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

Stem definitionDrug idCAS RN
4366 515814-01-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lupkynis
  • trans-R 1524
  • R-1524
  • orelvo
  • voclera
  • ISATX247
  • ISA-247
  • ISA247
  • ISA 247
  • voclosporin
Voclosporin is a calcineurin-inhibitor immunosuppressant. The mechanism of voclosporin suppression of calcineurin has not been fully established. Activation of lymphocytes involves an increase in intracellular calcium concentrations that bind to the calcineurin regulatory site and activate calmodulin binding catalytic subunit and through dephosphorylation activates the transcription factor, Nuclear Factor of Activated T-Cell Cytoplasmic (NFATc). The immunosuppressant activity results in inhibition of lymphocyte proliferation, T-cell cytokine production, and expression of T-cell activation surface antigens.
  • Molecular weight: 1214.65
  • Formula: C63H111N11O12
  • CLOGP: 12
  • LIPINSKI: 3
  • HAC: 23
  • HDO: 5
  • TPSA: 278.80
  • ALOGS: -5.48
  • ROTB: 16

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 2021 FDA AURINIA PHARMA U.S.

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 L04AD03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Calcineurin inhibitors
FDA EPC N0000175457 Calcineurin Inhibitor Immunosuppressant
FDA MoA N0000175458 Calcineurin Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Lupus nephritis indication 68815009
Noninfectious Uveitis indication




🐶 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
7.9MG LUPKYNIS AURINIA N213716 Jan. 22, 2021 RX CAPSULE ORAL 7332472 Oct. 17, 2022 TREATMENT OF PATIENTS WITH ACTIVE LUPUS NEPHRITIS
7.9MG LUPKYNIS AURINIA N213716 Jan. 22, 2021 RX CAPSULE ORAL 10286036 Dec. 7, 2037 TREATMENT OF PATIENTS WITH ACTIVE LUPUS NEPHRITIS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
7.9MG LUPKYNIS AURINIA N213716 Jan. 22, 2021 RX CAPSULE ORAL Jan. 22, 2026 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Peptidyl-prolyl cis-trans isomerase A Enzyme INHIBITOR Kd 7.82 IUPHAR

External reference:

IDSource
D09033 KEGG_DRUG
4040008 VANDF
C2607219 UMLSCUI
CHEBI:135957 CHEBI
CHEMBL2218919 ChEMBL_ID
DB11693 DRUGBANK_ID
C484071 MESH_SUPPLEMENTAL_RECORD_UI
11388 IUPHAR_LIGAND_ID
8889 INN_ID
2PN063X6B1 UNII
6918486 PUBCHEM_CID
2475166 RXNORM
343010 MMSL
39286 MMSL
d09707 MMSL
018620 NDDF
1149151008 SNOMEDCT_US
1149188006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LUPKYNIS HUMAN PRESCRIPTION DRUG LABEL 1 75626-001 CAPSULE 7.90 mg ORAL NDA 31 sections
LUPKYNIS HUMAN PRESCRIPTION DRUG LABEL 1 75626-001 CAPSULE 7.90 mg ORAL NDA 31 sections