INCB059872 + all-trans retinoic acid

A **combination** of INCB059872, an orally bioavailable **lysine-specific demethylase 1 (LSD1) inhibitor** with potential antineoplastic activity, and **all-trans retinoic acid (ATRA, tretinoin)**, a retinoid that modulates gene expression through nuclear retinoic acid receptors (RARs and RXRs). INCB059872 inhibits LSD1, resulting in altered methylation of histone proteins and modulation of gene expression, ultimately inhibiting tumor cell proliferation and promoting tumor suppressor gene expression. ATRA induces cellular differentiation and maturation by binding to retinoic acid receptors and is used clinically in diseases such as acute promyelocytic leukemia; its role in combination therapy aims to enhance differentiation and anti-tumor effects. This combination is being explored for the treatment of advanced hematologic malignancies, notably acute myeloid leukemia.

Brand names

Vesanoid

Other names

1-((4-(methoxymethyl)-4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)cyclobutane-1-carboxylic acidall-trans retinoic acidATRAtretinoin