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

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

  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.


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