Budiodarone tartrate
Budiodarone tartrate Basic information
- Product Name:
- Budiodarone tartrate
- Synonyms:
-
- Budiodarone tartrate
- CCX 168
- CS-2731
- Avacopan (CCX168)
- (2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl3-(trifluoromethyl)phenyl]piperidine-3-carboxamide
- 3-Piperidinecarboxamide, 2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]-, (2R,3S)-
- (S)-N-((3R,5R,6S)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide
- Avacopan, CCX 168, CS-2731
- CAS:
- 1346623-17-3
- MF:
- C33H35F4N3O2
- MW:
- 581.64
- Mol File:
- 1346623-17-3.mol
Budiodarone tartrate Chemical Properties
- Boiling point:
- 730.7±60.0 °C(Predicted)
- Density
- 1.287±0.06 g/cm3(Predicted)
- solubility
- DMF: 12 mg/ml; DMSO: 5 mg/ml; Ethanol: 3 mg/ml
- form
- A solid
- pka
- 14.02±0.70(Predicted)
- color
- White to off-white
- InChIKey
- PUKBOVABABRILL-YZNIXAGQSA-N
- SMILES
- C(C1C(=CC=CC=1C)F)(N1CCC[C@@H]([C@@H]1C1C=CC(=CC=1)NC1CCCC1)C(=O)NC1C=CC(=C(C=1)C(F)(F)F)C)=O
Budiodarone tartrate Usage And Synthesis
Uses
Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC50 of 0.1 nM.
in vivo
CCX168 is shown to be well tolerated across a broad dose range (1 to 100 mg) and it showed dose-dependent pharmacokinetics. An oral dose of 30 mg CCX168 given twice daily blocked the C5a-induced upregulation of CD11b in circulating neutrophils by 94% or greater throughout the entire day, demonstrating essentially complete target coverage. In mice dosed orally with 0.03 mg/kg of CCX168, the resulting plasma CCX168 concentration of 15 nM (8.7 ng/mL) reduces the drop in circulating leukocytes from 53% to 25%. In mice administered 0.3 mg/kg of CCX168, the resulting plasma CCX168 concentration of 75 nM (44 ng/mL) reduces the drop in circulating leukocytes from 53% to only 10% relative to baseline (p<0.05 for CCX168 vs. vehicle control). Oral doses of CCX168 of either 3 or 30 mg/kg completely blocks C5a-induced leukopenia in hC5aR knock-in mice[1]. Oral CCX168, 30 mg/kg daily, reduces the severity of anti-MPO NCGN in hC5aR mice. Glomerular crescents are reduced from 30.4% to 3.3% with CCX168. Urine hematuria, proteinuria, and leukocyturia are reduced in mice receiving CCX168, 30 mg/kg per day. The protection by CCX168 results in reduced crescents and necrosis[2].
References
[1] Bekker P, et al. Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study. PLoS One. 2016 Oct 21;11(10):e0164646. DOI:10.1371/journal.pone.0164646
[2] Xiao H, et al. C5a receptor (CD88) blockade protects against MPO-ANCA GN. J Am Soc Nephrol. 2014 Feb;25(2):225-31. DOI:10.1681/ASN.2013020143
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