Acoziborole

Acoziborole
Clinical data
Other names	SCYX-7158
Legal status
Legal status	US: 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 ;
PubChem CID	44178354;
ChemSpider	29407646;
UNII	2IOR2OO3GW;
CompTox Dashboard (EPA)	DTXSID301336035 ;
Chemical and physical data
Formula	C17H14BF4NO3
Molar mass	367.11 g·mol−1
3D model (JSmol)	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;

Acoziborole (SCYX-7158) is an antiprotozoal drug invented by Anacor Pharmaceuticals in 2009,^[1] 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 a one-day, one-dose oral treatment. Phase I human clinical trials were completed successfully in 2015.^[2] A single arm phase II/III trial, with no control group, was conducted from 2016 to 2019 in the Democratic Republic of the Congo and Guinea involving 208 eligible patients with trypanosomiasis caused by Trypanosoma brucei gambiense. The results of the study, published in The Lancet on 29 November 2022, found the treatment regimen had a efficacy greater than 95%. Two follow-up studies, one comparing acoziborole to nifurtimox/eflornithine and a double-blind, randomized trial of the drug based on WHO recommendations with 1,200 total participants, are underway as of November 2022.^[3]

As the regimen is significantly easier to administer compared to existing treatment options, some commentators expressed hope that acoziborole could significantly slow down or even eliminate the transmission of African trypanosomiasis in humans.^[4]^[5]

References

^ Jacobs RT, Nare B, Wring SA, Orr MD, Chen D, Sligar JM, et al. (June 2011). "SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis". PLOS Neglected Tropical Diseases. 5 (6): e1151. doi:10.1371/journal.pntd.0001151. PMC 3125149. PMID 21738803.
^ "DNDi announces successful completion of SCYX-7158 Phase I study for treatment of sleeping sickness". 9 September 2015.
^ Betu Kumeso VK, Kalonji WM, Rembry S, Valverde Mordt O, Ngolo Tete D, Prêtre A, et al. (April 2023). "Efficacy and safety of acoziborole in patients with human African trypanosomiasis caused by Trypanosoma brucei gambiense: a multicentre, open-label, single-arm, phase 2/3 trial". The Lancet. Infectious Diseases. 23 (4): 463–470. doi:10.1016/S1473-3099(22)00660-0. PMC 10033454. PMID 36460027. S2CID 254103255.
^ "Single dose of acoziborole 95% effective in treating sleeping sickness". CIDRAP. 30 November 2022. Retrieved 4 December 2022.
^ Pépin J (April 2023). "Sleeping sickness: time for dreaming". The Lancet. Infectious Diseases. 23 (4): 387–388. doi:10.1016/S1473-3099(22)00686-7. PMID 36460028. S2CID 254179909.

[pmid21738803-1] Jacobs RT, Nare B, Wring SA, Orr MD, Chen D, Sligar JM, et al. (June 2011). "SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis". PLOS Neglected Tropical Diseases. 5 (6): e1151. doi:10.1371/journal.pntd.0001151. PMC 3125149. PMID 21738803.

[2] "DNDi announces successful completion of SCYX-7158 Phase I study for treatment of sleeping sickness". 9 September 2015.

[3] Betu Kumeso VK, Kalonji WM, Rembry S, Valverde Mordt O, Ngolo Tete D, Prêtre A, et al. (April 2023). "Efficacy and safety of acoziborole in patients with human African trypanosomiasis caused by Trypanosoma brucei gambiense: a multicentre, open-label, single-arm, phase 2/3 trial". The Lancet. Infectious Diseases. 23 (4): 463–470. doi:10.1016/S1473-3099(22)00660-0. PMC 10033454. PMID 36460027. S2CID 254103255.

[4] "Single dose of acoziborole 95% effective in treating sleeping sickness". CIDRAP. 30 November 2022. Retrieved 4 December 2022.

[5] Pépin J (April 2023). "Sleeping sickness: time for dreaming". The Lancet. Infectious Diseases. 23 (4): 387–388. doi:10.1016/S1473-3099(22)00686-7. PMID 36460028. S2CID 254179909.

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See also

References