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JBI-802 is a first-in-class, orally administered, small-molecule dual inhibitor targeting two epigenetic regulators within the CoREST (Co-repressor of Repressor Element-1 Silencing Transcription) complex—Lysine-specific histone demethylase 1A (LSD1/KDM1A) and Histone deacetylase 6 (HDAC6). By inhibiting both LSD1 and HDAC6, JBI-802 modulates stem cell function and immune suppression. This dual inhibition leads to chromatin remodeling, altered gene expression favoring tumor suppressor genes, and induction of apoptosis in tumor cells overexpressing these targets. Preclinical studies have shown that JBI-802 can resensitize immunotherapy-resistant tumors and demonstrates synergistic anti-tumor activity superior to single-target inhibition. The drug is being developed by Jubilant Therapeutics for hematological malignancies such as acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), essential thrombocythemia, as well as solid tumors including small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), neuroendocrine tumors, and other advanced solid tumors.
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