U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C17H14BF4NO3
Molecular Weight 367.103
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ACOZIBOROLE

SMILES

CC1(C)OB(O)C2=CC(NC(=O)C3=C(C=C(F)C=C3)C(F)(F)F)=CC=C12

InChI

InChIKey=PTYGDEXEGLDNAZ-UHFFFAOYSA-N
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)

HIDE SMILES / InChI

Molecular Formula C17H14BF4NO3
Molecular Weight 367.103
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Acoziborole (previously known as SCYX-7158) is a product of Anacor’s novel boron chemistry, which has produced a number of compounds with efficacy against a range of fungal, inflammatory, and bacterial diseases. Acoziborole was developed as an orally active compound with potent antitrypanosoma activity for the potential treatment of stage 2 human African trypanosomiasis (HAT) or sleeping sickness, a deadly parasitic disease transmitted by the tsetse fly. HAT is an important public health problem in sub-Saharan Africa. Existing therapies suffer from poor safety profiles, difficult treatment regimens, limited effectiveness, and a high cost of goods. Acoziborole is participating in phase II/III clinical trial to study its efficacy and safety in patients infected by HAT due to T.b. Gambiense.

Approval Year

PubMed

PubMed

TitleDatePubMed
Optimal kinetic exposures for classic and candidate antitrypanosomals.
2019-08-01
Pharmacokinetics and pharmacodynamics utilizing unbound target tissue exposure as part of a disposition-based rationale for lead optimization of benzoxaboroles in the treatment of Stage 2 Human African Trypanosomiasis.
2014-01
Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis.
2011-08
SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis.
2011-06

Sample Use Guides

SCYX-7158, in 320-mg tablets, administered by the oral route to patients in the fasting state according to the following dosing regimen: 960 mg (3 tablets) in a single intake on Day 1.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:14:12 GMT 2025
Edited
by admin
on Mon Mar 31 22:14:12 GMT 2025
Record UNII
2IOR2OO3GW
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ACOZIBOROLE
INN  
INN  
Official Name English
acoziborole [INN]
Preferred Name English
Acoziborole [WHO-DD]
Common Name English
4-FLUORO-N-(1-HYDROXY-3,3-DIMETHYL-1,3-DIHYDRO-BENZO(C)(1),(2)OXABOROL-6-YL-2-TRIFLUOROMETHYL BENZAMIDE
Systematic Name English
BENZAMIDE, N-(1,3-DIHYDRO-1-HYDROXY-3,3-DIMETHYL-2,1-BENZOXABOROL-6-YL)-4-FLUORO-2-(TRIFLUOROMETHYL)-
Systematic Name English
SCYX-7158
Code English
Code System Code Type Description
NCI_THESAURUS
C166573
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
FDA UNII
2IOR2OO3GW
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
INN
10515
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
DRUG BANK
DB13086
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
SMS_ID
100000175539
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
WIKIPEDIA
SCYX-7158
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
EPA CompTox
DTXSID301336035
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
PUBCHEM
44178354
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
CAS
1266084-51-8
Created by admin on Mon Mar 31 22:14:12 GMT 2025 , Edited by admin on Mon Mar 31 22:14:12 GMT 2025
PRIMARY
Related Record Type Details
TARGET ORGANISM->INHIBITOR
TARGET ORGANISM->INHIBITOR
TARGET ORGANISM->INHIBITOR
Related Record Type Details
ACTIVE MOIETY