Olodaterol - CAS 868049-49-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Adrenergic Receptor
Olodaterol, also referred to BI1744, is a long acting β2-agonist (β2-ARs; EC50s = 97.7 and 2,725 nM for human β2- and β1-ARs, respectively) used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim.
Brife Description:
A long acting beta-adrenoceptor agonist (EC50= 1.4±0.08 Nm)
Related CAS:
869477-96-3 (HCl)
6-hydroxy-8-[(1R)-1-hydroxy-2-[[1-(4-methoxyphenyl)-2-methylpropan-2-yl]amino]ethyl]-4H-1,4-benzoxazin-3-one; 6-hydroxy-8-(1-hydroxy-2-((2-(4-methoxyphenyl)-1,1-dimethylethyl)amino)ethyl)-2H-1,4-benzoxazin-3(4H)-one; BI 1744 CL; BI-1744 CL; olodaterol; Striverdi; Respimat
H2O: 6.2 mg/mL
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
649.0±55.0 ℃ at 760 Torr
1.250±0.06 g/cm3
Canonical SMILES:
1.Efficacy of tiotropium-olodaterol fixed-dose combination in COPD.
Derom E;Brusselle GG;Joos GF Int J Chron Obstruct Pulmon Dis. 2016 Dec 13;11:3163-3177. doi: 10.2147/COPD.S92840. eCollection 2016.
Tiotropium-olodaterol, formulated in the Respimat soft-mist inhaler, is an inhaled fixed-dose combination (FDC) of a long-acting muscarinic antagonist (LAMA) and a long-acting β;2;-agonist (LABA), commercialized under the name of Spiolto or Stiolto. The efficacy of tiotropium-olodaterol 5-5 μg once daily in adult patients with COPD was documented in eleven large, multicenter trials of up to 52 weeks duration. Tiotropium-olodaterol 5-5 μg not only improved spirometric values to a significantly greater extent than placebo but also resulted in statistically significant beneficial effects on dyspnea, markers of hyperinflation, use of rescue medication, health-related quality of life, and exercise endurance. Improvements exceeded the minimal clinically important difference (MCID) for forced expiratory volume in 1 second (FEV;1;), dyspnea, and quality of life. Differences between tiotropium-olodaterol 5-5 μg and the respective monocomponents were statistically significant for FEV;1;, dyspnea, markers of hyperinflation, use of rescue medication, and health-related quality of life, but did not reach the MCID. However, dual bronchodilatation significantly increased the number of patients who exceeded the MCID for dyspnea and quality of life.
2.Bronchodilating drugs for chronic obstructive pulmonary disease: current status and future trends.
Montuschi P;Ciabattoni G J Med Chem. 2015 May 28;58(10):4131-64. doi: 10.1021/jm5013227. Epub 2015 Feb 9.
Inhaled bronchodilators, including long-acting muscarinic receptor antagonists (LAMA) and long-acting β2-adrenoreceptor agonists (LABA), are the mainstay of pharmacological treatment of stable chronic obstructive pulmonary disease (COPD). Among approved LAMA, tiotropium bromide, glycopyrronium bromide, and umeclidinium bromide are administered once daily, whereas aclidinium bromide is administered every 12 h. New LAMA are under development for COPD. Among the approved LABA, indacaterol has a 24 h duration of action, whereas salmeterol and formoterol require twice-daily administration. New once-daily LABA, including vilanterol, olodaterol, milveterol, carmoterol, and abediterol, are in development. LAMA/LABA fixed dose combinations (FDCs) provide the convenience of two bronchodilators with different mechanism of action in a single inhaler. Indacaterol/glycopyrronium, umeclidinium/vilanterol, and olodaterol/tiotropium FDCs have been approved or are under approval and are likely to become a standard pharmacological strategy for COPD. Inhaled dual-pharmacology compounds, combining muscarinic antagonism and β2-agonism (MABA) in a single molecule, potentially provide additive or synergistic bronchodilation over either inhaled antimuscarinic or β2-agonist monotherapy.
3.Clinicopharmacological profile of the fixed-dose combination of aclidinium bromide and formoterol fumarate in the management of chronic obstructive pulmonary disease.
Babu KS;Morjaria JB Ther Adv Respir Dis. 2015 Apr;9(2):56-68. doi: 10.1177/1753465815575254. Epub 2015 Mar 9.
The recent Global Initiative for Chronic Obstructive Lung Disease (GOLD) chronic obstructive pulmonary disease (COPD) guidelines consider symptoms and exacerbation history in addition to the degree of airflow obstruction for classifying patients. The improvement of symptoms is principally provided by bronchodilators, using β2 agonists and antimuscarinic agents. Aclidinium bromide is a novel long-acting antimuscarinic agent licensed for use in patients with COPD. Novel fixed-dose combinations that are either licensed or in their late phase of development include vilanterol/umeclidinium, indacaterol/glycopyrronium, olodaterol/tiotropium and formoterol/aclidinium. Fixed-dose combinations of aclidinium/formoterol have been evaluated in COPD patients and evidence suggests that this is efficacious, safe, has a quick onset of action and is well tolerated. This review provides a clinico-pharmacological profile of this compound.
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CAS 868049-49-4 Olodaterol

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