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Synonyms: CCX-168 | CCX168 | Tavneos®
avacopan is an approved drug (FDA (2021), EMA (2022))
Compound class: Synthetic organic
Comment: 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 [3,7]. The evidence confirming C5, C5a and the C5a receptor as anti-inflammatory and anti-cancer drug targets was reviewed by Horiuchi and Tsukamoto (2016) .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|Avacopan (research code CCX168) was evaluated in clinical trials for efficacy in ANCA-associated vasculitis and C3 glomerulopathy. Phase 2 results in ANCA-associated vasculitis were reported in . This study showed that avacopan safely and effectively replaced high dose glucocorticoid (prednisolone) therapy in patients with ANCA-associated vasculitis, which supported progression to Phase 3 trial.
The EMA granted orphan designations for avacopan as a treatment for granulomatosis with polyangiitis, microscopic polyangiitis (both 2014), and C3 glomerulopathy (2017).
Positive results from Phase 3 (ADVOCATE trial NCT02994927 ) led to FDA approval of avacopan as an adjunct (in combination with standard therapy) for the treatment of severe ANCA-associated vasculitis in October 2021.
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT03301467||Controlled Trial Evaluating Avacopan in C3 Glomerulopathy||Phase 2 Interventional||ChemoCentryx|
|NCT02994927||A Phase 3 Clinical Trial of CCX168 (Avacopan) in Patients With ANCA-Associated Vasculitis||Phase 3 Interventional||ChemoCentryx||6|
|NCT01363388||A Study to Evaluate the Safety and Efficacy of CCX168 in Subjects With ANCA-Associated Vasculitis||Phase 2 Interventional||ChemoCentryx||4|