177Lu-rosopatamab tetraxetan (TLX591) / Telix, BZL Biologics, China Grand Pharma - LARVOL DELTA

ProstACT Global: A phase 3 study of Lutetium (Lu177) rosopatamab tetraxetan plus SoC vs SoC alone in patients with metastatic castration-resistant prostate cancer (SUO 2025) - P3 | "In Part 1, patients are divided into 3 groups (n=10 each) to receive 2 single intravenous injections of 76 mCi each, 14d apart, of 177 Lu-rosopatamab with standard of care (SoC) combinations with abiraterone, enzalutamide, or docetaxel to characterize biodistribution & safety profiles of 177 Lu-rosopatamab + SoC combinations...Eligible patients must have PSMA-expressing mCRPC and have experienced disease progression on a minimum 12w prior therapy on their 1 st ARPI (abiraterone, apalutamide, darolutamide, or enzalutamide) in metastatic castration-sensitive PC, non-metastatic CRPC, or mCRPC settings...This study is sponsored by Telix Pharmaceuticals and is currently enrolling in Part 1. ClinicalTrials.gov ID: NCT06520345 "

Clinical • Metastases • P3 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Safety, tolerability, and dosimetry of 177Lu-TLX591 with best standard of care in patients with PSMA-expressing metastatic castration-resistant prostate cancer (ProstAct-SELECT). (ASCO-GU 2024) - P1 | "The primary endpoints include the absorbed radiation dose of administered 177Lu-TLX591 to kidneys, liver, lungs, spleen, bone/red marrow, and salivary glands; tumour-to-healthy tissue ratios and residence times; and type, frequency, and severity of TEAEs. Clinical trial information: NCT04786847."

Clinical • Metastases • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

CONVERGE-01: Dosimetry, randomized dose optimization, dose escalation, and efficacy of ac-225 rosopatamab tetraxetan in participants with PSMA-positive castration-resistant prostate cancer. (ASCO-GU 2025) - P2 | "Exploratory endpoints include: rPFS, ORR, and DOR via RECIST v1.1 (PCWG3-modified where appropriate), genomic and imaging biomarker nomination. Enrollment began in August 2024."

Clinical • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Safety and dosimetry of 177Lu-rosopatamab tetraxetan plus SoC in patients with metastatic castration-resistant prostate cancer: Preliminary results from part 1 of phase 3 ProstACT Global study. (ASCO 2026) - P3 | "Pts received 2 single IV injections 177Lu-rosopatamab (76 mCi each), 14d apart, with assigned SoC (Cohort 1, +abiraterone; Cohort 2, +enzalutamide; Cohort 3, followed by docetaxel; planned n=10 each). 177Lu-rosopatamab + SoC for pts with mCRPC demonstrates a manageable safety & tolerability profile; predictable PK profile with prolonged tumor residence; & organ radiation exposure below recommended thresholds. Radiation absorbed dose was highest for liver (clearance organ), which is comparatively radioresistant. Data support continued investigation in Part 2."

Clinical • Late-breaking abstract • Metastases • P3 data • P3 data: top line • Castration-Resistant Prostate Cancer • Dental Disorders • Genito-urinary Cancer • Neutropenia • Oncology • Prostate Cancer • Solid Tumor • Thrombocytopenia • Xerostomia

ProstACT Global: A Phase 3 Study of Lutetium (Lu177) Rosopatamab Tetraxetan plus Standard of Care vs. Standard of Care Alone in Patients with Metastatic Castration-Resistant Prostate Cancer (ASTRO 2025) - "In Part 1, patients are divided into 3 groups (n=10 each) to receive 2 single intravenous injections of 76 mCi each, 14 days apart, of 177Lu-rosopatamab with standard of care (SoC) combinations with abiraterone, enzalutamide, or docetaxel to characterize biodistribution & safety profiles of 177Lu-rosopatamab + SoC combinations...Eligible patients must have PSMA-expressing mCRPC and have experienced disease progression on a minimum 12w prior therapy on their 1st ARPI (abiraterone, apalutamide, darolutamide, or enzalutamide) in metastatic castration-sensitive PC, non-metastatic CRPC, or mCRPC settings... TBD"

Clinical • Metastases • P3 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

ProstACT GLOBAL: A phase 3 study of best standard of care with and without 177Lu-DOTA-rosopatamab (TLX591) for patients with PSMA expressing metastatic castration-resistant prostate cancer progressing despite prior treatment with a novel androgen axis drug. (ASCO-GU 2024) - P3 | "Eligible patients must have received prior therapy with either enzalutamide or abiraterone plus prednisone, and 1 line of prior taxane therapy or have refused or are ineligible for taxanes. Secondary endpoints include 5-year overall survival, tumor objective response rate, time to symptomatic skeletal event, progression free survival, and number of participants with treatment-related adverse events. Clinical trial information: NCT04876651."

Clinical • Metastases • P3 data • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

A PHASE 3 STUDY OF 177LU-TLX591 PLUS SOC VS SOC ALONE IN PATIENTS WITH MCRPC (PROSTACT GLOBAL) (SUO 2024) - "SoC may be an alternative ARPI or docetaxel. This study is currently enrolling. "

Clinical • P3 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Final results of a phase I/II dose-escalation study of fractionated dose 177 Lu-PSMA-617 for progressive metastatic castration resistant prostate cancer (mCRPC). (ASCO 2024) - P1/2 | "29 (58%) with prior >2 ARPI, 29 (58%) with >1 chemo, 14 (28%) with Ra-223, 2 (4%) with 177 Lu-J591... A single-cycle of fractionated-dose 177Lu-PSMA-617 is safe. Despite no pre-selection for PSMA expression, most had PSA decline with favorable PFS and OS compared to historical controls and similar to PSMA-selected targeted radionuclide studies administering multiple cycles in a less dose-intense approach."

Clinical • Metastases • P1/2 data • Anemia • Fatigue • Genito-urinary Cancer • Hematological Disorders • Metastatic Castration-Resistant Prostate Cancer • Neutropenia • Oncology • Pain • Prostate Cancer • Solid Tumor • Thrombocytopenia • Xerostomia • FOLH1

ProstACT Global: A phase 3 study of lutetium (Lu177) rosopatamab tetraxetan plus standard of care vs standard of care alone in patients with metastatic castration-resistant prostate cancer (ESMO 2025) - P3 | "In Part 1, patients are divided into 3 groups (n=10 each) to receive 2 single intravenous injections of 76 mCi each, 14d apart, of 177 Lu-rosopatamab with standard of care (SoC) combinations with abiraterone, enzalutamide, or docetaxel to characterize biodistribution & safety profiles of 177 Lu-rosopatamab + SoC combinations...Eligible patients must have PSMA-expressing mCRPC and have experienced disease progression on a minimum 12w prior therapy on their 1 st ARPI (abiraterone, apalutamide, darolutamide, or enzalutamide) in metastatic castration-sensitive PC, non-metastatic CRPC, or mCRPC settings...Legal entity responsible for the study Telix Pharmaceuticals. Funding Telix Pharmaceuticals."

Clinical • Metastases • P3 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Theranostic Potential of 177Lu-TLX591 with Best Standard-of-Care and 68Ga-PSMA-11 PET for Patients with Metastatic Castration-Resistant Prostate Cancer: Results from the Phase 1 ProstACT SELECT Trial. (PubMed, Cancers (Basel)) - P1 | "In a heterogenous population representative of a real-world setting, 177Lu-TLX591 therapy in combination with SOC demonstrated a manageable and predictable safety profile, durable retention, and low salivary gland radiation exposure. Further evaluation in larger, randomized studies is warranted."

Journal • P1 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

FDA Alignment to Advance ProstACT Global Phase 3 Trial (The Manila Times) - "The FDA has confirmed that the safety data from Part 1 of the study is sufficient to enable progression of Part 2 of ProstACT Global into the U.S. in which TLX591-Tx is administered in two doses, 14 days apart, in combination with one of three randomized standard of care (SOC) therapies: abiraterone, enzalutamide or docetaxel. The FDA and Telix also achieved alignment on the Part 2 clinical trial protocol, statistical analysis plan, and ongoing safety monitoring plan. The result is a consistent framework for study execution as enrollment continues internationally and expands into the U.S....Initiation of Part 2 in the U.S. remains subject to the FDA’s review of an Investigational New Drug (IND) amendment. The IND amendment will also be aligned with a pending regulatory submission to initiate the ProstACT Global study in Europe. The trial continues to enroll patients in regions where Part 2 is approved."

FDA event • Trial status • Castration-Resistant Prostate Cancer

ProstACT Global Phase 3 (Part 1) Data Presented in Late-Breaking Oral Session at ASCO 2026 (GlobeNewswire) - "Data from 36 patients (baseline median PSA4: 18.18 ng/mL) who received any study treatment were included: Cohort 1 (11 patients), TLX591-Tx + abiraterone; Cohort 2 (11 patients), TLX591-Tx + enzalutamide; Cohort 3 (14 patients), TLX591-Tx followed by docetaxel....No new safety signals identified. Almost all treatment-emergent non-hematologic events were Grade 1–2, primarily fatigue (53%), nausea (28%) and dry mouth (25%)....Telix has initiated Part 2, a 2:1 randomized treatment expansion, in jurisdictions where regulatory approvals have been obtained. Engagement is underway with the United States (U.S.) Food and Drug Administration (FDA) to discuss Part 1 data and seek an Investigational New Drug (IND) amendment to progress Part 2 in the U.S."

FDA event • Late-breaking abstract • P3 data • Trial status • Castration-Resistant Prostate Cancer

Effect of anti-PSMA Antibody J591 Co-administration on Tumor Uptake and Dosimetry of 64Cu-PSMA-I&T in Prostate Cancer Xenografts (SNMMI 2026) - "In prior preclinical work combining 177Lu-J591 and 177Lu-PSMA-617, we discovered an additive effect in radiation absorbed dose with co-injection of the two agents. Co-administration of anti-PSMA antibody J591 increases tumor uptake of 64Cu-PSMA-I&T and radiation absorbed dose in PSMA-positive prostate cancer xenograft models. These findings indicate that antibody co-administration may represent a viable strategy to increase internalization of PSMA-I&T and support further investigation of combination targeting approaches for optimization of PSMA-targeting radionuclide therapy."

Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Effect of anti-PSMA Antibody J591 Co-administration on Tumor Uptake and Dosimetry of 64Cu-PSMA-I&T in Prostate Cancer Xenografts (SNMMI 2026) - "In prior preclinical work combining 177Lu-J591 and 177Lu-PSMA-617, we discovered an additive effect in radiation absorbed dose with co-injection of the two agents. Co-administration of anti-PSMA antibody J591 increases tumor uptake of 64Cu-PSMA-I&T and radiation absorbed dose in PSMA-positive prostate cancer xenograft models. These findings indicate that antibody co-administration may represent a viable strategy to increase internalization of PSMA-I&T and support further investigation of combination targeting approaches for optimization of PSMA-targeting radionuclide therapy."

Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Integrating PSMA Radioligand Therapy with Pelvic Radiotherapy for Men with PSMA detected Oligorecurrent Pelvic Nodal Metastases of Prostate Cancer (ESTRO 2026) - "Overall survival with [177Lu]Lu-PSMA-617 versus cabazitaxel in metastatic castration-resistant prostate cancer (TheraP): secondary outcomes of a randomised, open-label, phase 2 trial. Combining SPRT with ¹⁷⁷Lu-TLX591-CHO RLT, without ADT, achieved promising biochemical and metabolic responses while delaying the need for ADT in PSMApositive oligorecurrent pelvic nodal PC. These findings support further evaluation in randomized trials to confirm efficacy and refine safety profiles References: 1. Ost P, et al."

Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Neutropenia • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor • Thrombocytopenia

ProstACT Global Phase 3 (Part 1) Selected as Late-Breaking Abstract at ASCO 2026 (The Manila Times) - "Part 1 of the trial is a safety and dosimetry lead-in, assessing the tolerability, biodistribution, and radiation dose profile of TLX591-Tx when administered in combination with SoC in patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC)."

Late-breaking abstract • P3 data • Castration-Resistant Prostate Cancer

177Lu Radiolabeled Monoclonal Antibody HuJ591 (177Lu-J591) and Ketoconazole in Patients With Prostate Cancer (clinicaltrials.gov) - P2 | N=55 | Active, not recruiting | Sponsor: Weill Medical College of Cornell University | Trial completion date: May 2026 ➔ Sep 2026

Trial completion date • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Descriptive analysis of patients with mCRPC and liver metastases receiving alpha and beta PSMA targeted radionuclide therapy (PSMA-TRT) (AACR 2024) - "Patients received alpha therapy (225Ac-J591), beta therapy (fractionated 177Lu-PSMA-617, single-dose and fractionated 177Lu-J591) or a combination of both (225Ac-591 and 177Lu-PSMA-I&T)... This dataset adds to the collective literature of two subgroups of patients with mCRPC receiving TRT: those with liver disease and those with mutations in DNA repair pathways. The results of this study suggest higher rates of response in patients receiving alpha therapy, either alone or in combination with beta therapy, and in patients with high radiotracer uptake on PSMA-PET, based on PSMA-imaging score of 3 or 4. Genomic alterations in DRR proteins did not have clear implications."

Clinical • Oncology • Prostate Cancer • BRCA2 • CHEK2 • MSH2 • TP53

ProstACT Global Phase 3 Study (Part 1) Achieves Primary Objectives (GlobeNewswire) - "Key findings include: Tolerability profile supported by dosimetry and low-grade non-hematologic events; Lesion dosimetry indicates no difference in absorbed dose profile across cohorts; No adverse drug-drug interactions observed in TLX591-Tx combinations; Hematologic events are in line with expectations and transient and manageable, with similar rates of recovery across all patient cohorts; The results from Part 1 are consistent with prior clinical studies of this first-in-class lutetium radio antibody-drug conjugate (rADC) therapy....Part 1 data will be presented to the United States (U.S.) Food and Drug Administration (FDA) to seek an Investigational New Drug (IND) amendment to progress Part 2 in the U.S."

FDA event • P3 data • Castration-Resistant Prostate Cancer

PROSTACT: The Present Study Aims to Compare Patients Who Receive the Investigational Product (177Lu-DOTA-rosopatamab) Plus Standard of Care, in Comparison to Standard of Care Only (clinicaltrials.gov) - P3 | N=16 | Terminated | Sponsor: Telix Pharmaceuticals (Innovations) Pty Ltd | N=392 ➔ 16 | Trial completion date: Dec 2028 ➔ Jul 2025 | Recruiting ➔ Terminated | Trial primary completion date: Nov 2025 ➔ Jul 2025; Telix is conducting a separate Phase 3 clinical trial - ProstACT Global NCT06520345- to expedite the development and approval process under an IND. Consequently, this necessitates the closure of the current 177Lu-TLX591-002 Phase 3 trial.

Enrollment change • Trial completion date • Trial primary completion date • Trial termination • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

ProstACT Global Phase 3 Update: First Patient Dosed in Randomized Treatment Expansion, Part 1 Readout Plans Confirmed (Telix Press Release) - "Telix Pharmaceuticals...announces that the first patient has been dosed in Part 2 (randomized treatment expansion) of its ProstACT Global Phase 3 study evaluating its lead prostate cancer therapy candidate TLX591 (lutetium (177Lu) rosopatamab tetraxetan) in patients with metastatic castration resistant prostate cancer (mCRPC). The patient was dosed at the Australian Prostate Centre (APC) in Melbourne, Australia....Telix will submit Part 1 data to the United States (U.S.) Food and Drug Administration (FDA) to enable clearance to expand Part 2 of the trial to U.S. sites. A public disclosure of preliminary results from Part 1 of the study will be aligned to engagement with the FDA."

FDA event • P3 data • Trial status • Castration-Resistant Prostate Cancer

ANALYSIS OF KETOCONAZOLE INDUCED SUPPRESSION OF ADRENAL HORMONES AND ITS CLINICAL IMPLICATIONS FOR PATIENTS WITH HIGH-RISK NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER TREATED WITH PSMA-TARGETED RADIONUCLIDE THERAPY (SUO 2025) - "All patients received keto (400 mg TID) with HC and were randomized 2:1 to either 177 Lu-J591 or 111 In-J591 after 1 month of keto/HC. Ketoconazole with hydrocortisone therapy in patients with high risk M0 CRPC results in androgen suppression, with pre-treatment testosterone and androstenedione associated with outcomes."

Clinical • Metastases • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Long-term adverse events (AEs) in PSMA targeted radionuclide therapy (TRT) for castration-resistant prostate cancer (CRPC) (ESMO 2025) - P1, P1/2, P2, P3 | "59 patients received 177Lu-J591 (51%), 19 (16%) 177Lu-PSMA-617, 25 (22%) 225Ac-J591, 8 (7%) 225Ac-J591 + 177Lu-PSMA-I&T, 4 (3%) 177Lu-PSMA-I&T, and 1 (1%) 90Y-J591. Table: 2404P Category of adverse events (AEs) by grade and number of cases attributed to a cause other than PSMA-targeted radionucleotide therapy AE Type AE (%) Grade 1 (n) Grade 2 (n) Grade 3 (n) Grade 4 (n) Alternate cause in AEs Grades 3-4 (%) Kidney Injury 32 (28) 6 19 3 4 5/7 (71) Elevated trasnaminases 40 (34) 25 12 0 3 2/3 (66) Elevated bilirubin 16 (14) 4 5 3 4 6/7 (86) Neutropenia 11 (9) 5 2 1 3 4/4 (100) Thrombocytopenia 57 (49) 24 14 10 9 18/19 (95) Anemia 79 (68) 34 24 17 4 19/21 (90) Conclusions To our knowledge, this is the largest updated study of long-term AEs on prospective trials of PSMA-TRT. Secondary cancers and renal, liver, and marrow toxicities exist, but are not commonly observed."

Adverse events • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Head and Neck Cancer • Melanoma • Oncology • Pancreatic Cancer • Prostate Cancer • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Urothelial Cancer

Real-world treatment patterns in patients with metastatic castration-resistant prostate cancer (mCRPC) previously treated with androgen receptor pathway inhibitor (ARPI) or docetaxelProstACT Global: A phase 3 study of Lutetium (Lu177) rosopatamab tetraxetan plus standard of care vs standard of care alone in patients with metastatic castration-resistant prostate cancer (PCF 2025) - "BACKGROUND: Patients with mCRPC whose disease progressed on an ARPI have a poor prognosis, with median overall survival of <2 years (Sayegh, Eur Urol Focus 2023). These real-world data show that ARPIs remain the most common 1L and 2L treatment in patients with mCRPC despite prior ARPI and/or docetaxel alongside androgen deprivation therapy for mHSPC or nmCRPC. TABLE. Treatment regimens by line of therapy in patients with mCRPC 1L regimen (N=510), 2L regimen (N=188), 3L regimen (N=80), n (%) n (%) n (%) ARPI*,† 289 (56.7) ARPI*,† 83 (44.1) Taxane‡ 23 (28.8) Abiraterone 149 (29.2) Abiraterone 35 (18.6) ARPI*,† 21 (26.3) Enzalutamide 124 (24.3) Enzalutamide 34 (18.1) Enzalutamide 10 (12.5) Taxane‡ 86 (16.9) Taxane‡ 50 (26.6) Abiraterone 8 (10.0) Abiraterone + Cabazitaxel + 16 (3.1) Olaparib 9 (4.8) 8 (10.0) Docetaxel Carboplatin 1 Olaparib 16 (3.1) Lutetium-177 7 (3.7) Lutetium-177 6 (7.5) Abiraterone + Sipuleucel-T 15 (2.9) 4 (2.1) Radium-223 5 (6.3) Sipuleucel-T Other..."

Clinical • HEOR • Metastases • P3 data • Real-world • Real-world evidence • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

ProstACT Global: A phase 3 study of Lutetium (Lu177) rosopatamab tetraxetan plus standard of care vs standard of care alone in patients with metastatic castration-resistant prostate cancer (EANM 2025) - No abstract available

Clinical • Metastases • P3 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor