^
    2ms
    INCB 57643-103: Safety and Tolerability Study of INCB057643 in Participants With Myelofibrosis and Other Advanced Myeloid Neoplasms (clinicaltrials.gov)
    P1, N=140, Active, not recruiting, Incyte Corporation | Recruiting --> Active, not recruiting | N=231 --> 140
    Enrollment closed • Enrollment change
    |
    Jakafi (ruxolitinib) • INCB057643
    6ms
    A Study to Evaluate the Relative Bioavailability of New Formulations of INCB057643 Tablets Administered Orally in Healthy Participants (clinicaltrials.gov)
    P1, N=48, Completed, Incyte Corporation | Recruiting --> Completed
    Trial completion
    |
    INCB057643
    7ms
    A Phase 2 Study of INCB57643 (BET Inhibitor) in Combination With Ruxolitinib in JAK Inhibitor-naïve Patients With Myelofibrosis (clinicaltrials.gov)
    P2, N=0, Withdrawn, M.D. Anderson Cancer Center | N=30 --> 0 | Trial completion date: Apr 2029 --> May 2025 | Initiation date: Mar 2025 --> Sep 2024 | Not yet recruiting --> Withdrawn | Trial primary completion date: Apr 2027 --> May 2025
    Enrollment change • Trial completion date • Trial initiation date • Trial withdrawal • Trial primary completion date
    |
    Jakafi (ruxolitinib) • INCB057643
    7ms
    A Study to Evaluate the Relative Bioavailability of New Formulations of INCB057643 Tablets Administered Orally in Healthy Participants (clinicaltrials.gov)
    P1, N=48, Recruiting, Incyte Corporation | Not yet recruiting --> Recruiting
    Enrollment open
    |
    INCB057643
    7ms
    A Study to Evaluate the Relative Bioavailability of New Formulations of INCB057643 Tablets Administered Orally in Healthy Participants (clinicaltrials.gov)
    P1, N=48, Not yet recruiting, Incyte Corporation
    New P1 trial
    |
    INCB057643
    1year
    LIMBER: Safety and Tolerability Study of INCB057643 in Participants With Myelofibrosis and Other Advanced Myeloid Neoplasms (clinicaltrials.gov)
    P1, N=231, Recruiting, Incyte Corporation | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Nov 2024 --> Dec 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    Jakafi (ruxolitinib) • INCB057643
    1year
    A Phase 2 Study of INCB57643 (BET Inhibitor) in Combination With Ruxolitinib in JAK Inhibitor-naïve Patients With Myelofibrosis (clinicaltrials.gov)
    P2, N=30, Not yet recruiting, M.D. Anderson Cancer Center
    New P2 trial
    |
    Jakafi (ruxolitinib) • INCB057643
    almost2years
    LIMBER: Safety and Tolerability Study of INCB057643 in Participants With Myelofibrosis and Other Advanced Myeloid Neoplasms (clinicaltrials.gov)
    P1, N=216, Recruiting, Incyte Corporation | N=138 --> 216
    Enrollment change • Metastases
    |
    Jakafi (ruxolitinib) • INCB057643
    2years
    Bromodomain and Extra-Terminal Inhibitor INCB057643 (LIMBER-103) in Patients with Relapsed or Refractory Myelofibrosis and Other Advanced Myeloid Neoplasms: A Phase 1 Study (ASH 2023)
    INCB057643 monotherapy (4 and 8 mg qd) and combined (4 and 6 mg qd) with ruxolitinib was generally well tolerated, whereas the 12 mg qd monotherapy dose caused 2 DLTs. There were no treatment-related fatal events. Improvements in spleen size and symptom burden were observed in patients receiving ≥8 mg in the monotherapy group and 4 mg in the combination therapy group.
    Clinical • P1 data • Metastases
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog)
    |
    Jakafi (ruxolitinib) • INCB057643
    2years
    The synergy of the XPO1 inhibitors combined with the BET inhibitor INCB057643 in high-grade B-cell lymphoma via downregulation of MYC expression. (PubMed, Sci Rep)
    This study demonstrated that the BET antagonist INCB057643 synergized with the XPO1 inhibitors (selinexor and eltanexor) to decrease cell viability and increase cell apoptosis in HGBCL-DH cells with or without TP53 mutations. Collectively, we might provide a potential promising combination therapy regimen for the management of HGBCL-DH. Clinical evaluations are warranted to confirm this conclusion.
    Journal • IO biomarker
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2)
    |
    TP53 mutation • TP53 wild-type • MYC expression • MYC rearrangement • BCL2 rearrangement
    |
    Xpovio (selinexor) • eltanexor (KPT-8602) • INCB057643
    over2years
    BROMODOMAIN AND EXTRA-TERMINAL (BET) INHIBITOR INCB057643 (LIMBER-103) IN PATIENTS (PTS) WITH RELAPSED OR REFRACTORY MYELOFIBROSIS (R/R MF) AND OTHER ADVANCED MYELOID NEOPLASMS: A PHASE 1 STUDY (EHA 2023)
    INCB057643 is a small-molecule BET inhibitor evaluated as monotherapy and in combination with ruxolitinib (RUX) in pts with advanced malignancies in 2 previous phase 1/2 clinical trials. Treatment with INCB057643 monotherapy (4 and 8 mg qd) and in combination (4 mg qd) with RUX was generally well tolerated in this pt population. The 12-mg qd monotherapy dose was not tolerated and caused 2 DLTs. There were no treatment-related fatal events.
    Clinical • P1 data • Metastases
    |
    Jakafi (ruxolitinib) • INCB057643
    3years
    INCB057643 Monotherapy in Patients with Relapsed or Refractory Myelofibrosis: A Phase 1 Study (ASH 2022)
    Treatment with a 4-mg qd dose of INCB057643 monotherapy in this patient population was generally well tolerated, with no treatment-related SAEs, no DLTs, and no TEAEs leading to treatment discontinuation. INCB057643 will be further evaluated at higher doses in dose-escalation and dose-expansion phases as monotherapy and in combination with ruxolitinib in patients with MF (preliminary combination data to be available for presentation).
    Clinical • P1 data
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2)
    |
    Jakafi (ruxolitinib) • INCB057643