irx-5183

IRX-5183 is an orally bioavailable, third-generation vitamin A derivative and a highly selective retinoic acid receptor alpha (RARα) agonist with potential antineoplastic activity. It binds to and activates RARα, promoting RARα-mediated signaling that leads to the transcription of genes responsible for cellular differentiation and proliferation. This results in the induction of cellular differentiation and apoptosis, ultimately inhibiting cell proliferation and tumorigenesis. Unlike pan-RAR agonists such as all-trans retinoic acid (ATRA), IRX‑5183 is resistant to stroma-mediated inactivation and does not induce CYP26 expression, which may enhance its bioactivity. It has shown efficacy in preclinical models of acute myeloid leukemia (AML) by decreasing clonogenicity and increasing mature myeloid markers. Clinical development has focused on relapsed or refractory AML and high-risk myelodysplastic syndromes (MDS), with phase I/II trials conducted primarily by Io Therapeutics[1][3][4][5][6].

Other names

367273-07-2