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• W2892413574 abstract "GNE-617 (N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide) is a potent, selective nicotinamide phosphoribosyltransferase (NAMPT) inhibitor being explored as a potential treatment for human cancers.Plasma clearance was low in monkeys and dogs (9.14 mL min−1 kg−1 and 4.62 mL min−1 kg−1, respectively) and moderate in mice and rats (36.4 mL min−1 kg−1 and 19.3 mL min−1 kg−1, respectively). Oral bioavailability in mice, rats, monkeys and dogs was 29.7, 33.9, 29.4 and 65.2%, respectively.Allometric scaling predicted a low clearance of 3.3 mL min−1 kg−1 and a volume of distribution of 1.3 L kg−1 in human.Efficacy (57% tumor growth inhibition) in Colo-205 CRC tumor xenograft mice was observed at an oral dose of 15 mg/kg BID (AUC = 10.4 µM h).Plasma protein binding was moderately high. GNE-617 was stable to moderately stable in vitro. Main human metabolites identified in human hepatocytes were formed primarily by CYP3A4/5. Transporter studies suggested that GNE-617 is likely a substrate for MDR1 but not for BCRP.Simcyp® simulations suggested a low (CYP2C9 and CYP2C8) or moderate (CYP3A4/5) potential for drug-drug interactions. The potential for autoinhibition was low.Overall, GNE-617 exhibited acceptable preclinical properties and projected human PK and dose estimates." @default.
• W2892413574 created "2018-10-05" @default.
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• W2892413574 date "2019-01-17" @default.
• W2892413574 modified "2023-09-23" @default.
• W2892413574 title "Preclinical assessment of the ADME, efficacy and drug-drug interaction potential of a novel NAMPT inhibitor" @default.
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• W2892413574 doi "https://doi.org/10.1080/00498254.2018.1528407" @default.
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