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    DRUG CLASS:

    Androgen receptor degrader

    Related drugs:
    8d
    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)
    8d
    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)
    9d
    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)
    29d
    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
    1m
    CC-94676-PCA-001: Study to Evaluate the Safety and Tolerability of CC-94676 in Participants With Metastatic Castration-Resistant Prostate Cancer (clinicaltrials.gov)
    P1, N=131, Completed, Celgene | Active, not recruiting --> Completed | N=250 --> 131 | Trial completion date: Dec 2026 --> Oct 2025
    Trial completion • Enrollment change • Trial completion date
    1m
    A Study to Assess the Safety, Pharmacokinetics, and Anti-Tumor Activity of Oral HP518 in mCRPC Patients (clinicaltrials.gov)
    P1/2, N=84, Recruiting, Hinova Pharmaceuticals Inc. | Trial primary completion date: Oct 2025 --> Mar 2026
    Trial primary completion date
    1m
    Evaluation of the Safety, Tolerability and Pharmacokinetics of AH-001 Following Topical Single and Multiple Ascending Dose Administration (clinicaltrials.gov)
    P1, N=64, Completed, AnHorn Medicines Co. Ltd. | Recruiting --> Completed
    Trial completion
    2ms
    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, Not yet recruiting, Celgene
    New P1 trial
    |
    itraconazole • rifampicin
    2ms
    A Study of HRS-5041 Tablets Combined With Antitumor Therapy in Subjects With Advanced Prostate Cancer (clinicaltrials.gov)
    P1/2, N=100, Recruiting, Jiangsu HengRui Medicine Co., Ltd. | Trial completion date: Dec 2026 --> Jun 2027 | Trial primary completion date: Sep 2025 --> Jun 2026
    Trial completion date • Trial primary completion date
    |
    docetaxel • abiraterone acetate • prednisone • zeprumetostat (SHR-2554) • HRS-5041 • M9466
    3ms
    A Study Evaluating the Safety, Pharmacokinetics, and Activity of RO7656594 In Participants With Advanced or Metastatic Prostate Cancer (clinicaltrials.gov)
    P1, N=210, Recruiting, Genentech, Inc. | Trial completion date: Jul 2026 --> Jun 2027 | Trial primary completion date: Jul 2026 --> Jun 2027
    Trial completion date • Trial primary completion date
    4ms
    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, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    |
    tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    4ms
    Proteolysis-Targeting Chimera (PROTAC): Current Applications and Future Directions. (PubMed, MedComm (2020))
    We evaluate clinical progression of breakthrough candidates such as ARV-110 for prostate cancer, ARV-471 for breast cancer, and BTK degraders, while discussing critical challenges including the "hook effect" and oral bioavailability limitations. This review provides essential foundations for rational target selection, molecular optimization, and clinical translation strategies. By integrating mechanistic insights with clinical realities, this analysis offers perspectives on PROTAC technology advancement and identifies opportunities for transforming treatment of complex diseases resistant to conventional therapies.
    Review • Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • STAT3 (Signal Transducer And Activator Of Transcription 3)
    |
    KRAS mutation • KRAS G12C • KRAS G12 • STAT3 mutation
    |
    bavdegalutamide (ARV-110) • vepdegestrant (ARV-471)