SCYX-7158

SCYX-7158
Legal status

Legal status	Investigational New Drug
Identifiers
IUPAC name 4-fluoro-N-(1-hydroxy-3,3-dimethyl-2,1-benzoxaborol-6-yl)-2-(trifluoromethyl)benzamide
CAS Number	1266084-51-8^Y
PubChem (CID)	44178354
ChemSpider	29407646
Chemical and physical data
Formula	C₁₇H₁₄BF₄NO₃
Molar mass	367.102
3D model (Jmol)	Interactive image
SMILES CC2(C)OB(O)c3c2ccc(c3)NC(=O)c1ccc(F)cc1C(F)(F)F
InChI InChI=1S/C17H14BF4NO3/c1-16(2)12-6-4-10(8-14(12)18(25)26-16)23-15(24)11-5-3-9(19)7-13(11)17(20,21)22/h3-8,25H,1-2H3,(H,23,24) Key:PTYGDEXEGLDNAZ-UHFFFAOYSA-N

SCYX-7158 (AN-5568) is an antiprotozoal drug invented by Anacor Pharmaceuticals in 2009,^[1]^[2] and now under development by the Drugs for Neglected Diseases Initiative for the treatment of African trypanosomiasis (Sleeping sickness). It is a structurally novel drug described as a benzoxaborole derivative, and is the first orally active drug treatment developed for sleeping sickness. Phase I human clinical trials were completed successfully in 2015, and it is now in Phase IIb/III trials being carried out in the Democratic Republic of the Congo, where most cases of sleeping sickness occur.^[3]

References

↑ Jacobs R, et al. Efficacy and Pharmacokinetics of SCYX-7158 (AN5568): a Novel and Potent Oxaborole-6-Carboxamide Selected as a Pre-Clinical Candidate for Once-Daily Oral Treatment for Stage 2 Human African Trypanosomiasis. (Conferance Paper, 2009).
↑ Jacobs RT, Nare B, Wring SA, Orr MD, Chen D, Sligar JM, Jenks MX, Noe RA, Bowling TS, Mercer LT, Rewerts C, Gaukel E, Owens J, Parham R, Randolph R, Beaudet B, Bacchi CJ, Yarlett N, Plattner JJ, Freund Y, Ding C, Akama T, Zhang YK, Brun R, Kaiser M, Scandale I, Don R. SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis. PLoS Negl Trop Dis. 2011 Jun;5(6):e1151. doi: 10.1371/journal.pntd.0001151. PMID 21738803
↑ DNDi announces successful completion of SCYX-7158 Phase I study for treatment of sleeping sickness. 9th September 2015

Trypanosomiasis	African trypanosomiasis: ornithine (Eflornithine^#) arsenical (Melarsoprol^#) benzamidine (Pentamidine^#) naphthalenesulfonate (Suramin^#) nitroimidazole (Fexinidazole^†) Chagas disease: nitroimidazole (Benznidazole^#) nitrofuran (Nifurtimox^#)

Leishmaniasis	macrolide (Amphotericin B^#) Pentavalent antimonials (Meglumine antimoniate^#, Sodium stibogluconate) benzamidine (Pentamidine^#) phosphorylcholine (Miltefosine) neomycin (Paromomycin)

PAM	macrolide (Amphotericin B)

Giardiasis	nitroimidazole (Metronidazole^#, Tinidazole) benzimidazole (Albendazole) thiazolide (Nitazoxanide) nitrofuran (Furazolidone) aminoacridine (Quinacrine)

Trichomoniasis	nitroimidazole (Carnidazole, Metronidazole^#, Tinidazole)

Dientamoebiasis	nitroimidazole (Metronidazole Secnidazole) oxyquinoline (Iodoquinol) tetracycline (Doxycycline) neomycin (Paromomycin)

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