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HURA-101 is a potent and selective small molecule delta opioid receptor (DOR) antagonist being developed by TuHURA Biosciences for the treatment of hematological malignancies, including relapsed/refractory acute myeloid leukemia (AML). The compound targets DORs expressed on myeloid immunosuppressive cells, such as tumor-associated macrophages and myeloid-derived suppressive cells (MDSCs), which play pivotal roles in dampening anti-tumor immune responses and promoting tumor progression. Preclinical characterization has shown that HURA-101 possesses sub-nanomolar potency (IC50 = 0.61 nM) and high selectivity for DOR over the mu-opioid receptor (MOR), with the potential to modulate macrophage polarization and signaling molecule secretion in the tumor microenvironment.
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