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=C1C=CC(NC(=O)C3=CC=C(F)C=C3C(F)(F)F)=C2

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
Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis.
2011 Aug
SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis.
2011 Jun
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 Jan
Optimal kinetic exposures for classic and candidate antitrypanosomals.
2019 Aug 1

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 Sat Dec 16 08:39:01 GMT 2023
Edited
by admin
on Sat Dec 16 08:39:01 GMT 2023
Record UNII
2IOR2OO3GW
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ACOZIBOROLE
INN  
INN  
Official 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
acoziborole [INN]
Common Name English
SCYX-7158
Code English
Code System Code Type Description
NCI_THESAURUS
C166573
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
PRIMARY
FDA UNII
2IOR2OO3GW
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
PRIMARY
INN
10515
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
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DRUG BANK
DB13086
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
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SMS_ID
100000175539
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
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WIKIPEDIA
SCYX-7158
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
PRIMARY
EPA CompTox
DTXSID301336035
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
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PUBCHEM
44178354
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
PRIMARY
CAS
1266084-51-8
Created by admin on Sat Dec 16 08:39:01 GMT 2023 , Edited by admin on Sat Dec 16 08:39:01 GMT 2023
PRIMARY
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