NOT_RECRUITING

Clinical Phase

PHASE3

Total Enrollment

455 participants

Study Classification

INTERVENTIONAL

Study Start Date

2021-02-25

Study Completion Date

2028-03-31

Brief Summary

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The purpose of this study is to evaluate the efficacy and safety of \[Lu-177\]-PNT2002 in patients with metastatic castration-resistant prostate cancer who have progressed following treatment with androgen receptor axis-targeted therapy (ARAT).

Detailed Description

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The primary objective of the study is to determine the efficacy of \[Lu-177\]-PNT2002 (\[Lu-177\]-PSMA-I\&T) versus abiraterone or enzalutamide in delaying radiographic progression in patients with mCRPC.

The study consists of 3 phases: Dosimetry, Randomized Treatment, and Long term Follow up.

The study will commence with a 25-patient safety and dosimetry lead-in (Part 1) and proceed to a randomization treatment phase in approximately 390 patients (Part 2). Patients in Part 2 will be randomized in a 2:1 ratio to receive either \[Lu-177\]-PNT2002 (Arm A), or enzalutamide or abiraterone (Arm B). Patients in Arm B who experience radiographic progression per central review and meet protocol defined eligibility, may crossover to receive \[Lu-177\]-PNT2002. After final overall survival (OS) analysis, all patients will continue to be followed through Continued Access, including long-term follow-up (LTFU) for at least 5 years from the first therapeutic dose, death, or loss to follow up (Part 3).

Only patients that meet PSMA PET avidity criteria per central review will be eligible for this study.

Conditions

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Metastatic Castration-Resistant Prostate Cancer

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Lead-in Dosimetry Phase: [Lu-177]-PNT2002

Participants received 6.8 gigabecquerels (GBq) (±10%) of \[Lu-177\]-PNT2002 by intravenous infusion every 8 weeks for 4 cycles.

Group Type EXPERIMENTAL

[Lu-177]-PNT2002

Intervention Type DRUG

Participants randomized to Arm A will receive 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 every 8 weeks for 4 cycles

Randomization Phase: [Lu-177]-PNT2002 (Arm A)

Participants received 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 by intravenous infusion every 8 weeks for 4 cycles.

Group Type EXPERIMENTAL

[Lu-177]-PNT2002

Intervention Type DRUG

Participants randomized to Arm A will receive 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 every 8 weeks for 4 cycles

Randomization Phase: Abiraterone or Enzalutamide (Arm B)

Participants received either of below treatments until radiographic progression.

* Enzalutamide 160 milligram (mg) orally once daily (or)
* Abiraterone 1000 mg orally once daily coadministered with prednisone 5 mg orally twice daily or dexamethasone 0.5 mg orally once daily.

Participants who experienced radiographic progression per Blinded Independent Central Review (BICR) (or after final overall survival (OS), per local investigator-assessment), had not started an intervening treatment, and had no uncontrolled adverse events (AEs) were eligible to consent to cross over to receive 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 intravenous infusion every 8 weeks for 4 cycles.

Group Type ACTIVE_COMPARATOR

[Lu-177]-PNT2002

Intervention Type DRUG

Participants randomized to Arm A will receive 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 every 8 weeks for 4 cycles

Abiraterone

Intervention Type DRUG

Abiraterone (1000 mg orally once daily with: 5 mg twice daily prednisone or 0.5 mg once daily dexamethasone)

Enzalutamide

Intervention Type DRUG

Enzalutamide (160 mg orally once daily)

Pharmacokinetic (PK) Extension Phase: [Lu-177]-PNT2002

Participants received 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 by intravenous infusion every 8 weeks for 4 cycles.

Group Type EXPERIMENTAL

[Lu-177]-PNT2002

Intervention Type DRUG

Participants randomized to Arm A will receive 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 every 8 weeks for 4 cycles

Interventions

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[Lu-177]-PNT2002

Participants randomized to Arm A will receive 6.8 GBq (±10%) of \[Lu-177\]-PNT2002 every 8 weeks for 4 cycles

Intervention Type DRUG

Abiraterone

Abiraterone (1000 mg orally once daily with: 5 mg twice daily prednisone or 0.5 mg once daily dexamethasone)

Intervention Type DRUG

Enzalutamide

Enzalutamide (160 mg orally once daily)

Intervention Type DRUG

Other Intervention Names

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[Lu-177]-PSMA-I&T LY4187525

Eligibility Criteria

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Inclusion Criteria

1. Male aged 18 years or older.
2. Histological, pathological, and/or cytological confirmation of adenocarcinoma of the prostate.
3. Ineligible or averse to chemotherapeutic treatment options.
4. Patients must have progressive mCRPC at the time of consent based on at least 1 of the following criteria:

1. Serum/plasma PSA progression defined as increase in PSA greater than 25% and \>2 ng/mL above nadir, confirmed by progression at 2 time points at least 3 weeks apart.
2. Soft-tissue progression defined as an increase ≥20% in the sum of the diameter (SOD) (short axis for nodal lesions and long axis for non-nodal lesions) of all target lesions based on the smallest SOD since treatment started or the appearance of one or a new lesion.
3. Progression of bone disease defined as the appearance of two or more new lesions by bone scan.
5. Progression on previous treatment with one ARAT (abiraterone or enzalutamide or darolutamide or apalutamide) in either the CSPC or CRPC setting.
6. PSMA-PET scan (i.e., 68Ga-PSMA-11 or 18F-DCFPyL) positive as determined by the sponsor's central reader.
7. Castrate circulating testosterone levels (\<1.7 nmol/L or \<50 ng/dL).
8. Adequate organ function, independent of transfusion:

1. Bone marrow reserve:

* i. White blood cell (WBC) count ≥2.5 × 10\^9/L OR absolute neutrophil count (ANC) ≥1.5 × 10\^9/L.
* ii. Platelets ≥100 × 10\^9/L.
* iii. Hemoglobin ≥8 mmol/L.
2. Liver function:

* i. Total bilirubin ≤1.5 × institutional upper limit of normal (ULN). For patients with known Gilbert's syndrome, ≤3 × ULN is permitted.
* ii. ALT or AST ≤3.0× ULN.
3. Renal function:

* i. Serum/plasma creatinine ≤1.5 × ULN or creatinine clearance ≥50 mL/min based on Cockcroft-Gault formula (for patients in France, serum/plasma creatinine ≤1.5 × ULN or CrCl ≥60 mL/min based on Cockcroft-Gault formula).
4. Albumin ≥30 g/L.
9. Human immunodeficiency virus-infected patients who are healthy and have a low risk of acquired immunodeficiency syndrome-related outcomes are included in this trial.
10. For patients who have partners who are pregnant or of childbearing potential: a condom is required along with a highly effective contraceptive method during the study and for 6 months after last study drug administration. Such methods deemed highly effective include a) combined (estrogen and progestogen containing) hormonal contraception associated with inhibition of ovulation, b) progestogen-only hormonal contraception associated with inhibition of ovulation, c) intrauterine device (IUD), d) intrauterine hormone-releasing system (IUS), e) bilateral tubal occlusion, f) vasectomy, g) true sexual abstinence: when this is in line with the preferred and usual lifestyle of the subject \[periodic abstinence (e.g., calendar, ovulation, symptothermal, post-ovulation methods), declaration of abstinence for the duration of exposure to IMP, and withdrawal are not acceptable methods of abstinence\].
11. Willing to initiate ARAT therapy (either enzalutamide or abiraterone), pre-specified by investigator, if randomized to Treatment Arm B.
12. ECOG performance status 0 to 1.
13. Willing and able to comply with all study requirements and treatments (including 177Lu PNT2002) as well as the timing and nature of required assessments.
14. Signed informed consent.

Exclusion Criteria

Patients are excluded from the study if any of the following criteria apply:

1. If noted in pathology report, prostate cancer with known significant (\>10% present in cells) sarcomatoid or spindle cell or neuroendocrine components. Any small cell component in the cancer should result in exclusion.
2. Prior treatment for prostate cancer ≤28 days prior to randomization, with the exclusion of first-line local external beam, ARAT, luteinizing hormone-releasing hormone (LHRH) therapy, or non-radioactive bone-targeted agents.
3. Any prior cytotoxic chemotherapy for CRPC (e.g., cabazitaxel or docetaxel); chemotherapy for hormone-sensitive prostate cancer (HSPC) is allowed if the last dose was administered \>1 year prior to consent.
4. Prior treatment with systemic radionuclides (e.g. radium-223, rhenium-186, strontium 89).
5. Prior immuno-therapy, except for sipuleucel-T.
6. Prior PSMA-targeted radioligand therapy, e.g., Lu-177-PSMA-617, I 131-1095.
7. Prior poly ADP ribose polymerase (PARP) inhibitor for prostate cancer.
8. Patients who progressed on 2 or more lines of ARATs.
9. Patients receiving bone-targeted therapy (e.g. denosumab, zoledronic acid) not on stable doses for at least 4 weeks prior to randomization.
10. Administration of an investigational agent ≤60 days or 5 half-lives, whichever is shorter, prior to randomization.
11. Major surgery ≤30 days prior to randomization.
12. Estimated life expectancy \<6 months as assessed by the principal investigator.
13. Presence of liver metastases \>1 cm on abdominal imaging.
14. A superscan on bone scan defined as a bone scan that demonstrates markedly increased skeletal radioisotope uptake relative to soft tissues in association with absent or faint genitourinary tract activity.
15. Dose escalation or initiation of opioids for cancer-related pain ≤30 days prior to consent up to and including randomization.
16. Known presence of central nervous system metastases.
17. Contraindications to the use of planned ARAT therapy, \[Ga-68\]-PSMA-11, \[F-18\]-DCFPyL or \[Lu-177\]-PNT2002 therapy, including but not limited to the following:

* Hypersensitivity to \[Ga-68\]-PSMA-11, \[F-18\]-DCFPyL or \[Lu-177\]-PNT2002 excipients (Diethylenetriaminepentaacetic acid (DTPA), Sodium ascorbate, Lascorbic acid, Sodium gentisate, HCl, Sodium hydroxide).
* Recent myocardial infarction or arterial thrombotic events (in the past 6 months) or unstable angina (in the past 3 months), bradycardia or left ventricular ejection fraction measurement of \< 50%.
* History of seizures in patients planned to receive enzalutamide.
18. Active malignancy other than low-grade non-muscle-invasive bladder cancer and non-melanoma skin cancer.
19. Concurrent illness that may jeopardize the patient's ability to undergo study procedures.
20. Serious psychological, familial, sociological, or geographical condition that might hamper compliance with the study protocol and follow-up schedule. Patients that travel need to be capable of repeated visits even if they are on the control arm.
21. Symptomatic cord compression, or clinical or radiologic findings indicative of impending cord compression.
22. Concurrent serious (as determined by the investigator) medical conditions, including, but not limited to, New York Heart Association class III or IV congestive heart failure (see 12.1 Appendix 1), unstable ischemia, uncontrolled symptomatic arrhythmia, history of congenital prolonged QT syndrome, uncontrolled infection, known active hepatitis B or C, or other significant co-morbid conditions that in the opinion of the investigator would impair study participation or cooperation.
Minimum Eligible Age

18 Years

Eligible Sex

MALE

Accepts Healthy Volunteers

No

Sponsors

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POINT Biopharma, a wholly owned subsidiary of Eli Lilly and Company

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Jessica Jensen

Role: STUDY_DIRECTOR

Eli Lilly and Company

Locations

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Arizona Institute of Urology (AIU) - Tucson

Tucson, Arizona, United States

Site Status

Cedars-Sinai Medical Center, Samuel Oschin Comprehensive Cancer Institute

Los Angeles, California, United States

Site Status

VA Greater Los Angeles Healthcare System

Los Angeles, California, United States

Site Status

University of California Los Angeles, Nuclear Medicine Clinic

Los Angeles, California, United States

Site Status

Hoag Memorial Hospital Presbyterian

Newport Beach, California, United States

Site Status

UC Irvine Chao Family Comprehensive Cancer Center

Orange, California, United States

Site Status

Stanford Cancer Institute

Palo Alto, California, United States

Site Status

University of Colorado Hospital

Aurora, Colorado, United States

Site Status

H. Lee Moffitt Cancer Center & Research Institute

Tampa, Florida, United States

Site Status

University of Iowa Hospitals and Clinics

Iowa City, Iowa, United States

Site Status

University of Kentucky Chandler Medical Center

Lexington, Kentucky, United States

Site Status

Tulane University Medical Center

New Orleans, Louisiana, United States

Site Status

University of Maryland Greenebaum Cancer Center

Baltimore, Maryland, United States

Site Status

Chesapeake Urology Associates (CUA) P.A.

Towson, Maryland, United States

Site Status

University of Michigan Hospitals

Ann Arbor, Michigan, United States

Site Status

Karmanos Cancer Center

Detroit, Michigan, United States

Site Status

VA St. Louis Health Care System

St Louis, Missouri, United States

Site Status

Saint Louis University Hospital

St Louis, Missouri, United States

Site Status

Washington University School of Medicine

St Louis, Missouri, United States

Site Status

Urology Cancer Center, PC

Omaha, Nebraska, United States

Site Status

Astera Cancer Care

East Brunswick, New Jersey, United States

Site Status

New Mexico Oncology Hematology Consultants Ltd., New Mexico Cancer Center

Albuquerque, New Mexico, United States

Site Status

New York Presbyterian Hospital/Weill Cornell Medical Center

New York, New York, United States

Site Status

Tri-State Urologic Services

Cincinnati, Ohio, United States

Site Status

Greater Dayton Cancer Center

Kettering, Ohio, United States

Site Status

Perelman Center for Advanced Medicine

Philadelphia, Pennsylvania, United States

Site Status

Fox Chase Cancer Center

Philadelphia, Pennsylvania, United States

Site Status

Carolina Urologic Research Center

Myrtle Beach, South Carolina, United States

Site Status

Vanderbilt-Ingram Cancer Center

Nashville, Tennessee, United States

Site Status

Dallas VA Medical Center, Nuclear Medicine Service

Dallas, Texas, United States

Site Status

UT Southwestern Medical Center

Dallas, Texas, United States

Site Status

Excel Diagnostics & Nuclear Oncology Center

Houston, Texas, United States

Site Status

Swedish Cancer Institute Research

Seattle, Washington, United States

Site Status

BC Cancer - Vancouver

Vancouver, British Columbia, Canada

Site Status

Nova Scotia Health Authority

Halifax, Nova Scotia, Canada

Site Status

London Health Sciences Center - Victoria Hospital

London, Ontario, Canada

Site Status

Sunnybrook Research Institute, Odette Cancer Center

Toronto, Ontario, Canada

Site Status

Princess Margaret Cancer Centre

Toronto, Ontario, Canada

Site Status

CHUM - University Hospital of Montreal

Montreal, Quebec, Canada

Site Status

Jewish General Hospital

Montreal, Quebec, Canada

Site Status

CHU of Quebec - Laval University

Québec, Quebec, Canada

Site Status

Center Jean Perrin, Department of Medical Oncology

Clermont-Ferrand, , France

Site Status

Claude Huriez Hospital

Lille, , France

Site Status

Leon Berard Center

Lyon, , France

Site Status

La Timone Hospital, Nuclear Medicine Department

Marseille, , France

Site Status

Montpellier Cancer Institute, Department of Nuclear Medicine

Montpellier, , France

Site Status

Tenon Hospital, Department of Medical Oncology

Paris, , France

Site Status

St. Antonius Hospital

Nieuwegein, , Netherlands

Site Status

Radboud University Medical Center (Radboudumc)

Nijmegen, , Netherlands

Site Status

Erasmus University Medical Center Rotterdam

Rotterdam, , Netherlands

Site Status

Sahlgrenska University Hospital

Gothenburg, , Sweden

Site Status

Norrlands University Hospital, Department of Radiation Sciences, Oncology

Umeå, , Sweden

Site Status

Charing Cross Hospital, Department of Medical Oncology

London, , United Kingdom

Site Status

Royal Marsden NHS Foundation Trust - Institute of Cancer Research

Sutton, , United Kingdom

Site Status

Countries

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United States Canada France Netherlands Sweden United Kingdom

References

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Baum RP, Kulkarni HR, Schuchardt C, Singh A, Wirtz M, Wiessalla S, Schottelius M, Mueller D, Klette I, Wester HJ. 177Lu-Labeled Prostate-Specific Membrane Antigen Radioligand Therapy of Metastatic Castration-Resistant Prostate Cancer: Safety and Efficacy. J Nucl Med. 2016 Jul;57(7):1006-13. doi: 10.2967/jnumed.115.168443. Epub 2016 Jan 21.

Reference Type BACKGROUND
PMID: 26795286 (View on PubMed)

Hansen AR, Probst S, Beauregard JM, Viglianti BL, Michalski JM, Tagawa ST, Sartor O, Tutrone RF, Oz OK, Courtney KD, Delpassand ES, Nordquist LT, Osman MM, Chi KN, Sparks R, George N, Hawley SM, Wu W, Jensen JD, Fleshner NE. Initial clinical experience with [177Lu]Lu-PNT2002 radioligand therapy in metastatic castration-resistant prostate cancer: dosimetry, safety, and efficacy from the lead-in cohort of the SPLASH trial. Front Oncol. 2025 Jan 7;14:1483953. doi: 10.3389/fonc.2024.1483953. eCollection 2024.

Reference Type DERIVED
PMID: 39839782 (View on PubMed)

American College of Nuclear Medicine (ACNM) 2022 ACNM Annual Meeting AbstractsJanuary 27-29, 2022 Virtual Meeting. Clin Nucl Med. 2023 Feb 3:e246-e277. doi: 10.1097/RLU.0000000000004535. Online ahead of print. No abstract available.

Reference Type DERIVED
PMID: 36735603 (View on PubMed)

Provided Documents

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Document Type: Study Protocol

View Document

Document Type: Statistical Analysis Plan

View Document

Related Links

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https://cslide.ctimeetingtech.com/esmo2022/attendee/confcal_2/presentation/list?q=1400P

1400P - Efficacy and safety of 177Lu-PNT2002 prostate-specific membrane antigen (PSMA) therapy in metastatic castration resistant prostate cancer (mCRPC): Initial results from SPLASH

Other Identifiers

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J5T-OX-JXCA

Identifier Type: OTHER

Identifier Source: secondary_id

PBP-301

Identifier Type: OTHER

Identifier Source: secondary_id

2021-002641-15

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

2024-515604-39-00

Identifier Type: CTIS

Identifier Source: secondary_id

27232

Identifier Type: -

Identifier Source: org_study_id

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