AQX-1125, A SHIP1 Activator In Clinical Development For Pulmonary Inflammation: Pharmacokinetics, Metabolism And Tolerability In Healthy Humans Volunteers
B33. ASTHMA THERAPY: NOVEL APPROACHES(2012)
摘要
Rationale: Pharmacological modulation of the phosphoinositide 3-kinase (PI3K)/Akt pathway is an established approach to controlling inflammatory disorders. SH2containing inositol-5'-phosphatase 1 (SHIP1) metabolizes PI(3,4,5)P3 to PI(3,4)P2. SHIP1-deficient mice exhibit pulmonary inflammation, characterized by significant granulocyte recruitment into the lung, while pharmacological SHIP1 activation exerts anti-inflammatory effects in preclinical models of lung inflammation. Here we present an overview of the results of a Phase I study with AQX-1125, a small molecule SHIP1 activator, and compare the pharmacokinetic profile of the compound across three species (human, dog and rat).
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关键词
pulmonary inflammation,ship1 activator,pharmacokinetics
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