^
    9ms
    EPI-7386-CS-010: EPI-7386 in Combination with Enzalutamide Compared with Enzalutamide Alone in Subjects with MCRPC (clinicaltrials.gov)
    P1/2, N=77, Terminated, ESSA Pharmaceuticals | N=150 --> 77 | Active, not recruiting --> Terminated; Study was terminated early due to a lack of improved efficacy.
    Enrollment change • Trial termination
    |
    Xtandi (enzalutamide) • masofaniten (EPI-7386)
    9ms
    EPI-7386-CS-001: Oral EPI-7386 in Patients with Castration-Resistant Prostate Cancer (clinicaltrials.gov)
    P1, N=71, Terminated, ESSA Pharmaceuticals | Active, not recruiting --> Terminated; Study was terminated early due to a lack of improved efficacy.
    Trial termination
    |
    abiraterone acetate • apalutamide • masofaniten (EPI-7386)
    10ms
    A Study of EPI-7386 in Combination With Abiraterone Acetate Plus Prednisone, or Apalutamide in Metastatic Castration-resistant Prostate Cancer (mCRPC) (clinicaltrials.gov)
    P1, N=3, Terminated, Janssen Research & Development, LLC | Phase classification: P1b --> P1
    Phase classification
    |
    abiraterone acetate • prednisone • apalutamide • masofaniten (EPI-7386)
    1year
    EPI-7386-CS-010: EPI-7386 in Combination with Enzalutamide Compared with Enzalutamide Alone in Subjects with MCRPC (clinicaltrials.gov)
    P1/2, N=150, Active, not recruiting, ESSA Pharmaceuticals | Recruiting --> Active, not recruiting | Trial completion date: Jan 2026 --> Jan 2025 | Trial primary completion date: Aug 2025 --> Oct 2024
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    Xtandi (enzalutamide) • masofaniten (EPI-7386)
    1year
    EPI-7386-CS-001: Oral EPI-7386 in Patients with Castration-Resistant Prostate Cancer (clinicaltrials.gov)
    P1, N=99, Active, not recruiting, ESSA Pharmaceuticals | Recruiting --> Active, not recruiting | Trial completion date: Sep 2026 --> Jan 2025 | Trial primary completion date: Apr 2026 --> Oct 2024
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    abiraterone acetate • apalutamide • masofaniten (EPI-7386)
    over1year
    Combining EPI-7386 w/ Enzalutamide & Androgen Deprivation Therapy for Newly Diagnosed Prostate Cancer (clinicaltrials.gov)
    P2, N=35, Not yet recruiting, Pedro Barata, MD, MSc
    New P2 trial • Metastases
    |
    Xtandi (enzalutamide) • masofaniten (EPI-7386)
    almost2years
    EPI-7386 in Combination With Enzalutamide Compared With Enzalutamide Alone in Subjects With mCRPC (clinicaltrials.gov)
    P1/2, N=150, Recruiting, ESSA Pharmaceuticals
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Xtandi (enzalutamide) • masofaniten (EPI-7386)
    over2years
    Phase I/II trial of oral EPI-7386 in combination with enzalutamide (enz) compared to enz alone in metastatic castration-resistant prostate cancer (mCRPC) subjects: Current phase I (PI) results (ESMO 2023)
    Conclusions With no safety concerns from cohorts 1-3, cohort 4 is currently enrolling at EPI-7386 BID + 160 mg QD Enz to evaluate optimal RP2Ds before the P2 component of the trial. Updated results, including cohort 4, will be presented.
    Clinical • P1/2 data • Combination therapy • Metastases
    |
    CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
    |
    Xtandi (enzalutamide) • masofaniten (EPI-7386)
    over2years
    A Study of EPI-7386 in Combination With Abiraterone Acetate Plus Prednisone, or Apalutamide in Metastatic Castration-resistant Prostate Cancer (mCRPC) (clinicaltrials.gov)
    P1b, N=3, Terminated, Janssen Research & Development, LLC | N=82 --> 3 | Trial completion date: Jun 2025 --> Sep 2022 | Suspended --> Terminated | Trial primary completion date: Jan 2024 --> Sep 2022; Administrative Decision
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date • Combination therapy • Metastases
    |
    abiraterone acetate • prednisone • apalutamide • masofaniten (EPI-7386)
    over3years
    Androgen receptor (AR) N-terminal domain degraders can degrade AR full length and AR splice variants in CRPC preclinical models (AACR 2022)
    However, we recently demonstrated that EPI-7386, an AR NTD small molecule inhibitor, inhibits AR activity by binding to Tau5 region of the NTD. In summary, we report preclinical data on the first generation of ANITAC molecules, that can be orally bioavailable and show activity against forms of AR expressed in late stage CRPC patients.
    Preclinical
    |
    AR (Androgen receptor)
    |
    AR expression • AR splice variant 7
    |
    masofaniten (EPI-7386) • EPI-8207