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Abediterol

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Abediterol
Clinical data
Routes of
administration
Inhalation
ATC code
  • None
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
IUPHAR/BPS
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), but it has never been marketed.

History

[edit]

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

[edit]

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

[edit]
  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. S2CID 20959248.
  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. ^ "Abediterol". Adis Insight. Springer International Publishing AG. Retrieved 6 February 2024.
  6. ^ "AdisInsight: Abediterol/mometasone". Adis Insight. Springer International Publishing AG. Retrieved 6 February 2024.
  7. ^ "Espacenet - Bibliographic data". worldwide.espacenet.com. Retrieved 2021-05-07.
  8. ^ "Espacenet - Bibliographic data". worldwide.espacenet.com. Retrieved 2021-05-07.
  9. ^ 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.