avacopan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
complement receptor antagonists or complement inhibitors 5494 1346623-17-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • avacopan
  • tavneos
  • CCX168
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. The precise mechanism by which avacopan exerts a therapeutic effect in patients with ANCA-associated vasculitis has not been definitively established.
  • Molecular weight: 581.66
  • Formula: C33H35F4N3O2
  • CLOGP: 7.62
  • LIPINSKI: 2
  • HAC: 5
  • HDO: 2
  • TPSA: 61.44
  • ALOGS: -6.42
  • ROTB: 7
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 11, 2022 EMA Vifor Fresenius Medical Care Renal Pharma France
Oct. 7, 2021 FDA CHEMOCENTRYX
Sept. 27, 2021 PMDA KISSEI PHARMACEUTICAL CO., LTD.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AA59 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA EPC N0000193973 Complement 5a Receptor Antagonist
FDA MoA N0000193974 Complement 5a Receptor Antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Granulomatosis with polyangiitis indication 195353004 DOID:12132
Anti-Neutrophil Cytoplasmic Autoantibody (ANCA)-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis) indication 722191003
Microscopic polyangiitis indication 1144805008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG TAVNEOS CHEMOCENTRYX N214487 Oct. 7, 2021 RX CAPSULE ORAL 11603356 May 29, 2041 AN ADJUNCTIVE TREATMENT OF ADULT PATIENTS WITH TAVNEOS (AVACOPAN) WITH SEVERE ACTIVE ANCA-ASSOCIATED VASCULITIS (GPA AND MPA) IN COMBINATION WITH STANDARD THERAPY INCLUDING GLUCOCORTICOIDS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG TAVNEOS CHEMOCENTRYX N214487 Oct. 7, 2021 RX CAPSULE ORAL Oct. 7, 2026 NEW CHEMICAL ENTITY
10MG TAVNEOS CHEMOCENTRYX N214487 Oct. 7, 2021 RX CAPSULE ORAL Oct. 7, 2028 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])

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
C5a anaphylatoxin chemotactic receptor 1 GPCR ANTAGONIST IC50 9.35 DRUG LABEL DRUG LABEL

External reference:

IDSource
EFD PDB_CHEM_ID
CHEMBL3989871 ChEMBL_ID
C000620232 MESH_SUPPLEMENTAL_RECORD_UI
9450 IUPHAR_LIGAND_ID
DB15011 DRUGBANK_ID
018869 NDDF
4040886 VANDF
D11093 KEGG_DRUG
C4507514 UMLSCUI
10211 INN_ID
1264265006 SNOMEDCT_US
1264467000 SNOMEDCT_US
49841217 PUBCHEM_CID
2572100 RXNORM
351739 MMSL
39994 MMSL
d09819 MMSL
O880NM097T UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TAVNEOS HUMAN PRESCRIPTION DRUG LABEL 1 73556-168 CAPSULE 10 mg ORAL NDA 28 sections