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Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well‐Controlled Asthma PDF
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Published on 2017 by

Abstract: BI 1021958, a novel antagonist of the chemoattractant‐receptor‐homologous molecule (CRTH2), targets airway inflammation in asthma by inhibiting prostaglandin binding to CRTH2 receptors. Two phase 1 studies assessed BI 1021958 safety/tolerability and pharmacokinetics (PK)/pharmacodynamics (PD) following single doses in healthy men and multiple doses in men/women with well‐controlled asthma. Studies 1 had 2 parts: a placebo‐controlled, fixed‐sequence, single‐blind, single‐rising‐dose part (n = 56) and a randomized, 2‐way crossover, open‐label, repeated‐dose part studying the food effect on PK/PD (n = 12). Study 2 was a placebo‐controlled, single‐center, double‐blind multiple‐rising‐dose study (n = 84). Primary end points were safety/tolerability and PK/PD (both studies); secondary end points were eosinophil shape change (ESC; study 1) and dose proportionality/linearity following first dose and at steady state (study 2). BI 1021958 was adequately tolerated in both studies; adverse events were infrequent, generally mild to moderate, and occurred similarly in treatment groups. Maximum measured concentration (Cmax ) was achieved in ≤2.5 hours in study 1 and ≤2.0 hours in study 2. BI 1021958 exposure increased proportionally with dose. In study 1, following a single 60‐mg dose, AUC parameters and Cmax were 20% and 15% lower, respectively, after a high‐fat meal compared with the fasted state. After ≥60‐mg single doses (study 1) and \u003e40‐mg multiple doses (study 2), \u003e95% ESC inhibition was observed for ≥24 hours. PK/PD was similar in healthy subjects and subjects with well‐controlled asthma. Data support further investigation of CRTH2 antagonists for the treatment of asthma.

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Download Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well‐Controlled Asthma PDF Free

Download Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well‐Controlled Asthma Books Free

Download Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well‐Controlled Asthma Free

Download Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well‐Controlled Asthma PDF

Download Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel CRTH2 Antagonist BI 1021958 at Single Oral Doses in Healthy Men and Multiple Oral Doses in Men and Women With Well‐Controlled Asthma Books