Abediterol
- None
- 5-[(1R)-2-{[6-(2,2-Difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one
- 915133-65-2
- 11962616
- 9326
- 10136846 Y
- QXA167CM6F
- D10219 Y
- CHEBI:142077
- ChEMBL3039530 Y
- DTXSID60238605
- Interactive image
- FC(F)(c1ccccc1)COCCCCCCNC[C@H](O)c3ccc(O)c2c3\C=C/C(=O)N2
- InChI=1S/C25H30F2N2O4/c26-25(27,18-8-4-3-5-9-18)17-33-15-7-2-1-6-14-28-16-22(31)19-10-12-21(30)24-20(19)11-13-23(32)29-24/h3-5,8-13,22,28,30-31H,1-2,6-7,14-17H2,(H,29,32)/t22-/m0/s1 Y
- Key:SFYAXIFVXBKRPK-QFIPXVFZSA-N Y
Abediterol (INN;[2] development codes AZD-0548 and LAS 100977) is a once-daily experimental drug candidate for the treatment of asthma and chronic obstructive pulmonary disease (COPD), but it has never been marketed.
History
Abediterol was under development by the Spanish pharmaceutical company Almirall and reached Phase II clinical trials,[3][4] but was discontinued in 2021.[5] Its coformulation with mometasone furoate also progressed to Phase II clinical trials, but was discontinued in 2019.[6]
Mechanism of action
Abediterol acts as a dual β2 adrenergic agonist[7][8] and muscarinic antagonist and is classified as an ultra-long-acting β2 agonist (ultra-LABA).[9]
References
- ^ Timmer W, Massana E, Jimenez E, Seoane B, de Miquel G, Ruiz S (December 2014). "First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of abediterol (LAS100977), a novel long-acting Β2 -agonist". Journal of Clinical Pharmacology. 54 (12): 1347–53. doi:10.1002/jcph.355. PMID 24989946. S2CID 20959248.
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 104" (PDF). WHO Drug Information. 24 (1): 352. 2010. Retrieved 25 March 2016.
- ^ Product development pipeline, Almirall
- ^ "AdisInsight: Abediterol". Adis Insight. Springer International Publishing AG. Retrieved 25 March 2016.
- ^ "Abediterol". Adis Insight. Springer International Publishing AG. Retrieved 6 February 2024.
- ^ "AdisInsight: Abediterol/mometasone". Adis Insight. Springer International Publishing AG. Retrieved 6 February 2024.
- ^ "Espacenet - Bibliographic data". worldwide.espacenet.com. Retrieved 2021-05-07.
- ^ "Espacenet - Bibliographic data". worldwide.espacenet.com. Retrieved 2021-05-07.
- ^ Beier J, Fuhr R, Massana E, Jiménez E, Seoane B, de Miquel G, Ruiz S (October 2014). "Abediterol (LAS100977), a novel long-acting β2-agonist: efficacy, safety and tolerability in persistent asthma". Respiratory Medicine. 108 (10): 1424–9. doi:10.1016/j.rmed.2014.08.005. PMID 25256258.
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Short-acting β2 agonists | |
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Long-acting β2 agonists |
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Ultra-long-acting β2 agonists |
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Other |
muscarinic antagonist
Leukotriene antagonists | |
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Arachidonate 5-lipoxygenase inhibitors | |
Thromboxane receptor antagonists | |
Non-xanthine PDE4 inhibitors |
- Aclidinium bromide/formoterol
- Beclometasone/formoterol
- Beclometasone/formoterol/glycopyrronium bromide
- Budesonide/formoterol
- Budesonide/glycopyrronium bromide/formoterol
- Fluticasone furoate/umeclidinium bromide/vilanterol
- Fluticasone furoate/vilanterol
- Fluticasone propionate/salmeterol
- Glycopyrronium bromide/formoterol
- Indacaterol/glycopyrronium bromide
- Indacaterol/glycopyrronium bromide/mometasone
- Indacaterol/mometasone
- Ipratropium bromide/salbutamol
- Mometasone/formoterol
- Salbutamol (albuterol)/budesonide
- Theophylline/ephedrine
- Theophylline/ephedrine/hydroxyzine
- Theophylline/ephedrine/phenobarbital
- Umeclidinium bromide/vilanterol
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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