Baloxavir
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MedKoo CAT#: 565272

CAS#: 1985605-59-1

Description: Baloxavir is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit.


Price and Availability

Size
Price

1mg
USD 330
Size
Price

5mg
USD 640
Size
Price

10mg
USD 1100

Baloxavir, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data, and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 565272
Name: Baloxavir
CAS#: 1985605-59-1
Chemical Formula: C24H19F2N3O4S
Exact Mass: 483.1064
Molecular Weight: 483.49
Elemental Analysis: C, 59.62; H, 3.96; F, 7.86; N, 8.69; O, 13.24; S, 6.63


Synonym: Baloxavir; Baloxavir acid; BXA

IUPAC/Chemical Name: (R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione

InChi Key: FIDLLEYNNRGVFR-CTNGQTDRSA-N

InChi Code: InChI=1S/C24H19F2N3O4S/c25-16-6-5-13-15(20(16)26)12-34-18-4-2-1-3-14(18)21(13)29-19-11-33-10-9-27(19)24(32)22-23(31)17(30)7-8-28(22)29/h1-8,19,21,31H,9-12H2/t19-,21+/m1/s1

SMILES Code: O=C1N2[C@](COCC2)([H])N([C@@H]3C4=CC=CC=C4SCC5=C(F)C(F)=CC=C35)N6C1=C(O)C(C=C6)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934990300


References

1: Koshimichi H, Ishibashi T, Wajima T. Population Pharmacokinetics of Baloxavir Marboxil in Japanese Pediatric Influenza Patients. J Pharm Sci. 2019 Apr 15. pii: S0022-3549(19)30236-9. doi: 10.1016/j.xphs.2019.04.010. [Epub ahead of print] PubMed PMID: 30998942.

2: LaVoie EJ, Sagong HY, Bauman JD, Nogales A, Martínez-Sobrido L, Arnold E. Aryl and arylalkyl substituted 3-hydroxypyridin(1H)-2-ones: Synthesis and evaluation as inhibitors of influenza A endonuclease. ChemMedChem. 2019 Apr 14. doi: 10.1002/cmdc.201900084. [Epub ahead of print] PubMed PMID: 30983160.

3: Beigel JH, Nam HH, Adams PL, Krafft A, Ince WL, El-Kamary SS, Sims AC. Advances in respiratory virus therapeutics - A meeting report from the 6th isirv Antiviral Group conference. Antiviral Res. 2019 Apr 8;167:45-67. doi: 10.1016/j.antiviral.2019.04.006. [Epub ahead of print] Review. PubMed PMID: 30974127.

4: Dziewiatkowski NA, Osmon EN, Chahine EB, Thornby KA. Baloxavir: A Novel Single-Dose Oral Antiviral for the Treatment of Influenza. Sr Care Pharm. 2019 Apr 1;34(4):243-252. doi: 10.4140/TCP.n.2019.243.. PubMed PMID: 30935446.

5: Takashita E, Kawakami C, Ogawa R, Morita H, Fujisaki S, Shirakura M, Miura H, Nakamura K, Kishida N, Kuwahara T, Ota A, Togashi H, Saito A, Mitamura K, Abe T, Ichikawa M, Yamazaki M, Watanabe S, Odagiri T. Influenza A(H3N2) virus exhibiting reduced susceptibility to baloxavir due to a polymerase acidic subunit I38T substitution detected from a hospitalised child without prior baloxavir treatment, Japan, January 2019. Euro Surveill. 2019 Mar;24(12). doi: 10.2807/1560-7917.ES.2019.24.12.1900170. PubMed PMID: 30914078.

6: de Haas EC, Luijendijk HJ. Baloxavir for influenza: Enrichment obscured lack of effect in North-American adults. Eur J Intern Med. 2019 Apr;62:e8-e9. doi: 10.1016/j.ejim.2018.12.002. Epub 2019 Mar 8. PubMed PMID: 30857671.

7: O'Hanlon R, Shaw ML. Baloxavir marboxil: the new influenza drug on the market. Curr Opin Virol. 2019 Mar 7;35:14-18. doi: 10.1016/j.coviro.2019.01.006. [Epub ahead of print] Review. PubMed PMID: 30852344.

8: Taniguchi K, Ando Y, Nobori H, Toba S, Noshi T, Kobayashi M, Kawai M, Yoshida R, Sato A, Shishido T, Naito A, Matsuno K, Okamatsu M, Sakoda Y, Kida H. Inhibition of avian-origin influenza A(H7N9) virus by the novel cap-dependent endonuclease inhibitor baloxavir marboxil. Sci Rep. 2019 Mar 5;9(1):3466. doi: 10.1038/s41598-019-39683-4. PubMed PMID: 30837531; PubMed Central PMCID: PMC6401108.

9: Taieb V, Ikeoka H, Ma FF, Borkowska K, Aballéa S, Tone K, Hirotsu N. A network meta-analysis of the efficacy and safety of baloxavir marboxil versus neuraminidase inhibitors for the treatment of influenza in otherwise healthy patients. Curr Med Res Opin. 2019 Apr 1:1-10. doi: 10.1080/03007995.2019.1584505. [Epub ahead of print] PubMed PMID: 30810054.

10: Koszalka P, Tilmanis D, Roe M, Vijaykrishna D, Hurt AC. Baloxavir marboxil susceptibility of influenza viruses from the Asia-Pacific, 2012-2018. Antiviral Res. 2019 Apr;164:91-96. doi: 10.1016/j.antiviral.2019.02.007. Epub 2019 Feb 13. PubMed PMID: 30771405.

11: Hayden FG, Shindo N. Influenza virus polymerase inhibitors in clinical development. Curr Opin Infect Dis. 2019 Apr;32(2):176-186. doi: 10.1097/QCO.0000000000000532. PubMed PMID: 30724789; PubMed Central PMCID: PMC6416007.

12: Najjar A, Karaman R. Successes, failures, and future prospects of prodrugs and their clinical impact. Expert Opin Drug Discov. 2019 Mar;14(3):199-220. doi: 10.1080/17460441.2019.1567487. Epub 2019 Feb 4. PubMed PMID: 30714428.

13: Kondo H, Shimada Y, Ozawa T. Promotion of Japan's participation in global clinical trials. Drug Discov Today. 2019 Apr;24(4):939-942. doi: 10.1016/j.drudis.2019.01.016. Epub 2019 Jan 30. PubMed PMID: 30710642.

14: Watanabe A, Ishida T, Hirotsu N, Kawaguchi K, Ishibashi T, Shishido T, Sato C, Portsmouth S, Tsuchiya K, Uehara T. Baloxavir marboxil in Japanese patients with seasonal influenza: Dose response and virus type/subtype outcomes from a randomized phase 2 study. Antiviral Res. 2019 Mar;163:75-81. doi: 10.1016/j.antiviral.2019.01.012. Epub 2019 Jan 23. PubMed PMID: 30684563.

15: Expanded table: Antiviral drugs for treatment and prophylaxis of seasonal influenza 2018-2019. Med Lett Drugs Ther. 2019 Jan 14;61(1563):e11-e12. PubMed PMID: 30681664.

16: Antiviral drugs for treatment and prophylaxis of seasonal influenza. Med Lett Drugs Ther. 2019 Jan 14;61(1563):1-4. PubMed PMID: 30681660.

17: Reina J, Reina N. [Baloxavir marboxil: a potent cap-dependent endonuclease inhibitor of influenza viruses]. Rev Esp Quimioter. 2019 Feb;32(1):1-5. Epub 2019 Jan 23. Review. Spanish. PubMed PMID: 30676002; PubMed Central PMCID: PMC6372968.

18: Omoto S, Speranzini V, Hashimoto T, Noshi T, Yamaguchi H, Kawai M, Kawaguchi K, Uehara T, Shishido T, Naito A, Cusack S. Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil. Sci Rep. 2018 Jun 25;8(1):9633. doi: 10.1038/s41598-018-27890-4. PubMed PMID: 29941893; PubMed Central PMCID: PMC6018108.