235,236 Early human clinical trials have yielded promising findings
Lutathera growing steadily in NETs
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Useful target-engagement readouts may include reduced 1-methylnicotinamide formation, changes in nicotinamide-related metabolites, and confirmation that the selected cellular or tissue model expresses NNMT at a level relevant to the experimental question
For instance, a number of ongoing or completed trials are evaluating inhibitors of the PI3K-AKT-mTOR cascade, such as gedatolisib (NCT03065062) in advanced solid tumors, capivasertib (NCT04305496) in hormone receptor-positive breast cancer, and alpelisib (NCT02437318), which has shown efficacy in advanced breast cancer and is already approved for PIK3CA-mutated cases
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