RGNCY-0026 (AZD6642)

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AZD6642 is a novel FLAP (5-lipoxygenase activating Protein) inhibitor for the long-term treatment of inflammatory diseases. Investigation of the pharmacokinetic and pharmacodynamic relationship based on ex vivo leukotriene B4  (LTB4) levels in dog demonstrated that AZD6642 has high specific potency and low lipophilicity and a selective and metabolically stable profile. The predicted human dose based on rat and dog in vivo PK data is suggested to be in the range of 15− 25 mg once daily dosing for AZD6642. pIC50 hWBfree = 8.3.

Systematic Name: (R)-5-(2-(4-(5-aminopyrazin-2-yl)phenyl)tetrahydrofuran-2-yl)-N-(2-hydroxy-2-methylpropyl)picolinamide

SMILES: O=C(NCC(C)(C)O)C(C=C1)=NC=C1[C@]2(OCCC2)C3=CC=C(C=C3)C4=NC=C(N)N=C4

Chemical Formula: C24H27N5O3

Molecular Weight: 433.51

PMID: 25643210

Reference: Lemurell, Malin, et al. "Discovery of AZD6642, an inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the treatment of inflammatory diseases." Journal of Medicinal Chemistry (2014).

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