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QTX3046 is a potent, selective, and orally bioavailable non-covalent small molecule inhibitor that targets the KRAS G12D mutation. It acts as a dual ON/OFF state allosteric inhibitor of KRAS G12D, meaning it can inhibit both the active (GTP-bound) and inactive (GDP-bound) forms of the mutant protein. The drug is brain-penetrant and is being developed for use in patients with advanced solid tumors harboring KRAS G12D mutations. Clinical trials are evaluating its safety, tolerability, pharmacokinetics, and antitumor activity as monotherapy and in combination with cetuximab. Indications under investigation include colorectal cancer, pancreatic cancer, lung cancer, endometrial cancer, and other solid tumors with KRAS G12D mutations[1][3][5][7].
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