Description of APTO-253 (LOR-253): APTO-253, also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis
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Aptose Biosciences Inc. (NASDAQ: APTO, TSX: APS), a clinical-stage company developing new therapeutics and molecular diagnostics that target the underlying mechanisms of cancer, today announced dosing of the first patient in its Phase 1b clinical study of APTO-253 in patients with relapsed or refractory hematologic malignancies. APTO-253 is a first-in-class inducer of the Krüppel-like factor 4 (KLF4) tumor suppressor gene, and the only clinical-stage compound targeted for patients with suppressed KLF4 levels.
"Epigenetic suppression of the KLF4 gene has been reported as a key transforming event in acute myeloid leukemia and high-risk myelodysplastic syndromes, and Aptose is a pioneer in advancing KLF4 induction as a new therapeutic approach for the treatment of these patient populations," commented William G. Rice, Ph.D., Chairman, President and CEO.
Aptose begins APTO-253 clinical study in patients with relapsed or refractory hematologic malignancies
