REC-4539

REC-4539 is a novel, reversible, and CNS-penetrant small molecule inhibitor of lysine-specific histone demethylase 1 (LSD1/KDM1A), developed by Recursion. It is the first LSD1 inhibitor specifically designed to cross the blood-brain barrier and act reversibly. The drug is being developed for oncology indications with a primary focus on small-cell lung cancer (SCLC), where brain metastases are common and current therapies have limited efficacy in the central nervous system. REC-4539’s selectivity and reversible mechanism aim to reduce adverse events such as thrombocytopenia that are associated with other LSD1 inhibitors. Preclinical studies have demonstrated dose-dependent tumor inhibition in SCLC models—including brain penetration—and limited impact on platelet levels. The agent also has a favorable pharmacokinetic profile with a shorter half-life compared to other drugs in its class. In addition to SCLC, development efforts include acute myeloid leukemia (AML) and potentially other solid tumors[1][2][3][4][5][6][7].

Other names

EXS74539EXS-74539EXS 74539'539REC-4539REC4539REC 4539