Avacopan

Avacopan is a complement 5a receptor (C5aR) antagonist that inhibits the interaction between C5aR and the anaphylatoxin C5a. Avacopan blocks C5a-mediated neutrophil activation and migration.

• TAVNEOS is indicated as an adjunctive treatment of adult patients with severe active anti-neutrophil cytoplasmic autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis [GPA] and microscopic polyangiitis [MPA]) in combination with standard therapy including glucocorticoids. TAVNEOS does not eliminate glucocorticoid use.

• TAVNEOS is contraindicated in patients with serious hypersensitivity reaction to avacopan or to any of the excipients [see Warnings and Precautions (5.2) ]. Serious hypersensitivity to avacopan or to any of the excipients.contraindicated

The recommended dosage is 30 mg (three 10 mg capsules) twice daily, with food. ( 2 ) 2.1 Recommended Evaluations Prior to Treatment Initiation Before initiating TAVNEOS, perform the following evaluations: Liver Function Tests: Obtain liver test panel (serum alanine aminotransferase [ALT], aspartate aminotransferase [AST], alkaline phosphatase, and total bilirubin) before initiating TAVNEOS. TAVNEOS is not recommended for use in patients with cirrhosis, especially those with severe hepatic impairment (Child-Pugh C) [see Warnings and Precautions (5.1) and Use in Specific Populations (8.7) ]. Hepatitis B (HBV) Serology: Screen patients for HBV infection by measuring HBsAg and anti-HBc . For patients with evidence of prior or current HBV infection, consult with a physician with expertise in managing hepatitis B regarding monitoring and consideration for HBV antiviral therapy before or during treatment with TAVNEOS [see Warnings and Precautions (5.3) ]. 2.2 Recommended Dosage and Administration The recommended dose of TAVNEOS is 30 mg (three 10 mg capsules) twice daily, with food. Advise patients that TAVNEOS capsules should not be crushed, chewed or opened. If a dose is missed, instruct the patient to wait until the usual scheduled time to take the next regular dose. Instruct the patient not to double the next dose. 2.3 Dosage Modifications Due to CYP3A4 Inhibitors Reduce the dosage of TAVNEOS to 30 mg once daily when used concomitantly with strong CYP3A4 inhibitors.

Hepatotoxicity: Increase in liver function tests occurred in clinical trials. Obtain liver function tests before initiation of therapy and monitor as clinically indicated. ( 5.1 ) Serious Hypersensitivity Reactions: Cases of angioedema occurred in a clinical trial. Observe for signs and symptoms of angioedema and manage accordingly. ( 5.2 ) Hepatitis B Virus (HBV) Reactivation: Cases of HBV reactivation occurred in a clinical trial. Withhold TAVNEOS and institute appropriate anti-infective therapy. ( 5.3 ) Serious Infections: Avoid use of TAVNEOS in patients with active, serious infection, including localized infections. ( 5.4 ) 5.1 Hepatotoxicity Serious cases of hepatic injury have been observed in patients taking TAVNEOS. During controlled trials, the TAVNEOS treatment group had a higher incidence of transaminase elevations and hepatobiliary events, including serious and life-threatening events [see Adverse Reactions 6.1 ] . Obtain liver test panel (serum alanine aminotransferase [ALT], aspartate aminotransferase [AST], alkaline phosphatase, and total bilirubin) before initiating TAVNEOS, every 4 weeks after start of therapy for the first 6 months of treatment and as clinically indicated thereafter. If a patient receiving treatment with TAVNEOS presents with an elevation in ALT or AST to >3 times the upper limit of normal, evaluate promptly and consider pausing treatment as clinically indicated.

The following adverse reactions are discussed in greater detail in other sections of the labeling: Hepatotoxicity [see Warnings and Precautions (5.1) ] Hypersensitivity Reactions [see Warnings and Precautions (5.2) ] Hepatitis B Virus (HBV) Reactivation [see Warnings and Precautions (5.3) ] Serious Infections [see Warnings and Precautions (5.4) ] The most common adverse reactions (≥5%) are: nausea, headache, hypertension, diarrhea, vomiting, rash, fatigue, upper abdominal pain, dizziness, blood creatinine increased, and paresthesia. To report SUSPECTED ADVERSE REACTIONS, contact Amgen Inc. at 1-800-77-AMGEN (1-800-772-6436) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because the clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. The identification of potential adverse drug reactions was based on safety data from the phase 3 clinical trial in which 330 patients with ANCA-associated vasculitis were randomized 1:1 to either TAVNEOS or prednisone [see Clinical Studies (14) ] . The mean age of patients was 60.9 years (range of 13 to 88 years), with a predominance of men (56.4%) and Caucasians (84.2%). The cumulative exposure to TAVNEOS was 138.7 patient-years. Additionally, two phase 2 trials were conducted in ANCA-associated vasculitis. The cumulative clinical trial exposure from the phase 2 and 3 trials equals 212.3 patient-years.

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies with TAVNEOS in pregnant women to inform a drug-associated risk. In animal reproduction studies, oral administration of avacopan to pregnant hamsters and rabbits during the period of organogenesis produced no evidence of fetal harm with exposures up to approximately 5 and 0.6 times, respectively, the exposure at the maximum recommended human dose (MRHD) of 30 mg twice daily (on an area under the curve [AUC] basis). Avacopan caused an increase in the number of abortions in rabbits at an exposure 0.6 times the MRHD (see Animal Data ) . The background risk of major birth defects and miscarriage for the indicated population are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data In an embryo-fetal development study with pregnant hamsters dosed by the oral route during the period of organogenesis from gestation days 6 to 12, avacopan produced an increase in the incidence of a skeletal variation, described as supernumerary ribs, at an exposure that was 5 times the MRHD (on an AUC basis with a maternal oral dose of 1000 mg/kg/day).

Metabolism

Based on population pharmacokinetic analysis, the mean steady state plasma exposure estimates of avacopan are 3466 ± 1921 ng∙h/mL for the 12-hour area under the plasma drug concentration over time curve (AUC 0-12hr ) and 349 ± 169 ng/mL for the maximum plasma concentration (C max ) in patients with ANCA-associated vasculitis receiving 30 mg avacopan twice daily. Steady state plasma levels of avacopan are reached by 13 weeks and the accumulation is approximately 4-fold.

• Oct 7, 2021NDANDA214487Chemocentryx

1. 1Hospitalisation76613%
2. 2Death3456.1%
3. 3Off Label Use3325.8%
4. 4Diarrhoea2454.3%
5. 5Fatigue2364.1%
6. 6Nausea2354.1%
7. 7Therapy Interrupted1993.5%
8. 8Pneumonia1913.4%
9. 9Headache1713.0%
10. 10Covid-191693.0%
11. 11Product Dose Omission Issue1492.6%
12. 12Drug Ineffective1302.3%
13. 13Dyspnoea1232.2%
14. 14Infection1202.1%
15. 15Dialysis1182.1%

The 10 most recently updated of 26 ClinicalTrials.gov registrations naming Avacopan as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Evaluate Avacopan in Participants With ANCA-associated Vasculitis
  Recruiting · Phase 4 · Interventional · 300 enrolled · Amgen
  NCT06072482updated 2026-06-12
• Study to Evaluate Avacopan in Combination With a Rituximab or Cyclophosphamide-containing Regimen, in Children From 6 Years to < 18 Years of Age With AAV.
  Recruiting · Phase 3 · Interventional · 20 enrolled · Amgen
  NCT06321601updated 2026-05-14
• Pharmacokinetics Of Emulsified Avacopan Applied By NG Tube
  Recruiting · Phase 1 · Interventional · 6 enrolled · Mayo Clinic
  NCT07556484updated 2026-04-29
• A Study of Avacopan in Participants With Normal Renal Function and Participants With End-Stage Renal Disease (ESRD)
  Completed · Phase 1 · Interventional · 13 enrolled · Amgen
  NCT06468826updated 2026-03-25
• Avacopan Added to Standard-of-care Therapy in ANCA-associated Vasculitis With Severe Kidney Involvement
  Not yet recruiting · Phase 3 · Interventional · 130 enrolled · University Hospital, Toulouse
  NCT07373262updated 2026-01-28
• Avacopan in Crescentic Immunoglobulin A Nephropathy (IgAN)
  Recruiting · Phase 2 · Interventional · 16 enrolled · Mayo Clinic
  NCT06676579updated 2025-10-03
• TAVNEOS for Otolaryngologic Manifestations of Granulomatosis With Polyangiitis
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 30 enrolled · Robert Spiera, MD
  NCT07176546updated 2025-09-19
• Avacopan vs Reduced-dose Glucocorticoids in ANCA-associated Vasculitis
  Recruiting · Phase 4 · Interventional · 160 enrolled · Chiba University
  NCT06611696updated 2025-05-04
• A Phase 3 Clinical Trial of CCX168 (Avacopan) in Patients With ANCA-Associated Vasculitis
  Completed · Phase 3 · Interventional · 331 enrolled · Amgen
  NCT02994927updated 2025-03-24
• Evaluation of Safety and Efficacy of Avacopan in Subjects With Moderate to Severe Hidradenitis Suppurativa (AURORA)
  Completed · Phase 2 · Interventional · 435 enrolled · Amgen
  NCT03852472updated 2025-03-17

Frequently asked questions

How does Avacopan work?

Avacopan is a complement 5a receptor (C5aR) antagonist that inhibits the interaction between C5aR and the anaphylatoxin C5a. Avacopan blocks C5a-mediated neutrophil activation and migration.

What is Avacopan used for?

According to FDA labeling, Avacopan carries indications including: TAVNEOS is indicated as an adjunctive treatment of adult patients with severe active anti-neutrophil cytoplasmic autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis [GPA] and microscopic polyangiitis [MPA]) in combination with standard therapy including glucocorticoids. TAVNEOS does not eliminate glucocorticoid use.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Avacopan?

Avacopan is classified as Complement inhibitors, Complement 5a Receptor Antagonist, Complement 5 Inactivators, Complement 5a Receptor Antagonists, Cytochrome P450 3A4 Inhibitors, Decreased Complement Activity.

What are the brand names for Avacopan?

Avacopan is marketed under brand names including Tavneos.

What are the contraindications for Avacopan?

Avacopan labeling lists contraindications including: TAVNEOS is contraindicated in patients with serious hypersensitivity reaction to avacopan or to any of the excipients [see Warnings and Precautions (5.2) ]. Serious hypersensitivity to avacopan or to any of the excipients.. Always consult the full prescribing information and a clinician.