bomedemstat (MK-3543) / Merck (MSD) 
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  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD), Jakafi (ruxolitinib) / Incyte
    Bomedemstat (MK3543) in Combination with Ruxolitinib in Patients with Advanced Myelofibrosis (Halls G-H (San Diego Convention Center)) -  Nov 6, 2024 - Abstract #ASH2024ASH_5935;    
    P2
    Conclusions These results suggest that the addition of bomedemstat to a ruxolitinib regimen is well tolerated, improves splenomegaly and symptom scores, and stabilizes hemoglobin both in the frontline and second-line setting. ClinicalTrials.gov Identifier : NCT05569538
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD), pinometostat (EPZ-5676) / Ipsen, GSK2879552 / GSK
    The Histone Methyltransferase DOT1L Cooperates with LSD1 to Control Cell Division in Blast-Phase MPN (Halls G-H (San Diego Convention Center)) -  Nov 6, 2024 - Abstract #ASH2024ASH_5912;    
    ClinicalTrials.gov Identifier : NCT05569538 To validate the synthetic lethal interaction between DOT1L and LSD1 we treated DOT1L-ko cells with Bomedemstat or GSK2879552 and discovered a 100-fold increase in drug sensitivity compared to WT cells (MTS-assay)...Consistent with this observation, treatment of the MPN blast-phase cell lines HEL or SET2 with LSD1-inhibitors in combination with the DOT1L-inhibitor EPZ5676 only showed a modest cooperative effect...This cooperation is caused by orchestrated binding of DOT1L and LSD1 at selected enhancer regions and is independent of DOT1L
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    The Transcription Factor IRF8 Regulates the Sensitivity of AML Cells to LSD1 Inhibition and All-Trans Retinoic Acid (Halls G-H (San Diego Convention Center)) -  Nov 6, 2024 - Abstract #ASH2024ASH_5281;    
    Methods : In murine retrovirally-induced AML cells (Hoxa9-Meis1, H9M; MN1) treated with LSD1 inhibitor (Bomedemstat) and ATRA, we assessed proliferation via the methoxynitrosulfophenyl-tetrazolium carboxanilide (XTT) assay, and the differentiation effect by flow cytometry...Conclusion : In summary, we found that IRF8 expression modulates the response of AML cells to both LSD1 inhibition and ATRA. These findings suggest IRF8 expression is a potential biomarker for selecting patients for treatment with an LSD1 inhibitor and ATRA.
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Phase 3 study of the lysine-specific demethylase 1 (LSD1) inhibitor bomedemstat in patients with essential thrombocythemia (ET). (Hall A; Poster Bd #: 149b) -  Apr 24, 2024 - Abstract #ASCO2024ASCO_1231;    
    P3
    Patients will be randomly assigned 1:1 to bomedemstat 50 mg/day by mouth (starting dose) or investigator's choice of best available therapy (anagrelide, busulfan, interferon alfa/pegylated interferon alpha, or ruxolitinib)...Exploratory end points include pharmacokinetics, the proportion of patients reporting stability or improvement versus decline on the MSAF v4.0 and PROMIS Fatigue SF-7a domains, and molecular biomarkers. Approximately 300 patients will be enrolled.
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Enrollment closed, Trial primary completion date:  A Study of Bomedemstat (MK-3543) in Participants With Polycythemia Vera (MK-3543-004) (clinicaltrials.gov) -  Mar 29, 2024   
    P2,  N=20, Active, not recruiting, 
    Recruiting --> Suspended Recruiting --> Active, not recruiting | Trial primary completion date: Apr 2025 --> Jan 2025
  • ||||||||||  Review, Journal, Combination therapy:  Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy. (Pubmed Central) -  Jan 26, 2024   
    Herein, we present a comprehensive overview of the combination of LSD1 inhibitors with various antitumor agents, as well as LSD1 multitarget inhibitors. Additionally, the challenges and future research directionsare also discussed, and we hope this review will provide new insight into the development of LSD1-targeted anticancer agents.
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Trial completion date, Trial primary completion date:  A Study of Bomedemstat (MK-3543) in Participants With Polycythemia Vera (MK-3543-004) (clinicaltrials.gov) -  Jan 12, 2024   
    P2,  N=20, Recruiting, 
    Additionally, the challenges and future research directionsare also discussed, and we hope this review will provide new insight into the development of LSD1-targeted anticancer agents. Trial completion date: Aug 2025 --> Apr 2025 | Trial primary completion date: Aug 2025 --> Apr 2025
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Trial completion date, Trial primary completion date:  A Study of Bomedemstat (MK-3543) in Participants With Polycythemia Vera (MK-3543-004) (clinicaltrials.gov) -  Nov 15, 2023   
    P2,  N=20, Recruiting, 
    Not yet recruiting --> Recruiting Trial completion date: Feb 2025 --> Aug 2025 | Trial primary completion date: Feb 2025 --> Aug 2025
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Trial completion date, Trial primary completion date:  IMG-7289 in Patients With Essential Thrombocythemia (ET) or Polycythemia Vera (PV) (clinicaltrials.gov) -  Nov 3, 2023   
    P2,  N=24, Recruiting, 
    Trial primary completion date: Aug 2028 --> Aug 2026 Trial completion date: Oct 2024 --> Oct 2025 | Trial primary completion date: Oct 2023 --> Oct 2024
  • ||||||||||  Venclexta (venetoclax) / Roche, AbbVie, Walter and Eliza Hall Institute
    LSD1 Inhibition Synergizes with Venetoclax in Acute Myeloid Leukemia By Targeting Cellular Metabolism (SDCC - Halls G-H) -  Nov 3, 2023 - Abstract #ASH2023ASH_5585;    
    It significantly reduced the leukemic burden in PDX AML models and synergistically downregulated cellular energy metabolism. These findings suggest that combining venetoclax with LSD1 inhibition holds promise as a combination treatment in AML and warrants further clinical investigation.
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD), rusfertide (PTG-300) / Protagonist Therap, bezuclastinib (PLX9486) / Cogent Biosci
    634. Myeloproliferative Syndromes - Clinical and Epidemiological - Treatment and Outcomes in MPNs (Ballroom 20CD (San Diego Convention Center)) -  Nov 3, 2023 - Abstract #ASH2023ASH_4867;    
    In mastocytosis, the KIT inhibitor bezuclastinib shows efficacy and safety in patients with indolent mastocytosis. In myeloid neoplasms with eosinophilia, a custom NGS panel is used to explore the molecular landscape in patients negative for tyrosine kinase fusion genes, identifying recurrent JAK/STAT mutations associated with response to JAK inhibitors.
  • ||||||||||  Review, Journal:  Lysine-Specific Demethylase 1 (LSD1) Inhibitors: Peptides as an Emerging Class of Therapeutics. (Pubmed Central) -  Oct 9, 2023   
    Moreover, numerous reversible inhibitors for LSD1 have been reported in the literature, including clinical candidates CC-90011 (pulrodemstat) and SP-2577 (seclidemstat)...For the first time, we comprehensively organized the peptide-based LSD1 inhibitors from the design strategy. Peptide inhibitors of LSD1 are classified as H3 peptide and SNAIL1 peptide derivatives, along with miscellaneous peptides that include naturally occurring LSD1 inhibitors.
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Trial completion date, Trial primary completion date:  A Study of Bomedemstat (MK-3543) in Participants With Polycythemia Vera (MK-3543-004) (clinicaltrials.gov) -  Oct 2, 2023   
    P2,  N=20, Recruiting, 
    Peptide inhibitors of LSD1 are classified as H3 peptide and SNAIL1 peptide derivatives, along with miscellaneous peptides that include naturally occurring LSD1 inhibitors. Trial completion date: Aug 2024 --> Feb 2025 | Trial primary completion date: Aug 2024 --> Feb 2025
  • ||||||||||  MODULE 3: Future Directions in the Management of MF (LEVEL 3, MEAL THEATER 1; Virtual) -  Aug 11, 2023 - Abstract #SOHO2023SOHO_338;    
    This activity is supported through independent medical education grants from Bristol Myers Squibb, CTI Biopharma Corp, and GlaxoSmithKline. Mechanism of antitumor activity of navitoclax and biological rationale for its evaluation in patients with MF, Published research with navitoclax alone and in combination with ruxolitinib for MF; ongoing Phase III studies, Rationale for the inhibition of BET proteins in patients with MF; mechanisms of action of pelabresib and BMS-986158, Early clinical trial findings and ongoing research with BET inhibitors as monotherapy and in combination with JAK2 inhibitors for MF, Mechanism of action of, available data with and ongoing evaluation of luspatercept as monotherapy or combined with a JAK2 inhibitor for patients with MF and anemia; current role, if any, Published activity and safety data with and ongoing investigation of other novel agents and strategies (eg, bomedemstat, zilurgisertib, selinexor, navtemadlin) in MF,
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Trial primary completion date:  A Study of Bomedemstat (MK-3543) in Participants With Polycythemia Vera (MK-3543-004) (clinicaltrials.gov) -  Aug 9, 2023   
    P2,  N=20, Recruiting, 
    Mechanism of antitumor activity of navitoclax and biological rationale for its evaluation in patients with MF, Published research with navitoclax alone and in combination with ruxolitinib for MF; ongoing Phase III studies, Rationale for the inhibition of BET proteins in patients with MF; mechanisms of action of pelabresib and BMS-986158, Early clinical trial findings and ongoing research with BET inhibitors as monotherapy and in combination with JAK2 inhibitors for MF, Mechanism of action of, available data with and ongoing evaluation of luspatercept as monotherapy or combined with a JAK2 inhibitor for patients with MF and anemia; current role, if any, Published activity and safety data with and ongoing investigation of other novel agents and strategies (eg, bomedemstat, zilurgisertib, selinexor, navtemadlin) in MF, Trial primary completion date: Dec 2024 --> Aug 2024
  • ||||||||||  Current and Emergent Therapies for ET (Level 3, Room 332C) -  Jun 21, 2023 - Abstract #SOHO2023SOHO_23;    
    P1, P1/2,
    Trial completion date: Jan 2024 --> Jan 2025 | Trial primary completion date: Jan 2023 --> Jan 2024 HU and Peg-IFN were compared in a phase 3 study (MPD-RC 112) in patients with ET and polycythemia vera (PV), which resulted in similar rates of complete response and thrombotic events at 12 months.7 With longer treatment, Peg-IFN has demonstrated improved molecular responses in both ET and PV, though the clinical implications of molecular response in these settings are not yet clear.7
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD)
    Enrollment closed, Trial completion date, Trial primary completion date:  Extension Study of Bomedemstat (IMG-7289/MK-3543) in Participants With Myeloproliferative Neoplasms (IMG-7289-CTP-202/MK-3543-005) (clinicaltrials.gov) -  Jun 1, 2023   
    P2,  N=80, Active, not recruiting, 
    HU and Peg-IFN were compared in a phase 3 study (MPD-RC 112) in patients with ET and polycythemia vera (PV), which resulted in similar rates of complete response and thrombotic events at 12 months.7 With longer treatment, Peg-IFN has demonstrated improved molecular responses in both ET and PV, though the clinical implications of molecular response in these settings are not yet clear.7 Enrolling by invitation --> Active, not recruiting | Trial completion date: Dec 2026 --> Dec 2024 | Trial primary completion date: Dec 2025 --> Dec 2024
  • ||||||||||  bomedemstat (MK-3543) / Merck (MSD), Jakafi (ruxolitinib) / Novartis, Incyte
    Enrollment change, Combination therapy:  Bomedemstat (IMG-7289) Plus Ruxolitinib for Myelofibrosis (clinicaltrials.gov) -  May 23, 2023   
    P2,  N=40, Recruiting, 
    Enrolling by invitation --> Active, not recruiting | Trial completion date: Dec 2026 --> Dec 2024 | Trial primary completion date: Dec 2025 --> Dec 2024 N=20 --> 40
  • ||||||||||  Review, Journal:  Recent advances of LSD1/KDM1A inhibitors for disease therapy. (Pubmed Central) -  Apr 5, 2023   
    The influence of the stereochemistry on the potency against LSD1 and its homolog LSD2 is briefly discussed. Finally, the challenges and prospects of LSD1-targeted drug discovery are also given.