First-in-human Study of 225Ac-PSMA-Trillium (BAY 3563254) in Participants With Advanced Metastatic Castration-resistant Prostate Cancer (mCRPC)

NCT ID: NCT06217822

Last Updated: 2026-01-05

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

RECRUITING

Clinical Phase

PHASE1

Total Enrollment

235 participants

Study Classification

INTERVENTIONAL

Study Start Date

2024-03-07

Study Completion Date

2031-05-24

Brief Summary

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Researchers are looking for a better way to treat participants who have metastatic castration-resistant prostate cancer (mCRPC).

mCRPC is a cancer of the prostate (male reproductive gland found below the bladder) that has spread to other parts of the body. This type of prostate cancer does not respond to hormone treatment used to lower the level of testosterone, a male sex hormone, to prevent cancer from growing.

The study treatment 225Ac-PSMA-Trillium, also called BAY3563254, is under development to treat advanced metastatic castration-resistant prostate cancer. It works by binding to PSMA and giving off radiation that can damage cancer cells and stop them from growing.

The main purpose of this first-in-human study is to learn:

* How safe is BAY3563254 in participants.
* What is the recommended dose of BAY3563254 that is safe and works well that will be further tested in Part 2 of the study.
* How well does BAY3563254 work in participants.

To answer this, the researchers will look at:

* The number and severity of medical problems including serious medical problems that participants experience after taking BAY3563254
* The number of dose-limiting toxicities (DLT) at each dose level. A DLT is a medical problem caused by a drug that is too severe to continue the use of that specific dose.
* The number of participants whose cancer completely disappears (complete response) or reduces by at least 30% (partial response) after taking the treatment (also known as objective response rate (ORR))
* The number of participants who have a decrease in the levels of PSA\* by at least 50% in their blood (also known as PSA50). PSA is a protein made by the prostate gland. High levels of PSA may indicate the presence of prostate cancer.
* Participants' best response to treatment based on their PSA levels (also known as the best overall PSA response).

The study will have two parts. The first part, called dose escalation, is done to find the most appropriate dose of BAY3563254 for use in the second part of the study. For this, each participant will receive one of different increasing amounts of BAY3563254. They will take BAY3563254 as an injection into a vein. All participants in the second part of the study, called dose expansion, will receive the most appropriate dose of BAY3563254 that was identified from the first part of the study.

Participants in this study will take the study treatment once every 6 weeks, which is known as a treatment cycle. Each participant will have up to 4 of these treatment cycles, if the participant benefits from the treatment. Each participant will be in the study for approximately 6 years, including a screening phase of up to 30 days, 6 months of treatment depending on the participant's benefit, and a follow up phase of 60 months after the end of treatment.

In addition, substudies performed during both dose escalation and dose expansion parts of the study will evaluate:

* the clearance of radioactivity from the body over time
* the doses of radiation that are delivered to normal organs and tumors

During the study, the doctors and their study team will:

* take blood and urine samples
* check vital signs such as blood pressure, heart rate, and body temperature
* examine heart health using electrocardiogram (ECG)
* take tumor samples if required
* check if the participants' cancer has grown and/or spread using CT (computed tomography) or MRI (magnetic resonance imaging) and bone scan
* check the tumor status using PET (positron emission tomography)
* check the amount of radiation absorbed by tumors and normal organs using SPECT/CT (single-photon emission tomography and computed tomography scan)
* ask the participants questions about how they are feeling and what adverse events they are having.

An adverse event is any medical problem that a participant has during a study. Doctors keep track of all adverse events, irrespective if they think it is related or not to the study treatments. In addition, the participants will be asked to complete a questionnaire on quality of life at certain time points during the study.

The treatment period ends with a visit in 6-12 weeks after the last BAY3563254 dose. About 6-12 weeks after the last dose and every 6 weeks thereafter, the study doctors and their team will check the participants' health and any changes in their cancer. This active follow-up period ends after 18 months. The long-term follow-up period will start after the end of the active follow-up visit and will continue for up to 60 months after the the last BAY3563254 dose. Participants will be contacted, typically by phone call or clinic visit, approximately every 12 weeks after the end of active follow-up.

Detailed Description

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Conditions

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Advanced Metastatic Castration-resistant Prostate Cancer Prostate Specific Membrane Antigen (PSMA) Expression

Study Design

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Allocation Method

NON_RANDOMIZED

Intervention Model

SEQUENTIAL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Dose escalation of BAY3563254

Participants with advanced mCRPC will receive increased 225Ac-PSMA-Trillium doses in a planned stepwise fashion.

Group Type EXPERIMENTAL

225Ac-PSMA-Trillium (BAY3563254)

Intervention Type DRUG

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

Dose expansion group A of BAY3563254

Participants with advanced mCRPC treated with 225Ac-PSMA-Trillium, who must have received at least 1 but no more than 2 prior taxane-based chemotherapy regimens. Prior radiopharmaceutical treatment is not permitted.

Group Type EXPERIMENTAL

225Ac-PSMA-Trillium (BAY3563254)

Intervention Type DRUG

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

Dose expansion group B of BAY3563254

Participants with advanced mCRPC treated with 225Ac-PSMA-Trillium, who must not have received taxane-based chemotherapy since becoming castration resistant. Prior radiopharmaceutical treatment is not permitted.

Group Type EXPERIMENTAL

225Ac-PSMA-Trillium (BAY3563254)

Intervention Type DRUG

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

Dose expansion group C of BAY3563254

Participants with advanced mCRPC treated with 225Ac-PSMA-Trillium, who must have had prior treatment with 177Lu-PSMA more than 6 weeks before the start of study treatment and at least 1 but no more than 2 taxane regimens (or been deemed ineligible for or refused taxane therapy on consultation with their physician).

Group Type EXPERIMENTAL

225Ac-PSMA-Trillium (BAY3563254)

Intervention Type DRUG

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

225Ac-PSMA-Trillium Imaging and Dosimetry

The 225Ac-PSMA-Trillium Imaging and Dosimetry Substudy will enroll throughout both dose escalation and dose expansion, starting with the first dose level in dose escalation. The substudy will generally be available at all study sites to participants in the main study.

Group Type EXPERIMENTAL

225Ac-PSMA-Trillium (BAY3563254)

Intervention Type DRUG

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

HPGe or NaI Whole Body Radioactivity Measurement of 225Ac-PSMA-Trillium

HPGe or NaI measurements of whole-body radioactivity of 225Ac and its daughters as a function of time will be conducted on an optional basis during dose escalation and dose expansion at selected sites to evaluate the clearance of total radioactivity from the body over time. Participants in the 111In-PSMA-Trillium and Tris-POC Imaging Substudy will not be eligible for this HPGe or NaI Whole Body Radioactivity Measurement of 225Ac-PSMA-Trillium Substudy.

Group Type EXPERIMENTAL

225Ac-PSMA-Trillium (BAY3563254)

Intervention Type DRUG

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

Interventions

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225Ac-PSMA-Trillium (BAY3563254)

Intravenous slow injection on Day 1 of a 6 week treatment cycle.

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

* mCRPC with pathological confirmation of adenocarcinoma without small-cell or neuroendocrine features.
* Previous treatment with at least 1 novel androgen axis drug (NAAD) (e.g., enzalutamide, apalutamide, darolutamide and/or abiraterone).
* Prior orchiectomy and/or ongoing androgen deprivation therapy and a castrate level of serum testosterone (\<50 ng/dL or \<1.7 nmol/L).
* Prior taxane treatment:

* Dose Escalation: Participants must either have had prior treatment with at least 1 but no more than 2 taxane regimens, or been deemed ineligible for or refused taxane therapy on consultation with their physician
* Dose Expansion Group A: Participants must have had prior treatment with at least 1 but no more than 2 taxane regimens, in the castration-resistant setting
* Dose Expansion Group B: Participants must not have received any taxane regimens since becoming castration-resistant

* Dose Expansion Group C: Participants must either have had prior treatment with at least 1 but no more than 2 taxane regimens, or been deemed ineligible for or refused taxane therapy on consultation with their physician
* Prior treatment with an established Lu-PSMA therapy (i.e., dose activity and cycles comparable to approved treatments) is required for participants in Dose Expansion Group C only. More specifically, to qualify for this expansion group, participants must not have discontinued 177Lu-PSMA treatment due to intolerance.
* Eastern Cooperative Oncology Group performance status (ECOG PS) of 0 or 1.
* Adequate bone marrow, hepatic, and renal function, as assessed by the following laboratory requirements within 30 days before start of study intervention, as indicated below. Note that blood transfusions (red blood cells or platelets) and administration of G-CSF or GM-CSF are prohibited within 21 days prior to screening for the below bone marrow-related parameters.

* Hemoglobin ≥9.0 g/dL
* Absolute neutrophil count (ANC) ≥1500/mm\^3
* Platelet count ≥100,000/mm\^3
* Total bilirubin ≤1.5 x the Upper limit of normal (ULN), or ≤3×ULN if the participant has a confirmed history of Gilbert's syndrome (note that participants with Gilbert's syndrome should be carefully evaluated for other liver-related disorders that may impact their suitability for this study).
* Alanine transaminase (ALT) and Aspartate transaminase (AST) ˂2.5 x ULN (≤5 x ULN for participants with liver involvement)
* Participants on a stable dose of anticoagulation therapy are allowed to participate if they have no sign of bleeding or clotting, and prothrombin time international normalized ratio (PT/INR) and activated partial thromboplastin time (aPTT) test results are acceptable at the Investigator's discretion
* Estimated glomerular filtration rate (eGFR) \>60 mL/min/1.73 m\^2, according to the Modified Diet in Renal Disease (MDRD) abbreviated formula and serum creatinine ≤1.5 x ULN
* Participants must have at least one PSMA-positive (prostate-specific membrane antigen) distant metastatic lesion on the screening PSMA PET/CT scan using the study-designated PSMA PET tracers, as determined by the site Investigator. For eligibility purposes, a PSMA-positive lesion must have activity greater than the liver by visual assessment of the screening PSMA PET/CT. A PSMA-positive metastatic lesion should not correspond to a normal tissue structure or benign lesion.
* Documented progressive mCRPC per PCWG3, and a minimum starting PSA value of 2.0 ng/mL is mandatory. Progressive mCRPC is defined as meeting at least one of the following criteria:

1. PSA progression (defined as 2 consecutive increases over a previous reference value obtained at a minimum of 1-week
2. Radiological progression in soft-tissue lesions according to PCWG3 modification of RECIST v1.1 criteria
3. Progression of bone disease (defined as ≥ 2 new bone lesions according to PCWG3 bone scan criteria)

Exclusion Criteria

* Participants who have any of the following tumor lesions which are PSMA negative AND meet the size criteria below are excluded as determined by the site Investigator. A PSMA-negative lesion for eligibility purposes must have activity equal to or less than the liver by visual assessment of the screening PSMA PET/CT scan using the study-designated PSMA PET/CT tracers. A PSMA-negative metastatic lesion should not correspond to a normal tissue structure or benign lesion.

* a. Any single or multiple lymph node(s) ≥2.5 cm in the short axis.
* b. Any solid organ metastasis (e.g., lung, liver, adrenal glands, etc.) that is ≥1 cm in the short axis.
* c. Any bone metastasis with a soft tissue component ≥ 1 cm in short axis with the soft tissue component being PSMA-negative. PSMA-negative osseous metastases without a soft tissue component do not exclude a participant.
* d. Predominantly necrotic lesions with greater than 1 cm of enhancing tissue on contrast-enhanced computed tomography / magnetic resonance imaging (CT/MRI).
* Prior systemic anticancer therapy including chemotherapy, NAAD, biologic therapy, immunotherapy, or investigational therapies within 4 weeks of the start of study treatment, except luteinizing hormone-releasing hormone (LHRH) or gonadotropin-releasing hormone (GnRH). Start of study treatment is allowed in shorter timeframes if 5 half-lives of the prior drug(s) have elapsed.
* Prior radiopharmaceutical treatment using actinium-225.

Other prior radiopharmaceutical treatments:

* Dose escalation and Dose expansion Groups A and B: Prior treatment with a radiopharmaceutical is prohibited.
* Dose expansion Group C: Prior treatment with a radiopharmaceutical is prohibited with the following exceptions: Prior treatment with radium-223 dichloride more than 3 months before the start of study intervention is permitted; and prior treatment with 177 Lu PSMA more than 6 weeks before the start of study intervention is required. Note: Participants who have discontinued 177 Lu-PSMA treatment due to intolerance are excluded from Group C.
* Prior definitive therapy (radiotherapy or surgery) completed less than 6 weeks before the start of study intervention. Note that palliative radiotherapy completed less than 6 weeks before the start of study intervention will be allowed if: (i) no more than 10% of the participants' bone marrow is irradiated, (ii) it does not encompass all potential target/measurable lesions for participants in dose expansion.
* Toxic effects of Common Terminology Criteria for Adverse Events (CTCAE) v5.0 Grade ≥2 from prior anticancer therapy not yet stabilized or where significant post-treatment toxicities have been observed. Chronic toxic effects of CTCAE Grade ≤2 from prior anticancer therapy where no further resolution is expected do not require exclusion with agreement between the Investigator and Sponsor (e.g., chemotherapy-induced neuropathy, fatigue, alopecia, anorexia, etc.).
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Bayer

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Locations

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City of Hope - Duarte Cancer Center

Duarte, California, United States

Site Status NOT_YET_RECRUITING

M Health Fairview Masonic Cancer Clinic - Clinics and Surgery Center

Minneapolis, Minnesota, United States

Site Status NOT_YET_RECRUITING

XCancer Omaha

Omaha, Nebraska, United States

Site Status NOT_YET_RECRUITING

The University of Texas MD Anderson Cancer Center - Texas Medical Center

Houston, Texas, United States

Site Status NOT_YET_RECRUITING

Institut Jules Bordet / Nuclear Medicine

Anderlecht, , Belgium

Site Status RECRUITING

AZ Groeninge Campus Kennedylaan - Urology

Kortrijk, , Belgium

Site Status RECRUITING

UZ Leuven - Campus Gasthuisberg - Nuclear Medicine

Leuven, , Belgium

Site Status NOT_YET_RECRUITING

Cross Cancer Institute, Clinical Trials Unit

Edmonton, Alberta, Canada

Site Status SUSPENDED

BC Cancer - Vancouver Site

Vancouver, British Columbia, Canada

Site Status RECRUITING

Juravinski Cancer Centre - Clinical Trials Department

Hamilton, Ontario, Canada

Site Status RECRUITING

Princess Margaret Cancer Centre - University Health Network - Department of Medical Oncology and Hematology

Toronto, Ontario, Canada

Site Status RECRUITING

Centre Hospitalier de l'Universite de Montreal (CHUM)

Montreal, Quebec, Canada

Site Status RECRUITING

McGill University Health Centre (MUHC) - Research Institute (RI) - McConnell Centre for Innovative Medicine (CIM)

Montreal, Quebec, Canada

Site Status RECRUITING

Centre Hospitalier Universitaire de Sherbrooke (CHUS) - Hopital Fleurimont

Sherbrooke, Quebec, Canada

Site Status RECRUITING

Kuopio University Hospital, Kuopion yliopistollinen sairaala (KYS) - Syövänhoitokeskus

Kuopio, Northern Savonia, Finland

Site Status RECRUITING

HUS-Yhtymä, Helsingin yliopistollinen sairaala (HUS) - Syöpäkeskus

Helsinki, Uusimaa, Finland

Site Status NOT_YET_RECRUITING

Docrates Mehiläinen Syöpäsairaala

Helsinki, Uusimaa, Finland

Site Status NOT_YET_RECRUITING

Tampere University Hospital, Tampereen yliopistollinen sairaala (TAYS) - Syöpäkeskus

Tampere, , Finland

Site Status SUSPENDED

Turku University Hospital, Turun yliopistollinen sairaala (TYKS)

Turku, , Finland

Site Status NOT_YET_RECRUITING

Istituto Europeo di Oncologia s.r.l - Medicina Nucleare

Milan, , Italy

Site Status NOT_YET_RECRUITING

IRCCS Istituto Nazionale Tumori Fondazione Pascale - S. C. Medicina Nucleare e Terapia Metabolica

Napoli, , Italy

Site Status NOT_YET_RECRUITING

Universitair Medisch Centrum Groningen (UMCG) - UMC Groningen Comprehensive Cancer Center

Groningen, , Netherlands

Site Status NOT_YET_RECRUITING

Erasmus Medisch Centrum

Rotterdam, , Netherlands

Site Status WITHDRAWN

Sahlgrenska Universitetssjukhuset - Klinisk prövningsenhet Fas I/FIH

Gothenburg, , Sweden

Site Status NOT_YET_RECRUITING

Skånes Universitetssjukhus Lund - Onkologens kliniska forskningsenhet

Lund, , Sweden

Site Status RECRUITING

Karolinska Universitetssjukhuset - Fas I-enheten Solna CKC

Stockholm, , Sweden

Site Status RECRUITING

Akademiska Sjukhuset - Fas-I-enheten

Uppsala, , Sweden

Site Status SUSPENDED

Kantonsspital Baden

Baden, Canton of Aargau, Switzerland

Site Status WITHDRAWN

Universitätsspital Basel

Basel, Canton of Basel-City, Switzerland

Site Status NOT_YET_RECRUITING

Univestitätsspital Zürich (USZ)

Zurich, , Switzerland

Site Status NOT_YET_RECRUITING

University College London Hospitals NHS Foundation Trust | University College Hospital - NIHR UCLH Clinical Research Facility

London, Greater London, United Kingdom

Site Status RECRUITING

The Royal Marsden NHS Foundation Trust | Sutton - Oak Foundation Drug Development Unit

Sutton, Surrey, United Kingdom

Site Status RECRUITING

The Newcastle upon Tyne Hospitals NHS Foundation Trust | Freeman Hospital - Cancer Trials Research Centre

Newcastle upon Tyne, Tyne and Wear, United Kingdom

Site Status NOT_YET_RECRUITING

Countries

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United States Belgium Canada Finland Italy Netherlands Sweden Switzerland United Kingdom

Central Contacts

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Bayer Clinical Trials Contact

Role: CONTACT

(+)1-888-84 22937

Related Links

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https://clinicaltrials.bayer.com/study/22049

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Other Identifiers

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2023-507486-26-00

Identifier Type: REGISTRY

Identifier Source: secondary_id

22049

Identifier Type: -

Identifier Source: org_study_id

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