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    DRUG CLASS:

    LSD1 inhibitor

    Related drugs:
    5d
    Iadademstat With Hypomethylating Agent in Patients With Myelodysplastic Syndrome (clinicaltrials.gov)
    P1, N=12, Recruiting, Medical College of Wisconsin | Trial completion date: Oct 2027 --> Dec 2027 | Trial primary completion date: Oct 2026 --> Dec 2026
    Trial completion date • Trial primary completion date
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    iadademstat (ORY-1001)
    5d
    NCI-2020-14163: Seclidemstat and Azacitidine for the Treatment of Myelodysplastic Syndrome or Chronic Myelomonocytic Leukemia (clinicaltrials.gov)
    P1/2, N=24, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting | N=44 --> 24
    Enrollment closed • Enrollment change
    |
    TP53 (Tumor protein P53) • NRAS (Neuroblastoma RAS viral oncogene homolog) • RUNX1 (RUNX Family Transcription Factor 1) • ASXL1 (ASXL Transcriptional Regulator 1) • SETBP1 (SET Binding Protein 1)
    |
    TP53 mutation • NRAS mutation • ASXL1 mutation
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    azacitidine • seclidemstat (SP2577)
    6d
    Uncovering BAP1 deubiquitination landscape enhances mechanism elucidation and therapeutic precision for BAP1-deficient pancancers. (PubMed, Sci Transl Med)
    Combined inhibition of LSD1 and PARP1, using SP2509/SP2577 and olaparib, respectively, synergistically hinders NER, induces apoptosis, reduces tumor burden, and prolongs the survival of multiple BAP1-deficient pancancer in vitro models and in vivo xenografts. In conclusion, our results provide a deubiquitination landscape of BAP1; elucidate the mechanisms of action of BAP1, LSD1, and PARP1 in pancancers; and describe a promising combination therapeutic strategy applicable across multiple cancers with BAP1 mutations.
    Journal • BRCA Biomarker • PARP Biomarker • Pan tumor
    |
    BAP1 (BRCA1 Associated Protein 1) • DDB1 (Damage Specific DNA Binding Protein 1) • RAD23B (RAD23 Homolog B)
    |
    BRCA1 mutation
    |
    Lynparza (olaparib) • seclidemstat (SP2577) • SP-2509
    13d
    LSD1 inhibitor, TAS1440, disrupts INSM1-LSD1 complex activating tumor-suppressive pathways via transcriptional reprogramming in neuroendocrine SCLC. (PubMed, Nat Commun)
    Loss of LSD1 enzymatic activity or INSM1 knockout abrogated TAS1440 effects, defining its mode of action and chemoresistance. These findings support TAS1440 as a next-generation epigenetic therapy candidate for INSM1-high SCLC-A.
    Journal
    |
    TGFB1 (Transforming Growth Factor Beta 1) • ASCL1 (Achaete-Scute Family BHLH Transcription Factor 1) • SMAD2 (SMAD Family Member 2)
    1m
    Phase 2 study of the lysine-specific demethylase 1 (LSD1) inhibitor bomedemstat for essential thrombocythemia. (PubMed, Blood Adv)
    Bomedemstat had clinically relevant activity and manageable safety in participants with ET. Registration: NCT04254978 (Study of Bomedemstat in Participants With Essential Thrombocythemia [IMG-7289-CTP-201/MK-3543-003]).
    P2 data • Journal
    |
    JAK2 (Janus kinase 2) • CALR (Calreticulin)
    |
    bomedemstat (MK-3543)
    1m
    MK-3453-023: A Study of Bomedemstat (MK-3543) in Participants With Mild or Moderate Hepatic Impairment (MK-3543-023) (clinicaltrials.gov)
    P1, N=9, Completed, Merck Sharp & Dohme LLC | Active, not recruiting --> Completed | N=24 --> 9
    Trial completion • Enrollment change
    |
    bomedemstat (MK-3543)
    1m
    CL06-ORY-1001: Phase 2 Study of iadademstat for the treatment of patients with essential thrombocythemia resistant/intolerant to hydroxyurea. (2025-523864-19-00)
    P1/2, N=36, Not yet recruiting, Oryzon Genomics S.A.
    New P1/2 trial
    |
    JAK2 (Janus kinase 2)
    |
    iadademstat (ORY-1001) • hydroxyurea
    2ms
    Bomedemstat (IMG-7289) in Combination With Momelotinib in Patients With Myelofibrosis (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, United Lincolnshire Hospitals NHS Trust
    New P2 trial
    |
    Ojjaara (momelotinib) • bomedemstat (MK-3543)
    2ms
    Therapeutic advances in acute myeloid leukemia: from LSD1 blockade to PROTAC-based strategies. (PubMed, Ann Med Surg (Lond))
    Several PROTAC therapies are now in AML trials. LSD1-targeted degradation is promising, but further research is needed to confirm its safety, overcome resistance, and identify optimal drug combinations for AML treatment.
    Journal
    |
    KDM1A (Lysine Demethylase 1A)
    |
    bomedemstat (MK-3543)
    2ms
    MK-3453-023: A Study of Bomedemstat (MK-3543) in Participants With Mild or Moderate Hepatic Impairment (MK-3543-023) (clinicaltrials.gov)
    P1, N=24, Active, not recruiting, Merck Sharp & Dohme LLC | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    bomedemstat (MK-3543)
    3ms
    TIARA: Iadademstat + SBRT With Atezo in ES-SCLC (clinicaltrials.gov)
    P1, N=15, Recruiting, Yale University | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Tecentriq (atezolizumab) • iadademstat (ORY-1001)