General
Preferred name
avacopan
Synonyms
CCX-168 ()
CCX168 ()
Avacopan (CCX168) ()
Tavneos ()
P&D ID
PD056899
CAS
1346623-17-3
Tags
available
probe
drug
Approved by
EMA
PMDA
FDA
First approval
2021
Drug indication
Hereditary haemolytic anemia
Eosinophilic granulomatosis with polyangiitis
IGA glomerulonephritis
Anca-associated vasculitis
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
1
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Small molecule antagonist of human C5a1 receptor; in Phase III clinical trials for pancreatic cancer treament.
DESCRIPTION
Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC50 of 0.1 nM.
PRICE
149
DESCRIPTION
Avacopan (CCX168) is a C5aR antagonist (IC50=0.1 nM) with selective and oral activity. Avacopan blocks the action of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a mouse model of AAV. Avacopan can be used to treat anti-neutrophil cytoplasmic antibody (ANCA)-related vasculitis.
DESCRIPTION
Avacopan is a small molecule, competitive and orally bioactive antagonist of human C5a1 receptor . It was originally proposed as an alternative to steroid (glucocorticoid) therapy for ANCA-associated vasculitis . The evidence confirming C5, C5a and the C5a receptor as anti-inflammatory and anti-cancer drug targets was reviewed by Horiuchi and Tsukamoto (2016) .
(GtoPdb)
MOA
Antagonist
(Chemical Probes.org)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
21
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
High-quality chemical probes
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
21
Molecular Weight
581.27
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
5
Aromatic Ring Count
3
cLogP
8.05
TPSA
61.44
Fraction CSP3
0.39
Chiral centers
2.0
Largest ring
6.0
QED
0.29
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
complement inhibitor
Target
Complement System
CD markers
C5AR1
Pathway
Immunology/Inflammation
Target class
GPCR
Target subclass
Complement peptide receptor
Source data
