--- title: "Avacopan | PepTracker Pro" url: https://peptrackerpro.com/peptides/avacopan description: "Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). It is designed to let patients taper off high-dose glucocorticoids, not to replace immunosuppression." lang: en --- Skip to main content **Educational information only.** This site does not provide medical advice. Read full disclaimer (https://peptrackerpro.com/disclaimer) **Research-only content.** This page is for educational purposes and does not constitute medical advice. Read full disclaimer → (https://peptrackerpro.com/research-disclaimer) # Avacopan High Evidence Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). It is designed to let patients taper off high-dose glucocorticoids, not to replace immunosuppression. Aliases Avacopan +15 more Evidence High Evidence Last Updated 2026-10-12 Reading Time 6 min ## What It Is Avacopan (brand name Tavneos, development code CCX168) is a first-in-class, orally available small molecule that selectively blocks the complement C5a receptor (C5aR1, also known as CD88) on neutrophils and other myeloid cells. It was discovered and developed by ChemoCentryx, which Amgen acquired in 2022; outside the United States it is commercialized by CSL Vifor (with Kissei holding rights in Japan). The complement anaphylatoxin C5a is one of the body's most powerful neutrophil-recruiting and -priming signals, and in ANCA-associated vasculitis (AAV) that C5a signaling is a central driver: ANCA antibodies and C5a together prime and activate neutrophils that then attack the walls of small blood vessels, damaging the kidneys, lungs, sinuses, and other organs. Rather than knocking out the whole terminal complement pathway the way anti-C5 antibodies do, avacopan narrowly blocks the C5a-to-C5aR1 interaction, leaving C5b and the downstream membrane-attack complex (which helps defend against encapsulated bacteria such as Neisseria) comparatively intact - a key difference from C5 inhibitors like eculizumab. Its clinical purpose is as much about steroids as about complement: AAV has traditionally been treated with months of high-dose glucocorticoids on top of rituximab or cyclophosphamide, and that steroid burden causes much of the long-term harm. In the pivotal Phase 3 ADVOCATE trial, avacopan plus standard immunosuppression matched a prednisone taper for remission at 26 weeks and was superior for sustained remission at 52 weeks, while sharply reducing glucocorticoid exposure. The FDA approved it on October 7, 2021 as an adjunctive (add-on) therapy. Avacopan is a prescription medicine prescribed and monitored by rheumatologists and nephrologists for a confirmed diagnosis - not a supplement, nootropic, or research chemical. Also known as: Avacopan, Tavneos, avacopan, CCX168, CCX-168, C5a receptor antagonist, C5aR1 antagonist, C5aR inhibitor, CD88 antagonist, selective C5a receptor inhibitor, oral complement inhibitor, Tavneos ANCA vasculitis, ANCA vasculitis oral treatment, ChemoCentryx avacopan, Amgen avacopan, CSL Vifor avacopan ## Why Researchers Study It Avacopan is studied as proof that blocking a single complement anaphylatoxin receptor - C5a's receptor C5aR1 (CD88) - can control a serious autoimmune vasculitis while sparing much of the rest of the complement system. In ANCA-associated vasculitis, C5a primes and activates neutrophils that then damage small vessels; by occupying C5aR1, avacopan blunts that neutrophil attack without knocking out the terminal membrane-attack complex the way anti-C5 antibodies do, which is why it does not carry the meningococcal boxed warning that defines C5 inhibitors. Its greater scientific and clinical interest is as a glucocorticoid-sparing agent: the ADVOCATE trial tested whether an oral C5aR1 blocker added to rituximab or cyclophosphamide could replace a months-long high-dose prednisone taper, and it reached sustained remission superiority at 52 weeks with far less steroid exposure. That makes avacopan a key datapoint in two broader questions - where in the complement cascade to intervene (anaphylatoxin receptor versus terminal C5 versus the proximal factor D, factor B, and C3 steps) and how to cut the long-term toxicity of steroids in autoimmune disease. ## Proposed Mechanisms - Selectively and competitively antagonizes the complement C5a receptor 1 (C5aR1 / CD88) on neutrophils and other myeloid cells, blocking the anaphylatoxin C5a from binding and signaling - Dampens C5a-driven neutrophil chemotaxis, adhesion, activation, and the respiratory burst that, together with ANCA antibodies, drive small-vessel inflammation and damage in GPA and MPA - Acts at the terminal anaphylatoxin arm of complement but spares C5b and the downstream membrane-attack complex, so terminal lytic defense against encapsulated bacteria is comparatively preserved - unlike anti-C5 antibodies - Used as an oral, twice-daily add-on to rituximab or cyclophosphamide, it enables sharply reduced glucocorticoid exposure during induction and early maintenance of ANCA-associated vasculitis ## Evidence Snapshot High Evidence Low Medium High | Study Type | Model | Outcome | Link | | --- | --- | --- | --- | | Phase 3, severe active ANCA-associated vasculitis (ADVOCATE, NCT02994927) | 330 adults with newly diagnosed or relapsing severe GPA or MPA across 20 countries, randomized double-blind, double-dummy to oral avacopan 30 mg twice daily (with a prednisone-matched placebo taper) vs a prednisone taper, both on background rituximab or cyclophosphamide | Remission at week 26: 72.3% with avacopan vs 70.1% with prednisone (non-inferior). Sustained remission at week 52: 65.7% vs 54.9% - superior to the prednisone taper (p=0.007) - with markedly lower glucocorticoid exposure and improved kidney (eGFR) and quality-of-life measures; published in the New England Journal of Medicine, February 2021 | Source: https://www.nejm.org/doi/full/10.1056/NEJMoa2023386 | | Regulatory milestone - FDA approval | Adjunctive treatment of adults with severe active ANCA-associated vasculitis (GPA and MPA) in combination with standard therapy (rituximab or cyclophosphamide); oral 30 mg (three 10 mg capsules) twice daily with food | FDA approved Tavneos (avacopan) on October 7, 2021 as the first C5a receptor antagonist for ANCA-associated vasculitis; labeled with a Warning for hepatotoxicity and for hypersensitivity/angioedema (no boxed warning). Also approved in the EU, UK, and Japan. Developed by ChemoCentryx, acquired by Amgen in 2022 | Source: https://www.drugs.com/history/tavneos.html | ## Commonly Discussed Benefits immunology: https://peptrackerpro.com/benefits/immunology rare-disease: https://peptrackerpro.com/benefits/rare-disease complement-inhibitor: https://peptrackerpro.com/benefits/complement-inhibitor vasculitis: https://peptrackerpro.com/benefits/vasculitis nephrology: https://peptrackerpro.com/benefits/nephrology Researching Avacopan? Track it, set reminders, and keep notes in the free app. Track in App (https://app.peptrackerpro.com/?add=avacopan) ## Safety & Cautions - Carries a Warning for hepatotoxicity: serious cases of liver injury (including some requiring evaluation for transplant in the broader development program) have been reported, so liver enzymes and bilirubin should be checked before starting and monitored during treatment; avacopan should not be started in patients with active, serious liver disease and should be interrupted or stopped if liver injury is suspected - Can cause hypersensitivity reactions, including angioedema; it is contraindicated in patients with serious hypersensitivity to avacopan or any excipient - Blocks part of the complement system and is given alongside rituximab or cyclophosphamide, so it can raise the risk of serious infections; it was not studied in and is not recommended with concomitant long-term high-dose daily glucocorticoids, and live vaccines should be avoided - Is adjunctive (add-on) therapy to standard immunosuppression (rituximab or cyclophosphamide) and does not fully replace glucocorticoids in every patient; it does not cure ANCA-associated vasculitis and relapse can occur - Metabolized by CYP3A4: strong CYP3A4 inducers should be avoided, and the dose should be reduced with strong CYP3A4 inhibitors - A prescription medicine for a confirmed diagnosis of severe active GPA or MPA under rheumatology or nephrology care - not a supplement, nootropic, or research chemical; any 'avacopan' or 'Tavneos' sold outside a pharmacy is unverified - Common side effects (reported more often than with prednisone) include nausea, headache, hypertension, diarrhea, vomiting, rash, fatigue, upper abdominal pain, dizziness, increased blood creatinine, and paresthesia ## Comparisons See how Avacopan compares to related peptides: Avacopan vs Pegcetacoplan: https://peptrackerpro.com/compare/avacopan-vs-pegcetacoplan Avacopan vs Pozelimab: https://peptrackerpro.com/compare/avacopan-vs-pozelimab Avacopan vs Crovalimab (Piasky): https://peptrackerpro.com/compare/avacopan-vs-crovalimab Avacopan vs Iptacopan: https://peptrackerpro.com/compare/avacopan-vs-iptacopan Avacopan vs Danicopan: https://peptrackerpro.com/compare/avacopan-vs-danicopan ## Calculator Tools Use our research tools to explore dosing and reconstitution data: Reconstitution Calculator: https://peptrackerpro.com/calculators ## Citations 1. [1] FDA label - TAVNEOS (avacopan) capsules, for oral use, prescribing information PubMed (https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214487s000lbl.pdf) 2. [2] Tavneos (avacopan) FDA Approval History - Drugs.com PubMed (https://www.drugs.com/history/tavneos.html) 3. [3] Jayne DRW, et al. Avacopan for the Treatment of ANCA-Associated Vasculitis. N Engl J Med. 2021;384:599-609 (ADVOCATE) PubMed (https://www.nejm.org/doi/full/10.1056/NEJMoa2023386) 4. [4] FDA Approves Avacopan for the Treatment of ANCA-Associated Vasculitis - The Rheumatologist PubMed (https://www.the-rheumatologist.org/article/fda-approves-avacopan-for-the-treatment-of-anca-associated-vasculitis/) 5. [5] Tavneos (avacopan) for the Treatment of ANCA-Associated Vasculitis - Clinical Trials Arena PubMed (https://www.clinicaltrialsarena.com/projects/tavneos-avacopan-anca-associated-vasculitis/) 6. [6] Amgen to Acquire ChemoCentryx for $4 Billion in Cash (2022) - Amgen PubMed (https://www.amgen.com/newsroom/press-releases/2022/08/amgen-to-acquire-chemocentryx-for-4-billion-in-cash) ### Keep researching in the app - Log Avacopan to your private tracker - Set a dosing reminder - Compare it side-by-side with your stack Open PepTracker Pro Free: https://app.peptrackerpro.com/?add=avacopan Browse more peptides: https://peptrackerpro.com/peptides ## Related Peptides ### Pegcetacoplan High Evidence A PEGylated cyclic-peptide inhibitor of complement component 3 (C3) built from two compstatin (Cp05) peptide domains bridged by a 40-kDa PEG chain; marketed as Empaveli/Aspaveli (subcutaneous, for paroxysmal nocturnal hemoglobinuria and, since July 2025, C3 glomerulopathy and primary IC-MPGN) and Syfovre (intravitreal, for geographic atrophy in age-related macular degeneration). It is one of the few complement-targeting therapeutic peptides to reach the market. Immune Support: https://peptrackerpro.com/benefits/immune-support Inflammation: https://peptrackerpro.com/benefits/inflammation View Details: https://peptrackerpro.com/peptides/pegcetacoplan \+ Compare: https://peptrackerpro.com/compare?select=pegcetacoplan Track in App: https://app.peptrackerpro.com/?add=pegcetacoplan ### Pozelimab High Evidence Regeneron's fully human anti-C5 monoclonal antibody (Veopoz) — the first approved treatment for CHAPLE disease and the antibody half of the cemdisiran combination for complement-driven disease. immunology: https://peptrackerpro.com/benefits/immunology rare-disease: https://peptrackerpro.com/benefits/rare-disease complement-inhibition: https://peptrackerpro.com/benefits/complement-inhibition Hematology: https://peptrackerpro.com/benefits/hematology View Details: https://peptrackerpro.com/peptides/pozelimab \+ Compare: https://peptrackerpro.com/compare?select=pozelimab Track in App: https://app.peptrackerpro.com/?add=pozelimab ### Crovalimab (Piasky) High Evidence Chugai/Roche's humanized recycling anti-C5 monoclonal antibody (Piasky) — FDA-approved for paroxysmal nocturnal hemoglobinuria as a low-volume, once-monthly subcutaneous injection patients can give themselves. View Details: https://peptrackerpro.com/peptides/crovalimab \+ Compare: https://peptrackerpro.com/compare?select=crovalimab Track in App: https://app.peptrackerpro.com/?add=crovalimab ### Iptacopan High Evidence Novartis's Fabhalta (iptacopan, development code LNP023) - the first approved oral, first-in-class small-molecule factor B inhibitor that selectively blocks the alternative complement pathway at its proximal amplification loop; taken as a 200 mg capsule twice daily, it is FDA-approved for paroxysmal nocturnal hemoglobinuria (PNH), for primary IgA nephropathy (IgAN), and as the first-ever treatment for C3 glomerulopathy (C3G), and in July 2026 it became the first and only complement inhibitor to win traditional FDA approval for slowing kidney function decline in IgAN, cutting the annual rate of eGFR loss by about 48% versus placebo in the Phase 3 APPLAUSE-IgAN trial. immunology (https://peptrackerpro.com/benefits/immunology)rare-disease (https://peptrackerpro.com/benefits/rare-disease)complement-inhibitor (https://peptrackerpro.com/benefits/complement-inhibitor)Hematology (https://peptrackerpro.com/benefits/hematology)+1 more View Details: https://peptrackerpro.com/peptides/iptacopan \+ Compare: https://peptrackerpro.com/compare?select=iptacopan Track in App: https://app.peptrackerpro.com/?add=iptacopan ### Danicopan High Evidence AstraZeneca/Alexion's Voydeya (danicopan, development code ALXN2040) - a first-in-class, oral, small-molecule inhibitor of complement factor D that selectively blocks the alternative complement pathway at its proximal amplification loop; taken as a 150 mg tablet three times daily (up-titratable to 200 mg three times daily), it is FDA-approved as add-on therapy to the C5 inhibitors ravulizumab or eculizumab to treat clinically significant extravascular hemolysis in adults with paroxysmal nocturnal hemoglobinuria (PNH). It is not used as monotherapy. View Details: https://peptrackerpro.com/peptides/danicopan \+ Compare: https://peptrackerpro.com/compare?select=danicopan Track in App: https://app.peptrackerpro.com/?add=danicopan ## Structured data ```json [ { "@context": "https://schema.org", "@type": "Organization", "name": "PepTracker Pro", "url": "https://peptrackerpro.com", "logo": "https://peptrackerpro.com/favicon.png", "description": "Evidence-based educational resource dedicated to improving peptide research literacy.", "contactPoint": { "@type": "ContactPoint", "email": "hello@peptrackerpro.com", "contactType": "customer support" }, "sameAs": [] }, { "@context": "https://schema.org", "@type": "MedicalWebPage", "name": "Avacopan", "description": "Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). 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Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). 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Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). It is designed to let patients taper off high-dose glucocorticoids, not to replace immunosuppression." } }, { "@type": "Question", "name": "Clinicians weighing avacopan as an oral add-on to rituximab or cyclophosphamide against a conventional prednisone taper, and how it fits with maintenance azathioprine or mycophenolate?", "acceptedAnswer": { "@type": "Answer", "text": "Avacopan is a research peptide studied in preclinical models. Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). It is designed to let patients taper off high-dose glucocorticoids, not to replace immunosuppression." } }, { "@type": "Question", "name": "Researchers and students studying the role of C5a and neutrophil priming in small-vessel vasculitis and the broader idea of selectively blocking a single complement anaphylatoxin receptor?", "acceptedAnswer": { "@type": "Answer", "text": "Avacopan is a research peptide studied in preclinical models. Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). It is designed to let patients taper off high-dose glucocorticoids, not to replace immunosuppression." } }, { "@type": "Question", "name": "Patients and prescribers trying to understand avacopan's liver-monitoring requirements and how its infection risk differs from anti-C5 antibodies that require meningococcal vaccination?", "acceptedAnswer": { "@type": "Answer", "text": "Avacopan is a research peptide studied in preclinical models. Avacopan (brand Tavneos, development code CCX168) is a first-in-class, oral, small-molecule antagonist of the complement C5a receptor (C5aR1, also called CD88) from ChemoCentryx (now part of Amgen). Taken as 30 mg (three 10 mg capsules) twice daily with food, it blocks C5a from activating neutrophils and is FDA-approved as an adjunctive treatment for adults with severe active ANCA-associated vasculitis (granulomatosis with polyangiitis, GPA, and microscopic polyangiitis, MPA) alongside standard therapy (rituximab or cyclophosphamide). It is designed to let patients taper off high-dose glucocorticoids, not to replace immunosuppression." } } ] } ] ```