RGD Reference Report - Prolonged bronchoprotection against inhaled methacholine by inhaled BI 1744, a long-acting beta(2)-agonist, in patients with mild asthma. - Rat Genome Database

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Prolonged bronchoprotection against inhaled methacholine by inhaled BI 1744, a long-acting beta(2)-agonist, in patients with mild asthma.

Authors: O'Byrne, PM  Van der Linde, J  Cockcroft, DW  Gauvreau, GM  Brannan, JD  Fitzgerald, M  Watson, RM  Milot, J  Davis, B  O'Connor, M  Hart, L  Korducki, L  Hamilton, AL  Boulet, LP 
Citation: O'Byrne PM, etal., J Allergy Clin Immunol. 2009 Dec;124(6):1217-21.
RGD ID: 4145105
Pubmed: PMID:20004781   (View Abstract at PubMed)
DOI: DOI:10.1016/j.jaci.2009.08.047   (Journal Full-text)

BACKGROUND: Long-acting ss(2)-agonists are an established controller medication in asthma. BI 1744 is a novel L\long-acting ss(2)-agonist with a preclinical profile that suggests 24-hour bronchodilation and bronchoprotection may be achieved. OBJECTIVE: To examine the bronchoprotective effects of single doses of BI 1744 against methacholine provocation in subjects with mild asthma. METHODS: Thirty-one subjects with mild asthma were randomized to receive single doses of BI 1744 (2, 5, 10, 20 microg) or placebo on separate days according to a double-blind, 5-way crossover design. Methacholine challenges were performed at 30 minutes and at 4, 8, 24, and 32 hours after each single dose of medication, and the results were expressed as PC(20) FEV(1). RESULTS: All doses of BI 1744 produced statistically significant increases in the methacholine PC(20) compared with placebo as long as 32 hours. The mean (geometric SEM) methacholine PC(20) 24 hours after dosing with placebo was 1.73 (1.13) mg/mL, which increased after 2 microg to 3.86 (1.14) mg/mL, after 5 microg to 5.67 (1.14) mg/mL, after 10 microg to 9.42 (1.13) mg/mL, and after 20 microg to 13.71 (1.14) mg/mL (all P < .0001). After 32 hours, the methacholine PC(20) value remained significantly increased for all doses. No safety or tolerability concerns were identified. CONCLUSION: BI 1744 provides significant bronchoprotection against inhaled methacholine for up to 32 hours after single-dose administration.

RGD Manual Disease Annotations    Click to see Annotation Detail View
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
asthma  IDA 4145105 RGD 
asthma  ISOADRB2 (Homo sapiens)4145105; 4145105 RGD 

Objects Annotated

Genes (Rattus norvegicus)
Adrb2  (adrenoceptor beta 2)

Genes (Mus musculus)
Adrb2  (adrenergic receptor, beta 2)

Genes (Homo sapiens)
ADRB2  (adrenoceptor beta 2)


Additional Information