luxdegalutamide (ARV-766) / Arvinas, Novartis - LARVOL DELTA

A phase II study of luxdegalutamide in combination with abiraterone in adult patients with metastatic hormone-sensitive prostate cancer (mHSPC). (ASCO-GU 2026) - P1/2, P2 | "Arm 3 (control): Abiraterone 1000 mg QD or enzalutamide 160 mg QD (Investigator's choice). Exploratory endpoints include assessment of biomarkers associated with treatment response and/or resistance. As of October 9, 2025, 4 patients have been enrolled."

Clinical • Combination therapy • Metastases • P2 data • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

ARV-766, a proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC): Initial results of a phase 1/2 study. (ASCO 2024) - P1/2 | "In this phase 1/2 study of pretreated patients with mCRPC, ARV-766 was well tolerated and showed promising clinical activity in those with tumors harboring AR LBD mutations. ARV-766 warrants further development in advanced prostate cancer."

Metastases • P1/2 data • Alopecia • Fatigue • Genito-urinary Cancer • Immunology • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor • Targeted Protein Degradation • AR

The LuxAR-02 phase II study of luxdegalutamide in combination with 177Lu]Lu-PSMA-617 in patients with prostate-specific membrane antigen (PSMA)–positive metastatic castration resistant prostate cancer (mCRPC). (ASCO-GU 2026) - P1/2, P2 | "The primary objectives are to identify the recommended phase III dose of the combination based on efficacy (PSA50 response rate), safety, tolerability and PK data, and to compare the efficacy in arms 1 and 2 versus control. As of 07 October 2025, 15 patients have been enrolled."

Clinical • Combination therapy • Metastases • P2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

CJSB462C12201: An Open-label Study of JSB462 (Luxdegalutamide) in Combination With Abiraterone in Adult Male Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC) (clinicaltrials.gov) - P2 | N=165 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals | Recruiting ➔ Active, not recruiting

Enrollment closed • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Luxdegalutamide: Data readout from P2 trial (NCT07047118) for mCRPC in 2030 (Novartis) - Q2 2026 Results: Data readout from P2 trial (NCT06991556) for mHSPC in 2032

P2 data • Castration-Resistant Prostate Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer

A Phase I Study of JSB462 (Luxdegalutamide) in Japanese Patients With Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=6 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals | N=15 ➔ 6 | Recruiting ➔ Active, not recruiting

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

A Phase I Study of JSB462 (Luxdegalutamide) in Japanese Patients With Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=15 | Recruiting | Sponsor: Novartis Pharmaceuticals | Trial completion date: Jun 2027 ➔ Jan 2027 | Trial primary completion date: Jun 2027 ➔ Jan 2027

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

An Open-label Study of JSB462 (Luxdegalutamide) in Combination With Abiraterone in Adult Male Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC) (clinicaltrials.gov) - P2 | N=150 | Recruiting | Sponsor: Novartis Pharmaceuticals

Trial initiation date • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

A Study of JSB462 (Luxdegalutamide) Plus Lutetium (177Lu) Vipivotide Tetraxetan in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2 | N=138 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals | Trial completion date: Nov 2028 ➔ May 2028 | Trial primary completion date: Jan 2028 ➔ Jul 2027

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

Preclinical characterization and evaluation of JSB462 (Luxdegalutamide), a novel AR degrader, and its combinations in prostate cancer (AACR 2026) - P2 | "JSB462 demonstrates potent AR degradation at sub-nanomolar concentrations in vitro and dose-dependent tumor growth inhibition in mouse xenograft models, including those resistant to enzalutamide and with high levels of AR. Here, we show preclinical combination data of JSB462 with abiraterone and Pluvicto® that support further investigation of these regimens. Towards that end, two phase 2 trials of JSB462 in combination with abiraterone in patients with high-volume mHSPC (NCT06991556) as well as in combination with Pluvicto® in patients with mCRPC (NCT07047118) are ongoing."

Preclinical • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor • CRBN • CYP17A1

An Open-label Dose Escalation and Expansion, Followed by a Phase II Study of Tulmimetostat (DZR123) and JSB462 (Luxdegalutamide) in Patients With Progressive Metastatic Castrate Resistant Prostate Cancer (mCRPC) (TulmiSTAR-01) (clinicaltrials.gov) - P1/2 | N=188 | Recruiting | Sponsor: Novartis Pharmaceuticals

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

A Study of JSB462 (Luxdegalutamide) Plus Lutetium (177Lu) Vipivotide Tetraxetan in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2 | N=134 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals

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

A Study of JSB462 (Luxdegalutamide) Plus Lutetium (177Lu) Vipivotide Tetraxetan in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2 | N=130 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals | Recruiting ➔ Active, not recruiting

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

Discovery of GLR203701, a highly potent AR PROTAC with favorable PK profile and optimized tissue distribution characteristic (AACR 2025) - "Phase 1 dose escalation trial showed systemic exposure of ARV-766 reached maximum at 320 mg/day in humans. Taking the high exposure level and good bioavailability, GLR203701 is expected to generate a board therapeutic window. These preclinical data support the clinical development of GLR203701 for the treatment of mCRPC."

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

CDZR123A12107: A clinical trial to learn about the effects of DZR123 and JSB462 given together in men with advanced prostate cancer that has stopped responding to other treatments (clinicaltrialsregister.eu) - P1/2 | N=76 | Recruiting | Sponsor: Novartis Pharma AG | Not yet recruiting ➔ Recruiting

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

CDZR123A12107: A clinical trial to learn about the effects of DZR123 and JSB462 given together in men with advanced prostate cancer that has stopped responding to other treatments (clinicaltrialsregister.eu) - P1/2 | N=76 | Not yet recruiting | Sponsor: Novartis Pharma AG

New P1/2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

CJSB462B12201: A Phase II, randomized, open-label, multi-center study of JSB462 (luxdegalutamide) in combination with lutetium (177Lu) vipivotide tetraxetan in adult male patients with PSMA-positive metastatic castration resistant prostate cancer (mCRPC) (clinicaltrialsregister.eu) - P1/2 | N=46 | Recruiting | Sponsor: Novartis Pharma AG

New P1/2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

TulmiSTAR-01: A phase I/II dose optimization study of tulmimetostat in combination with luxdegalutamide versus standard of care (SOC) in patients (pts) with progressive metastatic castrate-resistant prostate cancer (mCRPC). (ASCO-GU 2026) - P1/2 | "Research Funding Novartis Pharma AG. *Choice of ARPI, chemotherapy or lutetium (177Lu) vipivotide tetraxetan. BOR, best overall response; mo, months; DOR, duration of response; QD, once a daily; ORR, objective radiographic response; OS, overall survival; PK, pharmacokinetics, PSA, prostate-specific antigen; RDE, recommended dose for expansion; rPFS, radiographic progression-free survival; R, randomization; RP2D, recommended phase II dose; SOC, standard of care; TTSSE, time to first symptomatic skeletal event."

Clinical • Combination therapy • Metastases • P1/2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • EZH2

Luxdegalutamide: Data readout from P2 trial (NCT07047118) for mCRPC in 2030 (Novartis) - Q4 & FY2025 Results: Data readout from P2 trial (NCT06991556) for mHSPC in 2032

P2 data • Castration-Resistant Prostate Cancer • Hormone Sensitive Prostate Cancer • Oncology

A Phase I Study of JSB462 (Luxdegalutamide) in Japanese Patients With Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=15 | Recruiting | Sponsor: Novartis Pharmaceuticals | Not yet recruiting ➔ Recruiting

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

An Open-label Dose Escalation and Expansion, Followed by a Phase II Study of Tulmimetostat (DZR123) and JSB462 (Luxdegalutamide) in Patients With Progressive Metastatic Castrate Resistant Prostate Cancer (mCRPC) (TulmiSTAR-01) (clinicaltrials.gov) - P1/2 | N=188 | Recruiting | Sponsor: Novartis Pharmaceuticals | Not yet recruiting ➔ Recruiting

Enrollment open • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

An Open-label Dose Escalation and Expansion, Followed by a Phase II Study of Tulmimetostat (DZR123) and JSB462 (Luxdegalutamide) in Patients With Progressive Metastatic Castrate Resistant Prostate Cancer (mCRPC) (TulmiSTAR-01) (clinicaltrials.gov) - P1/2 | N=188 | Not yet recruiting | Sponsor: Novartis Pharmaceuticals

New P1/2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A Phase I Study of JSB462 (Luxdegalutamide) in Japanese Patients With Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=15 | Not yet recruiting | Sponsor: Novartis Pharmaceuticals

New P1 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A Study of JSB462 (Luxdegalutamide) Plus Lutetium (177Lu) Vipivotide Tetraxetan in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2 | N=130 | Recruiting | Sponsor: Novartis Pharmaceuticals

New P2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

An Open-label Study of JSB462 (Luxdegalutamide) in Combination With Abiraterone in Adult Male Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC) (clinicaltrials.gov) - P2 | N=150 | Recruiting | Sponsor: Novartis Pharmaceuticals | Not yet recruiting ➔ Recruiting

Enrollment open • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor