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    DRUG CLASS:

    Androgen receptor degrader

    Related drugs:
    14d
    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
    17d
    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
    1m
    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
    2ms
    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)
    2ms
    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)
    2ms
    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, Novartis Pharmaceuticals
    New P1/2 trial
    |
    tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    2ms
    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. | N=160 --> 210
    Enrollment change
    2ms
    A Clinical Study of QLC5508 and/or QLH12016 in Combination With Other Anti-tumor Therapies in Subjects With Advanced Prostate Cancer (clinicaltrials.gov)
    P1/2, N=212, Not yet recruiting, Qilu Pharmaceutical Co., Ltd.
    New P1/2 trial
    |
    Xtandi (enzalutamide) • abiraterone acetate • MHB088C
    3ms
    A Phase I Study of JSB462 (Luxdegalutamide) in Japanese Patients With Metastatic Prostate Cancer (clinicaltrials.gov)
    P1, N=15, Not yet recruiting, Novartis Pharmaceuticals
    New P1 trial
    |
    luxdegalutamide (ARV-766)
    3ms
    Clinical Trial to Evaluate the Tolerance of TQB3201 Tablets (clinicaltrials.gov)
    P1/2, N=291, Not yet recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    New P1/2 trial
    |
    Xtandi (enzalutamide)
    3ms
    A Study to Evaluate the Effect of Rifampicin on the Pharmacokinetics of Oral HRS-5041 in Healthy Subjects (clinicaltrials.gov)
    P1, N=16, Completed, Jiangsu HengRui Medicine Co., Ltd. | Not yet recruiting --> Completed
    Trial completion
    |
    HRS-5041 • rifampicin
    4ms
    Discovery of BMS-986365, a first-in-class dual androgen receptor ligand-directed degrader (AR LDD) and antagonist, for the treatment of advanced prostate cancer. (PubMed, Clin Cancer Res)
    The preclinical observations, coupled with clinical data, strongly support the potential for BMS-986365 to overcome ARPI-resistant disease regardless of AR mutational status. These findings establish BMS-986365 as a first-in-class, dual AR degrader and competitive antagonist, likely to emerge as an important tool in the armamentarium to treat PC.
    Journal
    |
    CRBN (Cereblon)
    |
    Xtandi (enzalutamide)