Gefapixant

Gefapixant
Clinical data
Trade names	Lyfnua
Other names	MK-7264
ATC code	R05DB29 (WHO) ;
Legal status
Legal status	EU: Rx-only;
Identifiers
	IUPAC name 5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide;
CAS Number	1015787-98-0;
PubChem CID	24764487;
DrugBank	DB15097;
ChemSpider	58828660;
UNII	6K6L7E3F1L;
KEGG	D11349;
ChEMBL	ChEMBL3716057;
CompTox Dashboard (EPA)	DTXSID401337212 ;
ECHA InfoCard	100.258.106
Chemical and physical data
Formula	C14H19N5O4S
Molar mass	353.40 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC;
	InChI InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19); Key:HLWURFKMDLAKOD-UHFFFAOYSA-N;

Gefapixant, sold under the brand name Lyfnua, is a medication used to treat chronic (long-term) cough.^[1] It acts as an antagonist of the P2RX3 receptor.^[2]^[3]^[4]

It was approved for medical use in the European Union in September 2023.^[1]

Medical uses

Gefapixant is indicated for the treatment of refractory or unexplained chronic cough.^[1]

Society and culture

Names

It was named in honour of Geoff Burnstock.^[5]

References

^ ^a ^b ^c ^d "Lyfnua EPAR". European Medicines Agency. 29 September 2023. Retrieved 5 October 2023.
^ Muccino D, Green S (June 2019). "Update on the clinical development of gefapixant, a P2X3 receptor antagonist for the treatment of refractory chronic cough". Pulmonary Pharmacology & Therapeutics. 56: 75–78. doi:10.1016/j.pupt.2019.03.006. PMID 30880151. S2CID 81982653.
^ Richards D, Gever JR, Ford AP, Fountain SJ (July 2019). "Action of MK-7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation". British Journal of Pharmacology. 176 (13): 2279–2291. doi:10.1111/bph.14677. PMC 6555852. PMID 30927255.
^ Marucci G, Dal Ben D, Buccioni M, Martí Navia A, Spinaci A, Volpini R, et al. (December 2019). "Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications". Expert Opinion on Therapeutic Patents. 29 (12): 943–963. doi:10.1080/13543776.2019.1693542. hdl:11581/435751. PMID 31726893. S2CID 208037373.
^ Ford AP, Dillon MP, Kitt MM, Gever JR (November 2021). "The discovery and development of gefapixant". Autonomic Neuroscience. 235: 102859. doi:10.1016/j.autneu.2021.102859. PMID 34403981. S2CID 236524967.

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[Lyfnua_EPAR-1] "Lyfnua EPAR". European Medicines Agency. 29 September 2023. Retrieved 5 October 2023.

[pmid30880151-2] Muccino D, Green S (June 2019). "Update on the clinical development of gefapixant, a P2X3 receptor antagonist for the treatment of refractory chronic cough". Pulmonary Pharmacology & Therapeutics. 56: 75–78. doi:10.1016/j.pupt.2019.03.006. PMID 30880151. S2CID 81982653.

[pmid30927255-3] Richards D, Gever JR, Ford AP, Fountain SJ (July 2019). "Action of MK-7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation". British Journal of Pharmacology. 176 (13): 2279–2291. doi:10.1111/bph.14677. PMC 6555852. PMID 30927255.

[pmid31726893-4] Marucci G, Dal Ben D, Buccioni M, Martí Navia A, Spinaci A, Volpini R, et al. (December 2019). "Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications". Expert Opinion on Therapeutic Patents. 29 (12): 943–963. doi:10.1080/13543776.2019.1693542. hdl:11581/435751. PMID 31726893. S2CID 208037373.

[5] Ford AP, Dillon MP, Kitt MM, Gever JR (November 2021). "The discovery and development of gefapixant". Autonomic Neuroscience. 235: 102859. doi:10.1016/j.autneu.2021.102859. PMID 34403981. S2CID 236524967.

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