^
    8d
    Phase II trial of multi-tyrosine kinase inhibitor ESK981 in combination with PD-1 inhibitor nivolumab in patients with metastatic castration-resistant prostate cancer. (PubMed, Invest New Drugs)
    (Trial registration: ClinicalTrials.gov NCT04159896. Registration date: November 12, 2019.).
    P2 data • Journal • Combination therapy • Metastases
    |
    AR (Androgen receptor)
    |
    AR positive • AR amplification
    |
    Opdivo (nivolumab) • ESK981
    2ms
    Phase II trial of multi-kinase inhibitor ESK981 in patients with metastatic castration-resistant prostate cancer. (PubMed, Invest New Drugs)
    (Trial registration: ClinicalTrials.gov, NCT03456804. Registration date: March 7, 2018).
    P2 data • Journal • Metastases
    |
    AR (Androgen receptor)
    |
    AR positive
    |
    ESK981
    4ms
    ESK981 and Nivolumab for the Treatment of Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=10, Terminated, Barbara Ann Karmanos Cancer Institute | N=49 --> 10 | Recruiting --> Terminated; The study was closed to accrual on 3/1/21 due to safety concerns since 2 patients experienced CVA events.
    Enrollment change • Trial termination • Combination therapy • Metastases
    |
    TP53 (Tumor protein P53)
    |
    Opdivo (nivolumab) • ESK981
    7ms
    Multicenter Trial of ESK981 in Patients With Select Solid Tumors (clinicaltrials.gov)
    P2, N=66, Recruiting, University of Michigan Rogel Cancer Center | Not yet recruiting --> Recruiting
    Enrollment open
    |
    SYP (Synaptophysin) • CHGA (Chromogranin A)
    |
    ESK981
    8ms
    Multicenter Trial of ESK981 in Patients With Select Solid Tumors (clinicaltrials.gov)
    P2, N=66, Not yet recruiting, University of Michigan Rogel Cancer Center | Trial completion date: Jan 2029 --> May 2029 | Initiation date: Jan 2024 --> May 2024 | Trial primary completion date: Jan 2027 --> May 2027
    Trial completion date • Trial initiation date • Trial primary completion date
    |
    SYP (Synaptophysin) • CHGA (Chromogranin A)
    |
    ESK981
    12ms
    Multicenter Trial of ESK981 in Patients With Select Solid Tumors (clinicaltrials.gov)
    P2, N=66, Not yet recruiting, University of Michigan Rogel Cancer Center | Trial completion date: Sep 2028 --> Jan 2029 | Initiation date: Oct 2023 --> Jan 2024 | Trial primary completion date: Aug 2026 --> Jan 2027
    Trial completion date • Trial initiation date • Trial primary completion date
    |
    SYP (Synaptophysin) • CHGA (Chromogranin A)
    |
    ESK981
    over1year
    Multicenter Trial of ESK981 in Patients With Select Solid Tumors (clinicaltrials.gov)
    P2, N=66, Not yet recruiting, University of Michigan Rogel Cancer Center
    New P2 trial
    |
    SYP (Synaptophysin) • CHGA (Chromogranin A)
    |
    ESK981
    over1year
    ESK981 in Treating Patients With Metastatic Castrate-Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=13, Completed, Barbara Ann Karmanos Cancer Institute | Active, not recruiting --> Completed | N=27 --> 13
    Trial completion • Enrollment change • Metastases
    |
    ESK981
    3years
    Autophagy Inhibition by Targeting PIKfyve Potentiates Response to Immune Checkpoint Blockade in Prostate Cancer. (PubMed, Nat Cancer)
    PIKfyve-knockdown recapitulated ESK981's anti-tumor activity and enhanced the therapeutic benefit of immune checkpoint blockade. Our study reveals that targeting PIKfyve via ESK981 turns tumors from cold into hot through inhibition of autophagy, which may prime the tumor immune microenvironment in advanced prostate cancer patients and be an effective treatment strategy alone or in combination with immunotherapies.
    Journal • Checkpoint inhibition • IO biomarker
    |
    IFNG (Interferon, gamma) • CXCL10 (Chemokine (C-X-C motif) ligand 10)
    |
    ESK981