Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C29H27N3O4 |
Molecular Weight | 481.5424 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)C1=CC=C(CN2C[C@@H]3C[C@H]2CN3CC4=CC=C(OC5=CC=C(C=C5)C6=NC=CO6)C=C4)C=C1
InChI
InChIKey=GERJIEKMNDGSCS-DQEYMECFSA-N
InChI=1S/C29H27N3O4/c33-29(34)23-5-1-20(2-6-23)16-31-18-25-15-24(31)19-32(25)17-21-3-9-26(10-4-21)36-27-11-7-22(8-12-27)28-30-13-14-35-28/h1-14,24-25H,15-19H2,(H,33,34)/t24-,25-/m0/s1
Acebilustat (formerly CTX-4430) is an investigational oral drug under development by Celtaxsys. It is a potent inhibitor of the enzyme leukotriene A4 hydrolase (LTA4H), which catalyzes the rate‐limiting step in the formation of leukotriene B4 (LTB4), a potent chemoattractant and activator of inflammatory immune cells including neutrophils. Acebilustat is currently being tested in Phase 2 clinical trial as a modulator of inflammation in patients with cystic fibrosis (CF). The U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have granted orphan drug status to acebilustat as a treatment for cystic fibrosis.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27806191
Seventeen patients with mild to moderate cystic fibrosis were enrolled and randomized into groups receiving placebo or doses of 50 mg or 100 mg acebilustat administered orally, once daily for 15 days. Sputum neutrophil counts were reduced by 65% over baseline values in patients treated with 100 mg acebilustat.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27806191
IC50 of acebilustat for inhibition of LTB4 production in human whole blood is 31 ng/ml, ∼0.064 uM.
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EU-Orphan Drug |
EU/3/14/1363
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FDA ORPHAN DRUG |
432114
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ACTIVE MOIETY