Indacaterol

Last updated
Indacaterol
Indacaterol structure.svg
Indacaterol ball-and-stick model.png
Clinical data
Trade names Onbrez, Arcapta
AHFS/Drugs.com International Drug Names
License data
Pregnancy
category
  • AU:B3
Routes of
administration
Inhalation
ATC code
Legal status
Legal status
Identifiers
  • 5-[2-[(5,6-Diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.218.577 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C24H28N2O3
Molar mass 392.499 g·mol−1
3D model (JSmol)
  • O=C4/C=C\c1c(c(O)ccc1[C@@H](O)CNC3Cc2cc(c(cc2C3)CC)CC)N4
  • InChI=1S/C24H28N2O3/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29)/t22-/m0/s1 Yes check.svgY
  • Key:QZZUEBNBZAPZLX-QFIPXVFZSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Indacaterol is an ultra-long-acting beta-adrenoceptor agonist [5] developed by Novartis. It needs to be taken only once a day, [6] unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD) (long-term data in patients with asthma are thus far lacking). It is delivered as an aerosol formulation through a dry powder inhaler.

Contents

Medical uses

A Cochrane review found benefit in lung function in people with COPD at least as good as that seen with twice-daily long-acting beta2-agonists. [7]

History

It was approved by the European Medicines Agency (EMA) under the brand name Onbrez Breezhaler on November 30, 2009, [8] and by the United States Food and Drug Administration (FDA), under the brand name Arcapta Neohaler, on July 1, 2011. [9] [10] In 2016, Novartis licensed its U.S. commercial rights for Arcapta Neohaler to Sunovion Pharmaceuticals. [11]

Related Research Articles

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Budesonide/formoterol, sold under the brand name Symbicort among others, is a fixed-dose combination medication used in the management of asthma or chronic obstructive pulmonary disease (COPD). It contains budesonide, a steroid and formoterol, a long-acting β2-agonist (LABA). The product monograph does not support its use for sudden worsening or treatment of active bronchospasm. However, a 2020 review of the literature does support such use. It is used by breathing in the medication.

<span class="mw-page-title-main">Formoterol</span> Chemical compound

Formoterol, also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4 h to 6 h. Formoterol has a relatively rapid onset of action compared to other LABAs, and is effective within 2-3 minutes. The 2022 Global Initiative for Asthma report recommends a combination formoterol/inhaled corticosteroid inhaler as both a preventer and reliever treatment for asthma in adults. In children, a short-actingβ2 agonist is still recommended.

<span class="mw-page-title-main">Glycopyrronium bromide</span> Chemical compound

Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has few to no central effects. It is given by mouth, via intravenous injection, on the skin, and via inhalation. It is a synthetic quaternary ammonium compound. The cation, which is the active moiety, is called glycopyrronium (INN) or glycopyrrolate (USAN).

Beta<sub>2</sub>-adrenergic agonist Compounds that bind to and activate adrenergic beta-2 receptors

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<span class="mw-page-title-main">Long-acting beta-adrenoceptor agonist</span> Drug prescribed for asthma patients

Long-acting β adrenoceptor agonists are usually prescribed for moderate-to-severe persistent asthma patients or patients with chronic obstructive pulmonary disease (COPD). They are designed to reduce the need for shorter-acting β2 agonists such as salbutamol (albuterol), as they have a duration of action of approximately 12 hours in comparison with the 4-to-6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol, long-acting β2 agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β2 receptors in the smooth muscle in the lungs.

<span class="mw-page-title-main">Roflumilast</span> Medication

Roflumilast, sold under the brand name Daxas among others, is a medication that acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). It has anti-inflammatory effects and is used as an orally administered drug for the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease (COPD).

<span class="mw-page-title-main">Fluticasone furoate</span> Chemical compound

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<span class="mw-page-title-main">Tiotropium bromide</span> Long-acting bronchodilator in the maintenance of COPD and asthma

Tiotropium bromide, sold under the brand name Spiriva among others, is a long-acting bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma. Specifically it is used during periods of breathing difficulty to prevent them from getting worse, rather than to prevent them from happening. It is used by inhalation through the mouth. Onset typically begins within half an hour and lasts for 24 hours.

<span class="mw-page-title-main">Olodaterol</span> Chemical compound

Olodaterol is an ultra-long-acting β adrenoreceptor agonist (ultra-LABA) used as an inhalation for treating people with chronic obstructive pulmonary disease (COPD). It is manufactured by Boehringer Ingelheim.

<span class="mw-page-title-main">Vilanterol</span> Asthma drug – β2 adrenoreceptor agonist

Vilanterol is an ultra-long-acting β2 adrenoreceptor agonist (ultra-LABA), which was approved in May 2013 in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).. The combination is also approved for the treatment of asthma in Canada, Europe, Japan and New Zealand.

<span class="mw-page-title-main">Fluticasone furoate/vilanterol</span> Pharmaceutical drug formulation

Fluticasone furoate/vilanterol (FF/VI), sold under the brand name Breo Ellipta among others, is a combination medication for the treatment of chronic obstructive pulmonary disease (COPD) and asthma. It contains fluticasone furoate, an inhaled corticosteroid, and vilanterol, an ultra-long-acting β2 agonist (ultra-LABA).

<span class="mw-page-title-main">Umeclidinium bromide/vilanterol</span> Pharmaceutical drug

Umeclidinium bromide/vilanterol, sold under the brand name Anoro Ellipta, among others, is a fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It is administered by inhalation.

<span class="mw-page-title-main">Indacaterol/glycopyrronium bromide</span> Combination drug

Indacaterol/glycopyrronium bromide, sold under the brand name Ultibro Breezhaler among others, is a fixed-dose combination medication for inhalation consisting of the following two active ingredients:

Aclidinium bromide/formoterol, sold under the brand names Duaklir and Brimica, is a fixed-dose combination medication for inhalation, used in the management of chronic obstructive pulmonary disease (COPD). It consists of aclidinium bromide, a long-acting muscarinic antagonist, and formoterol, a long-acting β2 agonist.

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Fluticasone furoate/umeclidinium bromide/vilanterol, sold under the brand name Trelegy Ellipta among others, is a fixed-dose combination inhaled medication that is used for the maintenance treatment of chronic obstructive pulmonary disease (COPD). The medications work in different ways: fluticasone furoate is an inhaled corticosteroid (ICS), umeclidinium is a long-acting muscarinic antagonist (LAMA), and vilanterol is a long-acting beta-agonist (LABA).

Glycopyrronium bromide/formoterol, sold under the brand name Bevespi Aerosphere, is a combination medication for the maintenance treatment of chronic obstructive pulmonary disease (COPD). It is a combination of glycopyrronium bromide and formoterol. It is inhaled.

Indacaterol/mometasone, sold under the brand name Atectura Breezhaler among others, is a fixed-dose combination medication for the treatment of asthma in adults and adolescents twelve years of age and older not adequately controlled with inhaled corticosteroids and inhaled short acting beta2 agonists.

Indacaterol/glycopyrronium bromide/mometasone, sold under the brand name Enerzair Breezhaler among others, is an inhalable fixed-dose combination medication for the treatment of asthma. It contains indacaterol as acetate, glycopyrronium bromide, and mometasone furoate.

Budesonide/glycopyrronium bromide/formoterol, sold under the brand name Breztri Aerosphere among others, is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It contains budesonide, glycopyrronium bromide, and formoterol fumarate dihydrate. It is inhaled.

References

  1. "Arcapta Neohaler (indacaterol) inhalation powder Initial U.S. Approval: 2011". DailyMed. 1 April 2020. Retrieved 14 June 2021.
  2. "Onbrez Breezhaler EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 20 January 2021.
  3. "Oslif Breezhaler EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 20 January 2021.
  4. "Hirobriz Breezhaler EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 20 January 2021.
  5. Cazzola M, Matera MG, Lötvall J (July 2005). "Ultra long-acting beta 2-agonists in development for asthma and chronic obstructive pulmonary disease". Expert Opin Investig Drugs. 14 (7): 775–83. doi:10.1517/13543784.14.7.775. PMID   16022567. S2CID   11930383.
  6. Beeh KM, Derom E, Kanniess F, Cameron R, Higgins M, van As A (May 2007). "Indacaterol, a novel inhaled beta2-agonist, provides sustained 24-h bronchodilation in asthma". Eur. Respir. J. 29 (5): 871–8. doi: 10.1183/09031936.00060006 . PMID   17251236.
  7. Geake, James B (2015). "Indacaterol, a once-daily beta2-agonist, versus twice-daily beta2-agonists or placebo for chronic obstructive pulmonary disease". Reviews. 1 (3): CD010139. doi:10.1002/14651858.CD010139.pub2. PMC   6464646 . PMID   25575340.
  8. European Public Assessment Report for Onbrez Breezhaler Archived 2010-01-16 at the Wayback Machine
  9. "FDA approves Arcapta Neohaler to treat chronic obstructive pulmonary disease" (Press release). U.S. Food and Drug Administration. 2011-07-01. Archived from the original on 2011-07-03. Retrieved 2011-07-02.
  10. "Drug Approval Package: Arcapta Neohaler (indacaterol maleate) NDA #022383". U.S. Food and Drug Administration. 13 August 2013. Retrieved 14 June 2021.
  11. Faulkner, Sarah (22 December 2016). "Sunovion, Novartis ink licensing deal for inhaled COPD drugs". Drug Delivery Business.