AZD9898

AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Gutathione S-transferase

Research Areas >> Inflammation/Immunology

IC50: 0.28 nM (LTC4S)[1].

AZD9898 with the single dose of 100 mg/kg is well tolerated and no safety concerns are raised[1]. Animal Model: Rat 6M/group[1]. Dosage: 10 and 100 mg/kg (for Toxicology Study). Administration: Sing oral dose. Result: Showed no signs of testicular toxicity, and only adaptive changes in the liver due to cytochrome P450 induction which were not judged adverse, providing a 200 fold margin between the no adverse effect level and the predicted human exposure at the predicted therapeutic dose.

[1]. Munck Af Rosenschöld M, et al. Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1S,2S)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma. J Med Chem. 2019 Aug 30.