Baloxavir marboxil

Baloxavir marboxil
Clinical data
Synonyms	S-033188/S-033447
Identifiers
	IUPAC name ({(12aR)-12-[(11S)-7,8-Difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-6,8-dioxo-3,4,6,8,12,12a-hexahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin-7-yl}oxy)methyl methyl carbonate;
CAS Number	1985606-14-1;
PubChem CID	124081896;
UNII	505CXM6OHG;
KEGG	D11021;
Chemical and physical data
Formula	C27H23F2N3O7S
Molar mass	571.55 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(OCOC(C(C=C1)=O)=C(N1N([C@@H]2C3=CC=CC=C3SCC4=C(F)C(F)=CC=C24)[C@@]5([H])N6CCOC5)C6=O)OC;
	InChI InChI=1S/C27H23F2N3O7S/c1-36-27(35)39-14-38-25-19(33)8-9-31-24(25)26(34)30-10-11-37-12-21(30)32(31)23-15-6-7-18(28)22(29)17(15)13-40-20-5-3-2-4-16(20)23/h2-9,21,23H,10-14H2,1H3/t21-,23+/m1/s1; Key:RZVPBGBYGMDSBG-GGAORHGYSA-N;

Baloxavir marboxil (trade name Xofluza) is a medication being developed by Shionogi Co., a Japanese pharmaceutical company, for treatment of influenza A and influenza B. The drug was in late-stage trials in Japan and the United States as of early 2018, with collaboration from Roche AG.^[1]. The medication is unique in that it is given as a single dose, and may reduce the duration of flu symptoms by about a day.^[2]

Approval

It was approved for sale in Japan on February 23, 2018.^[3] In June 2018, the FDA granted priority review and is expected to make a decision on approval by December.^[2]

Pharmacology

It is an influenza therapeutic agent (cap-dependent endonuclease inhibitor), characterized by only taking one dose. Unlike neuraminidase inhibitors such as oseltamivir (Tamiflu) and zanamivir (Relenza) that inhibit the action of neuraminidase, which liberates viruses from the infected cells surface, baloxavir marboxil may prevent replication by inhibiting the cap-dependent endonuclease activity of the viral polymerase.^[4] It achieves this by inhibiting the process known as cap snatching^[5], which is a mechanism exploited by viruses to hijack the host mRNA transcription system to allow synthesis of viral RNAs.

References

↑ Rana, Preetika (10 February 2018). "Experimental Drug Promises to Kill the Flu Virus in a Day". Wall Street Journal.
1 2 "Flu drug, taken in single dose, could upend treatment if approved in U.S." STAT. 27 June 2018.
↑ "XOFLUZA (Baloxavir Marboxil) Tablets 10mg/20mg Approved For The Treatment Of Influenza Types A And B In Japan". 23 February 2018 – via www.publicnow.com.
↑ Dias, Alexandre; Bouvier, Denis; Crépin, Thibaut; McCarthy, Andrew A.; Hart, Darren J.; Baudin, Florence; Cusack, Stephen; Ruigrok, Rob W. H. (2009). "The cap-snatching endonuclease of influenza virus polymerase resides in the PA subunit". Nature. 458 (7240): 914–918. doi:10.1038/nature07745. ISSN 0028-0836.
↑ "Cap snatching".

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[1] Rana, Preetika (10 February 2018). "Experimental Drug Promises to Kill the Flu Virus in a Day". Wall Street Journal.

[stat-2] 1 2 "Flu drug, taken in single dose, could upend treatment if approved in U.S." STAT. 27 June 2018.

[3] "XOFLUZA (Baloxavir Marboxil) Tablets 10mg/20mg Approved For The Treatment Of Influenza Types A And B In Japan". 23 February 2018 – via www.publicnow.com.

[4] Dias, Alexandre; Bouvier, Denis; Crépin, Thibaut; McCarthy, Andrew A.; Hart, Darren J.; Baudin, Florence; Cusack, Stephen; Ruigrok, Rob W. H. (2009). "The cap-snatching endonuclease of influenza virus polymerase resides in the PA subunit". Nature. 458 (7240): 914–918. doi:10.1038/nature07745. ISSN 0028-0836.

[5] "Cap snatching".