^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    Androgen receptor degrader

    Related drugs:
    6d
    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, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    Pluvicto (lutetium Lu 177 vipivotide tetraxetan) • luxdegalutamide (ARV-766)
    6d
    D7270C00001: A trial to learn how safe AZD9750 is and how well it works in people with metastatic prostate cancer when given with or without other anticancer drugs (2024-516976-14-00)
    P1/2, N=52, Not yet recruiting, AstraZeneca AB
    New P1/2 trial
    |
    saruparib (AZD5305)
    22d
    Androgen receptor-dependent DRAM1 activation drives autophagic resistance to BRAF inhibitors in BRAFV600-mutant melanoma. (PubMed, Cell Death Dis)
    Functional studies reveal that AR-driven autophagy confers resistance to BRAFi by enhancing cellular survival under therapeutic stress. Our findings establish AR-regulated autophagy as a critical resistance mechanism and provide preclinical evidence for combining AR-targeting PROTAC degrader ARV110 with autophagy inhibitors to overcome BRAFi resistance.
    Journal
    |
    AR (Androgen receptor)
    |
    BRAF mutation • BRAF V600
    |
    bavdegalutamide (ARV-110)
    26d
    A Phase I Clinical Study of GLR2037 in Patients With Advanced Prostate Cancer (clinicaltrials.gov)
    P1, N=65, Not yet recruiting, Gan & Lee Pharmaceuticals.
    New P1 trial
    1m
    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 (2025-521880-10-00)
    P1/2, N=76, Recruiting, Novartis Pharma AG | Not yet recruiting --> Recruiting
    Enrollment open
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • cabazitaxel • tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    2ms
    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) (2024-520155-24-00)
    P1/2, N=46, Recruiting, Novartis Pharma AG
    New P1/2 trial
    |
    Pluvicto (lutetium Lu 177 vipivotide tetraxetan) • luxdegalutamide (ARV-766)
    2ms
    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 (2025-521880-10-00)
    P1/2, N=76, Not yet recruiting, Novartis Pharma AG
    New P1/2 trial
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • cabazitaxel • tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    2ms
    Discovery of AZD9750, an Orally Bioavailable Androgen Receptor Degrader for the Treatment of Prostate Cancer. (PubMed, J Med Chem)
    This compound inhibited AR signaling in vitro and was able to inhibit tumor growth in vivo in a mouse prostate cancer xenograft model. Extensive profiling in terms of drug-like properties allowed this to be progressed into development as AZD9750.
    Journal
    |
    AR (Androgen receptor)
    3ms
    ANDROMEDA: A Trial to Learn How Safe AZD9750 is and How Well it Works in People With Metastatic Prostate Cancer When Given With or Without Other Anticancer Drugs (clinicaltrials.gov)
    P1/2, N=300, Not yet recruiting, AstraZeneca
    New P1/2 trial • First-in-human
    |
    saruparib (AZD5305)
    3ms
    A Study of BMS986365 in Combination With Degarelix in People With Prostate Cancer (clinicaltrials.gov)
    P2, N=30, Recruiting, Memorial Sloan Kettering Cancer Center
    New P2 trial
    |
    Firmagon (degarelix)
    3ms
    A Phase I Study of JSB462 (Luxdegalutamide) in Japanese Patients With Metastatic Prostate Cancer (clinicaltrials.gov)
    P1, N=15, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    |
    luxdegalutamide (ARV-766)
    3ms
    A Study to Evaluate the Effect of Itraconazole and Rifampin on the Drug Levels of AR-LDD (BMS-986365) in Healthy Adult Male Participants (clinicaltrials.gov)
    P1, N=42, Recruiting, Celgene | Not yet recruiting --> Recruiting
    Enrollment open
    |
    itraconazole • rifampicin