Avacopan

Complement 5a Receptor Antagonist — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Avacopan is an onp drug in the Complement 5a Receptor Antagonist class catalogued in DrugCentral. It was first approved by the PMDA in 2021. Its mechanism of action is classified as Complement 5a Receptor Antagonists and Cytochrome P450 3A4 Inhibitors. DrugCentral lists 1 molecular target, including C5AR1. Recorded indications include Anti-Neutrophil Cytoplasmic Autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis), Granulomatosis with polyangiitis and Microscopic polyangiitis.

• Approval status: onp (first approved 2021 by the PMDA).
• Drug class: Complement 5a Receptor Antagonist.
• Mechanism of action: Complement 5a Receptor Antagonists; Cytochrome P450 3A4 Inhibitors.
• Molecular targets: C5AR1 (1 listed in DrugCentral).
• Indications: Anti-Neutrophil Cytoplasmic Autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis), Granulomatosis with polyangiitis and Microscopic polyangiitis.
• ATC code: L04AJ05 (Complement inhibitors).
• Molecular formula: C33H35F4N3O2; molecular weight 581.66 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Anti-Neutrophil Cytoplasmic Autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis)
• Granulomatosis with polyangiitis
• Microscopic polyangiitis

Mechanism & targets

• Mechanism of action (MoA): Complement 5a Receptor Antagonists; Cytochrome P450 3A4 Inhibitors
• Established pharmacologic class: Complement 5a Receptor Antagonist

Molecular targets (1)

Target	Gene	Action	Activity
C5a anaphylatoxin chemotactic receptor 1	C5AR1	antagonist	IC50 9.35

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2022-01-11	EMA	—	Vifor Fresenius Medical Care Renal Pharma France	Yes
2021-10-07	FDA	—	CHEMOCENTRYX	Yes
2021-09-27	PMDA	—	KISSEI PHARMACEUTICAL CO., LTD.	Yes

ATC classification

ATC code	Therapeutic hierarchy
L04AJ05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Complement inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Hospitalisation	510.0
Vanishing bile duct syndrome	220.8
Hepatic function abnormal	213.0
Drug-induced liver injury	184.9
Liver disorder	159.3
Dialysis	123.1
Intentional underdose	122.5
Jaundice	122.4
COVID-19	98.1
Death	83.6
Pneumocystis jirovecii pneumonia	82.3
Therapy interrupted	81.5

Chemical structure

• Molecular formula: C₃₃H₃₅F₄N₃O₂
• Molecular weight: 581.66 g/mol
• CAS number: 1346623-17-3
• InChIKey: PUKBOVABABRILL-YZNIXAGQSA-N
• PubChem CID: 49841217

CC1=C(C(=CC=C1)F)C(=O)N2CCC[C@@H]([C@@H]2C3=CC=C(C=C3)NC4CCCC4)C(=O)NC5=CC(=C(C=C5)C)C(F)(F)F

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Avacopan used for?

DrugCentral lists the following indications for Avacopan: Anti-Neutrophil Cytoplasmic Autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis), Granulomatosis with polyangiitis and Microscopic polyangiitis.

How does Avacopan work?

Avacopan is classified as Complement 5a Receptor Antagonists and Cytochrome P450 3A4 Inhibitors; its molecular targets in DrugCentral include C5AR1 (antagonist).

When was Avacopan first approved?

Avacopan was first approved by the PMDA in 2021.

What drug class does Avacopan belong to?

Avacopan is in the Complement 5a Receptor Antagonist class.

What is the chemical formula of Avacopan?

Avacopan has the molecular formula C33H35F4N3O2 and a molecular weight of 581.66 g/mol.

Sources

• DrugCentral drug card 5494 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3989871 — compound record and bioactivity
• PubChem CID 49841217 — chemical identifiers
• DrugBank DB15011 — drug record
• FDA UNII O880NM097T — substance identity
• DailyMed: FDA labels for Avacopan — current prescribing information (label search)
• UniProt P21730 (C5AR1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.