Icenticaftor

Icenticaftor
Clinical data
Other names	QBW251
ATC code	none;
Identifiers
	IUPAC name 3-Amino-6-methoxy-N-[(2S)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide;
CAS Number	1334546-77-8;
PubChem CID	58442344;
ChemSpider	88296259;
UNII	AMB0BO0WFH;
KEGG	D12454;
CompTox Dashboard (EPA)	DTXSID601336884 ;
Chemical and physical data
Formula	C12H13F6N3O3
Molar mass	361.244 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@](CNC(=O)C1=C(C=C(C(=N1)OC)C(F)(F)F)N)(C(F)(F)F)O;
	InChI InChI=1S/C12H13F6N3O3/c1-10(23,12(16,17)18)4-20-8(22)7-6(19)3-5(11(13,14)15)9(21-7)24-2/h3,23H,4,19H2,1-2H3,(H,20,22)/t10-/m0/s1; Key:USHQRIKZLHNPQR-JTQLQIEISA-N;

Icenticaftor (development code QBW251) is a drug candidate for the treatment of chronic obstructive pulmonary disease (COPD)^[1]^[2] and cystic fibrosis.^[3]^[4] The drug is being developed by Novartis.^[5]

Like ivacaftor (which is marketed as Kalydeco), icenticaftor functions by acting as a stimulator of the protein cystic fibrosis transmembrane conductance regulator (CFTR).^[5]

References

^ Rowe SM, Jones I, Dransfield MT, Haque N, Gleason S, Hayes KA, et al. (2020). "Efficacy and Safety of the CFTR Potentiator Icenticaftor (QBW251) in COPD: Results from a Phase 2 Randomized Trial". International Journal of Chronic Obstructive Pulmonary Disease. 15: 2399–2409. doi:10.2147/COPD.S257474. PMC 7547289. PMID 33116455.
^ Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, et al. (June 2021). "Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease". Journal of Medicinal Chemistry. 64 (11): 7241–7260. doi:10.1021/acs.jmedchem.1c00343. ISSN 0022-2623. PMID 34028270.
^ Kazani S, Rowlands DJ, Bottoli I, Milojevic J, Alcantara J, Jones I, et al. (March 2021). "Safety and efficacy of the cystic fibrosis transmembrane conductance regulator potentiator icenticaftor (QBW251)". Journal of Cystic Fibrosis. 20 (2): 250–256. doi:10.1016/j.jcf.2020.11.002. PMC 8935475. PMID 33293212.
^ Ray F (December 9, 2020). "Icenticaftor Effective in CF Patients With Certain Mutations, Phase 1/2 Trial Shows". cysticfibrosisnewstoday.com. BioNews Services.
^ ^a ^b "Icenticaftor – Novartis". Adis Insight. Springer Nature Switzerland AG.

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