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

    CYP11A1 inhibitor

    Related drugs:
    7d
    A Study to Evaluate the Safety, Pharmacokinetics, Pharmacodynamics, and Antitumor Activity of INV-9956 in Adult Patients With Advanced Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P1/2, N=84, Recruiting, Shenzhen Ionova Life Sciences Co., Ltd. | Trial primary completion date: Apr 2026 --> Jan 2028
    Trial primary completion date
    16d
    A Drug-Drug Interaction Study of Itraconazole and Opevesostat (MK-5684) in Healthy Adult Male Participants (MK-5684-017) (clinicaltrials.gov)
    P1, N=14, Active, not recruiting, Merck Sharp & Dohme LLC | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    prednisone • itraconazole • opevesostat (MK-5684)
    1m
    OMAHA-003: Study of Opevesostat (MK-5684) Versus Alternative NHA in mCRPC (MK-5684-003) (clinicaltrials.gov)
    P3, N=1310, Recruiting, Merck Sharp & Dohme LLC | Trial completion date: Aug 2028 --> Feb 2030
    Trial completion date
    |
    enzalutamide • abiraterone acetate • prednisone • dexamethasone • opevesostat (MK-5684) • Yonsa (abiraterone acetate)
    1m
    A Drug-Drug Interaction Study of Itraconazole and Opevesostat (MK-5684) in Healthy Adult Male Participants (MK-5684-017) (clinicaltrials.gov)
    P1, N=14, Recruiting, Merck Sharp & Dohme LLC | Not yet recruiting --> Recruiting
    Enrollment open
    |
    prednisone • itraconazole • opevesostat (MK-5684)
    1m
    A Study of Opevesostat (MK-568)4 in Japanese Participants With Metastatic Castration-resistant Prostate Cancer (mCRPC) (MK-5684-005) (clinicaltrials.gov)
    P1, N=7, Completed, Merck Sharp & Dohme LLC | Active, not recruiting --> Completed
    Trial completion
    |
    opevesostat (MK-5684)
    2ms
    A Drug-Drug Interaction Study of Itraconazole and Opevesostat (MK-5684) in Healthy Adult Male Participants (MK-5684-017) (clinicaltrials.gov)
    P1, N=14, Not yet recruiting, Merck Sharp & Dohme LLC
    New P1 trial
    |
    prednisone • itraconazole • opevesostat (MK-5684)
    2ms
    A Study of MK-5684 in People With Certain Solid Tumors (MK-5684-015/OMAHA-015) (clinicaltrials.gov)
    P2, N=250, Recruiting, Merck Sharp & Dohme LLC
    Trial initiation date • Pan tumor
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative • EGFR positive
    |
    tamoxifen • fulvestrant • letrozole • exemestane • megestrol • opevesostat (MK-5684)
    3ms
    OMAHA-004: A Study of Opevesostat (MK-5684) Versus Alternative Next-generation Hormonal Agent (NHA) in Metastatic Castration-resistant Prostate Cancer (mCRPC) Post One NHA (MK-5684-004) (clinicaltrials.gov)
    P3, N=1314, Active, not recruiting, Merck Sharp & Dohme LLC | Suspended --> Active, not recruiting
    Enrollment closed
    |
    enzalutamide • abiraterone acetate • prednisone • opevesostat (MK-5684)
    3ms
    A Study of Opevesostat (MK-5684) in China Participants With Metastatic Castration-Resistant Prostate Cancer (mCRPC) (MK-5684-001) (clinicaltrials.gov)
    P1, N=14, Completed, Merck Sharp & Dohme LLC | Active, not recruiting --> Completed
    Trial completion
    |
    opevesostat (MK-5684)
    4ms
    A Study to Evaluate Opevesostat (MK-5684) in Male Participants With Moderate Hepatic Impairment (MK-5684-009) (clinicaltrials.gov)
    P1, N=16, Completed, Merck Sharp & Dohme LLC | Active, not recruiting --> Completed
    Trial completion
    |
    prednisone • opevesostat (MK-5684)
    4ms
    A Study of Opevesostat (MK-5684) in China Participants With Metastatic Castration-Resistant Prostate Cancer (mCRPC) (MK-5684-001) (clinicaltrials.gov)
    P1, N=14, Active, not recruiting, Merck Sharp & Dohme LLC | Trial completion date: Mar 2027 --> Mar 2026 | Trial primary completion date: Nov 2025 --> Mar 2026
    Trial completion date • Trial primary completion date
    |
    opevesostat (MK-5684)
    4ms
    Design, synthesis, and biological evaluation of cytochrome P450 CYP11A1 inhibitors. (PubMed, Bioorg Med Chem Lett)
    Based on the clinical candidate Opevesostat, two series of 23 new compounds were designed and synthesized using a 4H-pyran-4-one core to explore structure-activity relationships at the C2 and C6 positions.Compound II-4 exhibited potent inhibitory activity (95.2% at 100 nM; IC₅₀ = 26.7 nM), comparable to Opevesostat (IC₅₀ = 20.4 nM). Importantly, II-4 showed superior selectivity against CYP1A2, 2C9, and 2D6 (2- to 4-fold improvement), attributed to hydrophobic interactions between its C6 methyl group and Ile 84.These results highlight II-4 as a promising lead compound with optimized activity and selectivity, providing valuable insights for overcoming resistance in prostate cancer therapy.
    Journal
    |
    CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2)
    |
    opevesostat (MK-5684)