Quinolines are an important class of biologically active heterocyclic compounds, and their derivatives usually exhibit a variety of biological activities. They can be used as antimalarial drugs and in the preparation of other antimalarial drugs. Other important activities of quinoline derivatives include inhibitory activity against EGFR-TK and antipsychotic activity. Futhermore, quinoline scaffolds are present in various drug molecules, including the antimalarial drugs aablaquine, chloroquine, mefloquine and primaquine, and the antibacterial agents gatifloxacin, levofloxacin, and moxifloxacin.
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XRad Therapeutics announced that the first patient has been dosed in the company’s Phase 1a trial evaluating XRD-0394 in combination with radiation therapy for the treatment of metastatic, locally-advanced or recurrent solid tumors.
XRD-0394, is a first-in-class dual inhibitor of ataxia-telangiectasia mutated (ATM) and DNA-dependent protein kinase (DNA-PK). Initial development efforts are focused on evaluating XRD-0394’s ability to enhance radiation therapy when used in combination. In parallel, the company is exploring the potential benefits of using XRad’s dual kinase inhibitors in combination with targeted radionuclides, immune checkpoint inhibitors, polyadenosine diphosphate-ribose polymerase inhibitors and antibody drug conjugates.