Fexinidazole | Hoe-239 | CAS#59729-37-2

MedKoo Cat#: 326982 | Name: Fexinidazole

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Fexinidazole, also known as Hoe-239, antiparasitic agent potentially for the treatment of trypanosomiasis and leishmaniasis. It has activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone. Fexinidazole is the first drug candidate for the treatment of advanced-stage sleeping sickness in thirty years.

Chemical Structure

Fexinidazole

CAS#59729-37-2

Theoretical Analysis

MedKoo Cat#: 326982

Name: Fexinidazole

CAS#: 59729-37-2

Chemical Formula: C12H13N3O3S

Exact Mass: 279.0678

Molecular Weight: 279.31

Elemental Analysis: C, 51.60; H, 4.69; N, 15.04; O, 17.18; S, 11.48

Price and Availability

Size	Price	Availability
50mg	USD 250.00	2 Weeks
100mg	USD 450.00	2 Weeks
200mg	USD 750.00	2 Weeks
500mg	USD 1,450.00	2 Weeks

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Related CAS #

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Synonym

Fexinidazole; Fexinidazol; Fexinidazolum; Hoe-239; Hoe 239; Hoe239

IUPAC/Chemical Name

1-Methyl-2-((p-(methylthio)phenoxy)methyl)-5-nitroimidazole

InChi Key

MIWWSGDADVMLTG-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H13N3O3S/c1-14-11(13-7-12(14)15(16)17)8-18-9-3-5-10(19-2)6-4-9/h3-7H,8H2,1-2H3

SMILES Code

O=[N+](C1=CN=C(COC2=CC=C(SC)C=C2)N1C)[O-]

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

>2 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).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 279.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Fexinidazole. 2023 Jul 18. PMID: 37535799. 2: Deeks ED. Fexinidazole: First Global Approval. Drugs. 2019 Feb;79(2):215-220. doi: 10.1007/s40265-019-1051-6. PMID: 30635838. 3: Fexinidazole. Am J Health Syst Pharm. 2021 Nov 9;78(22):2005-2008. doi: 10.1093/ajhp/zxab336. PMID: 34498033. 4: Bernhard S, Kaiser M, Burri C, Mäser P. Fexinidazole for Human African Trypanosomiasis, the Fruit of a Successful Public-Private Partnership. Diseases. 2022 Oct 17;10(4):90. doi: 10.3390/diseases10040090. PMID: 36278589; PMCID: PMC9589988. 5: Fairlamb AH. Fexinidazole for the treatment of human African trypanosomiasis. Drugs Today (Barc). 2019 Nov;55(11):705-712. doi: 10.1358/dot.2019.55.11.3068795. PMID: 31840685. 6: Hidalgo J, Ortiz JF, Fabara SP, Eissa-Garcés A, Reddy D, Collins KD, Tirupathi R. Efficacy and Toxicity of Fexinidazole and Nifurtimox Plus Eflornithine in the Treatment of African Trypanosomiasis: A Systematic Review. Cureus. 2021 Aug 4;13(8):e16881. doi: 10.7759/cureus.16881. PMID: 34513456; PMCID: PMC8411996. 7: Rogers I, Berg K, Ramirez H, Hovel-Miner GA. Fexinidazole induced cytotoxicity is distinct from related anti-trypanosome nitroaromatic drugs. bioRxiv [Preprint]. 2023 Oct 9:2023.10.09.561529. doi: 10.1101/2023.10.09.561529. PMID: 37873123; PMCID: PMC10592674. 8: Zuma AA, de Souza W. Fexinidazole interferes with the growth and structural organization of Trypanosoma cruzi. Sci Rep. 2022 Nov 27;12(1):20388. doi: 10.1038/s41598-022-23941-z. PMID: 36437273; PMCID: PMC9701812. 9: Chappuis F. Oral fexinidazole for human African trypanosomiasis. Lancet. 2018 Jan 13;391(10116):100-102. doi: 10.1016/S0140-6736(18)30019-9. PMID: 29353603. 10: Neau P, Hänel H, Lameyre V, Strub-Wourgaft N, Kuykens L. Innovative Partnerships for the Elimination of Human African Trypanosomiasis and the Development of Fexinidazole. Trop Med Infect Dis. 2020 Jan 27;5(1):17. doi: 10.3390/tropicalmed5010017. PMID: 32012658; PMCID: PMC7157581. 11: Imran M, Khan SA, Alshammari MK, Alqahtani AM, Alanazi TA, Kamal M, Jawaid T, Ghoneim MM, Alshehri S, Shakeel F. Discovery, Development, Inventions and Patent Review of Fexinidazole: The First All-Oral Therapy for Human African Trypanosomiasis. Pharmaceuticals (Basel). 2022 Jan 21;15(2):128. doi: 10.3390/ph15020128. PMID: 35215241; PMCID: PMC8878566. 12: Mesu VKBK, Kalonji WM, Bardonneau C, Mordt OV, Blesson S, Simon F, Delhomme S, Bernhard S, Kuziena W, Lubaki JF, Vuvu SL, Ngima PN, Mbembo HM, Ilunga M, Bonama AK, Heradi JA, Solomo JLL, Mandula G, Badibabi LK, Dama FR, Lukula PK, Tete DN, Lumbala C, Scherrer B, Strub-Wourgaft N, Tarral A. Oral fexinidazole for late-stage African Trypanosoma brucei gambiense trypanosomiasis: a pivotal multicentre, randomised, non-inferiority trial. Lancet. 2018 Jan 13;391(10116):144-154. doi: 10.1016/S0140-6736(17)32758-7. Epub 2017 Nov 4. Erratum in: Lancet. 2018 Jan 13;391(10116):124. PMID: 29113731. 13: Bahia MT, de Andrade IM, Martins TA, do Nascimento ÁF, Diniz Lde F, Caldas IS, Talvani A, Trunz BB, Torreele E, Ribeiro I. Fexinidazole: a potential new drug candidate for Chagas disease. PLoS Negl Trop Dis. 2012;6(11):e1870. doi: 10.1371/journal.pntd.0001870. Epub 2012 Nov 1. PMID: 23133682; PMCID: PMC3486905. 14: Kande Betu Ku Mesu V, Mutombo Kalonji W, Bardonneau C, Valverde Mordt O, Ngolo Tete D, Blesson S, Simon F, Delhomme S, Bernhard S, Mahenzi Mbembo H, Mpia Moke C, Lumeya Vuvu S, Mudji E'kitiak J, Akwaso Masa F, Mukendi Ilunga M, Mpoyi Muamba Nzambi D, Mayala Malu T, Kapongo Tshilumbwa S, Botalema Bolengi F, Nkieri Matsho M, Lumbala C, Scherrer B, Strub-Wourgaft N, Tarral A. Oral fexinidazole for stage 1 or early stage 2 African Trypanosoma brucei gambiense trypanosomiasis: a prospective, multicentre, open-label, cohort study. Lancet Glob Health. 2021 Jul;9(7):e999-e1008. doi: 10.1016/S2214-109X(21)00208-4. PMID: 34143998; PMCID: PMC8220131. 15: Valverde Mordt O, Tarral A, Strub-Wourgaft N. Development and Introduction of Fexinidazole into the Global Human African Trypanosomiasis Program. Am J Trop Med Hyg. 2022 Mar 15;106(5_Suppl):61-66. doi: 10.4269/ajtmh.21-1176. PMID: 35292581; PMCID: PMC9154641. 16: Torreele E, Bourdin Trunz B, Tweats D, Kaiser M, Brun R, Mazué G, Bray MA, Pécoul B. Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness. PLoS Negl Trop Dis. 2010 Dec 21;4(12):e923. doi: 10.1371/journal.pntd.0000923. PMID: 21200426; PMCID: PMC3006138. 17: Pollastri MP. Fexinidazole: A New Drug for African Sleeping Sickness on the Horizon. Trends Parasitol. 2018 Mar;34(3):178-179. doi: 10.1016/j.pt.2017.12.002. Epub 2017 Dec 20. PMID: 29275007; PMCID: PMC5828866. 18: Kande Betu Kumesu V, Mutombo Kalonji W, Bardonneau C, Valverde Mordt O, Ngolo Tete D, Blesson S, Simon F, Delhomme S, Bernhard S, Nganzobo Ngima P, Mahenzi Mbembo H, Fina Lubaki JP, Lumeya Vuvu S, Kuziena Mindele W, Ilunga Wa Kyhi M, Mandula Mokenge G, Kaninda Badibabi L, Kasongo Bonama A, Kavunga Lukula P, Lumbala C, Scherrer B, Strub-Wourgaft N, Tarral A. Safety and efficacy of oral fexinidazole in children with gambiense human African trypanosomiasis: a multicentre, single-arm, open-label, phase 2-3 trial. Lancet Glob Health. 2022 Nov;10(11):e1665-e1674. doi: 10.1016/S2214-109X(22)00338-2. Epub 2022 Sep 27. PMID: 36179736; PMCID: PMC9554014. 19: Bayão TS, Cupertino MDC, Gomes AP, Siqueira-Batista R. Fexinidazole and Human African Trypanosomiasis: good news for this important neglected tropical disease. Rev Soc Bras Med Trop. 2019 Oct 3;52:e20190176. doi: 10.1590/0037-8682-0176-2019. PMID: 31596351. 20: Mohamed A, Chilingerian JN, Bali P, Obonyo M, Debnath A. A Bioluminescence- Based Drug Screen Identifies Activities of Fexinidazole and Its Metabolites against Helicobacter pylori. Antibiotics (Basel). 2022 Nov 11;11(11):1605. doi: 10.3390/antibiotics11111605. PMID: 36421252; PMCID: PMC9686901.