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| protein_bound =
| protein_bound =
| metabolism =
| metabolism =
| elimination_half-life = 24.3 hours<ref>{{cite journal|last1=Timmer|first1=Wolfgang|last2=Massana|first2=Eric|last3=Jimenez|first3=Eulalia|last4=Seoane|first4=Beatriz|last5=de Miquel|first5=Gonzalo|last6=Ruiz|first6=Sandrine|title=First-in-Human Study of the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Abediterol (LAS100977), a Novel Long-Acting β<sub>2</sub>-agonist|journal=The Journal of Clinical Pharmacology|date=December 2014|volume=54|issue=12|pages=1347–53|doi=10.1002/jcph.355}}</ref>
| elimination_half-life = 24.3 hours<ref>{{cite journal | vauthors = Timmer W, Massana E, Jimenez E, Seoane B, de Miquel G, Ruiz S | title = First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of abediterol (LAS100977), a novel long-acting Β2 -agonist | journal = Journal of Clinical Pharmacology | volume = 54 | issue = 12 | pages = 1347–53 | date = December 2014 | pmid = 24989946 | doi = 10.1002/jcph.355 }}</ref>
| excretion =
| excretion =


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'''Abediterol''' ([[International Nonproprietary Name|INN]];<ref>{{cite journal|title=International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 104|journal=WHO Drug Information|date=2010|volume=24|issue=1|page=352|url=http://www.who.int/medicines/publications/druginformation/issues/PL-104.pdf|accessdate=25 March 2016}}</ref> 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). It is currently under [[drug development|development]] by the Spanish pharmaceutical company [[Almirall]] and is in [[Phases of clinical research#Phase II|Phase II]] clinical trials.<ref>[http://www.almirall.com/webcorp2/cda/ImD_03_02.jsp Product development pipeline], [[Almirall]]</ref><ref>{{cite web|title=AdisInsight: Abediterol|url=http://adisinsight.springer.com/drugs/800026746|website=Adis Insight|publisher=Springer International Publishing AG|accessdate=25 March 2016}}</ref>
'''Abediterol''' ([[International Nonproprietary Name|INN]];<ref>{{cite journal|title=International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 104|journal=WHO Drug Information|date=2010|volume=24|issue=1|page=352|url=http://www.who.int/medicines/publications/druginformation/issues/PL-104.pdf|access-date=25 March 2016}}</ref> 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). It is currently under [[drug development|development]] by the Spanish pharmaceutical company [[Almirall]] and is in [[Phases of clinical research#Phase II|Phase II]] clinical trials.<ref>[http://www.almirall.com/webcorp2/cda/ImD_03_02.jsp Product development pipeline], [[Almirall]]</ref><ref>{{cite web|title=AdisInsight: Abediterol|url=http://adisinsight.springer.com/drugs/800026746|website=Adis Insight|publisher=Springer International Publishing AG|access-date=25 March 2016}}</ref>


It acts as a dual [[Beta2-adrenergic agonist|β<sub>2</sub> adrenergic agonist]]<ref>{{cite patent|WO|2006122788}}</ref><ref>{{cite patent|WO|2010094484}}</ref> and [[muscarinic antagonist]] and is classified as an [[Long-acting beta-adrenoceptor agonist|ultra-long-acting β<sub>2</sub> agonist]] (ultra-LABA).<ref>{{cite journal|last1=Beier|first1=J|last2=Fuhr|first2=R|last3=Massana|first3=E|last4=Jiménez|first4=E|last5=Seoane|first5=B|last6=de Miquel|first6=G|last7=Ruiz|first7=S|title=Abediterol (LAS100977), a novel long-acting β<sub>2</sub>-agonist: Efficacy, safety and tolerability in persistent asthma|journal=Respiratory Medicine|date=October 2014|volume=108|issue=10|pages=1424–1429|doi=10.1016/j.rmed.2014.08.005|pmid=25256258|url=http://www.resmedjournal.com/article/S0954-6111(14)00287-X/pdf|accessdate=25 March 2016}}</ref>
It acts as a dual [[Beta2-adrenergic agonist|β<sub>2</sub> adrenergic agonist]]<ref>{{cite patent|WO|2006122788}}</ref><ref>{{cite patent|WO|2010094484}}</ref> and [[muscarinic antagonist]] and is classified as an [[Long-acting beta-adrenoceptor agonist|ultra-long-acting β<sub>2</sub> agonist]] (ultra-LABA).<ref>{{cite journal | vauthors = Beier J, Fuhr R, Massana E, Jiménez E, Seoane B, de Miquel G, Ruiz S | title = Abediterol (LAS100977), a novel long-acting β2-agonist: efficacy, safety and tolerability in persistent asthma | journal = Respiratory Medicine | volume = 108 | issue = 10 | pages = 1424–9 | date = October 2014 | pmid = 25256258 | doi = 10.1016/j.rmed.2014.08.005 | url = http://www.resmedjournal.com/article/S0954-6111(14)00287-X/pdf }}</ref>


Its coformulation with [[mometasone furoate]] is also in Phase II clinical trials.<ref>{{cite web|title=AdisInsight: Abediterol/mometasone|url=http://adisinsight.springer.com/drugs/800033847|website=Adis Insight|publisher=Springer International Publishing AG|accessdate=25 March 2016}}</ref>
Its coformulation with [[mometasone furoate]] is also in Phase II clinical trials.<ref>{{cite web|title=AdisInsight: Abediterol/mometasone|url=http://adisinsight.springer.com/drugs/800033847|website=Adis Insight|publisher=Springer International Publishing AG|access-date=25 March 2016}}</ref>


==References==
== References ==
{{reflist|2}}
{{reflist|2}}


Revision as of 20:14, 7 January 2020

Abediterol
Clinical data
Routes of
administration		Inhalation
ATC code
  • None
Legal status
Legal status
  • Experimental
Pharmacokinetic data
Elimination half-life24.3 hours[1]
Identifiers
  • 5-[(1R)-2-{[6-(2,2-Difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H30F2N2O4
Molar mass460.522 g·mol−1
3D model (JSmol)
  • 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 checkY
  • Key:SFYAXIFVXBKRPK-QFIPXVFZSA-N checkY

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). It is currently under development by the Spanish pharmaceutical company Almirall and is in Phase II clinical trials.[3][4]

It acts as a dual β2 adrenergic agonist[5][6] and muscarinic antagonist and is classified as an ultra-long-acting β2 agonist (ultra-LABA).[7]

Its coformulation with mometasone furoate is also in Phase II clinical trials.[8]

References

  1. ^ 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.
  2. ^ "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.
  3. ^ Product development pipeline, Almirall
  4. ^ "AdisInsight: Abediterol". Adis Insight. Springer International Publishing AG. Retrieved 25 March 2016.
  5. ^ WO 2006122788 
  6. ^ WO 2010094484 
  7. ^ 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.
  8. ^ "AdisInsight: Abediterol/mometasone". Adis Insight. Springer International Publishing AG. Retrieved 25 March 2016.
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