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Optimisation of a novel series of ENaC inhibitors, leading to the selection of the long-acting inhaled clinical candidate ETD001, a potential new treatment for cystic fibrosis.
Danahay H, Gosling M, Fox R, Lilley S, Charlton H, Hargrave JD, Schofield TB, Hay DA, Went N, McMahon P, Marlin F, Scott J, Vile J, Hewison S, Ellam S, Brown S, Sabater J, Kennet G, Lightowler S, Collingwood SP. Danahay H, et al. Eur J Med Chem. 2025 Jan 15;282:117040. doi: 10.1016/j.ejmech.2024.117040. Epub 2024 Nov 8. Eur J Med Chem. 2025. PMID: 39561495 Free article.
ETD001: A novel inhaled ENaC blocker with an extended duration of action in vivo.
Danahay H, McCarthy C, Schofield T, Fox R, Charlton H, Lilley S, Sabater J, Salathe M, Baumlin N, Collingwood SP, Gosling M. Danahay H, et al. J Cyst Fibros. 2024 Jun 7:S1569-1993(24)00081-X. doi: 10.1016/j.jcf.2024.06.002. Online ahead of print. J Cyst Fibros. 2024. PMID: 38851923 Free article.
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, Budd E, Butler R, Cheung AK, Choudhury H, Collingwood SP, Cox B, Danahay H, Edwards L, Everatt B, Glaenzel U, Glotin AL, Groot-Kormelink P, Hall E, Hatto J, Howsham C, Hughes G, King A, Koehler J, Kulkarni S, Lightfoot M, Nicholls I, Page C, Pergl-Wilson G, Popa MO, Robinson R, Rowlands D, Sharp T, Spendiff M, Stanley E, Steward O, Taylor RJ, Tranter P, Wagner T, Watson H, Williams G, Wright P, Young A, Sandham DA. Grand DL, et al. Among authors: danahay h. J Med Chem. 2021 Jun 10;64(11):7241-7260. doi: 10.1021/acs.jmedchem.1c00343. Epub 2021 May 24. J Med Chem. 2021. PMID: 34028270
Safety and efficacy of the cystic fibrosis transmembrane conductance regulator potentiator icenticaftor (QBW251).
Kazani S, Rowlands DJ, Bottoli I, Milojevic J, Alcantara J, Jones I, Kulmatycki K, Machineni S, Mostovy L, Nicholls I, Nick JA, Rowe SM, Simmonds NJ, Vegesna R, Verheijen J, Danahay H, Gosling M, Ayalavajjala PS, Salman M, Strieter R. Kazani S, et al. Among authors: danahay h. J Cyst Fibros. 2021 Mar;20(2):250-256. doi: 10.1016/j.jcf.2020.11.002. Epub 2020 Dec 6. J Cyst Fibros. 2021. PMID: 33293212 Free PMC article.
Efficacy and Safety of the CFTR Potentiator Icenticaftor (QBW251) in COPD: Results from a Phase 2 Randomized Trial.
Rowe SM, Jones I, Dransfield MT, Haque N, Gleason S, Hayes KA, Kulmatycki K, Yates DP, Danahay H, Gosling M, Rowlands DJ, Grant SS. Rowe SM, et al. Among authors: danahay h. Int J Chron Obstruct Pulmon Dis. 2020 Oct 5;15:2399-2409. doi: 10.2147/COPD.S257474. eCollection 2020. Int J Chron Obstruct Pulmon Dis. 2020. PMID: 33116455 Free PMC article. Clinical Trial.
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