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

Stem definition	Drug id	CAS RN
ciclosporin derivatives	4366	515814-01-4

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
Sept. 15, 2022	EMA	OTSUKA PHARMACEUTICAL NETHERLANDS B.V.
Jan. 22, 2021	FDA	AURINIA PHARMA U.S.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Urine protein/creatinine ratio increased	217.23	36.85	29	550	641	63487802
Glomerular filtration rate decreased	77.26	36.85	19	560	13422	63475021
Proteinuria	56.68	36.85	16	563	19129	63469314
Hypertension	49.73	36.85	31	548	279272	63209171
Product packaging difficult to open	37.92	36.85	5	574	98	63488345

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Urine protein/creatinine ratio increased	196.57	39.76	26	309	1208	79742845
Hypertension	64.80	39.76	30	305	330962	79413091
Glomerular filtration rate decreased	46.33	39.76	12	323	22690	79721363

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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 | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
7.9MG	LUPKYNIS	AURINIA	N213716	Jan. 22, 2021	RX	CAPSULE	ORAL	7332472	Oct. 17, 2023	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
7.9MG	LUPKYNIS	AURINIA	N213716	Jan. 22, 2021	RX	CAPSULE	ORAL	11622991	Dec. 7, 2037	TREATMENT OF PATIENTS WITH ACTIVE LUPUS NEPHRITIS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
7.9MG	LUPKYNIS	AURINIA	N213716	Jan. 22, 2021	RX	CAPSULE	ORAL	Jan. 22, 2026	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Peptidyl-prolyl cis-trans isomerase A	Enzyme	P62937	PPIA_HUMAN	INHIBITOR	Kd	7.82		IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
LUPKYNIS	HUMAN PRESCRIPTION DRUG LABEL	1	75626-001	CAPSULE	7.90 mg	ORAL	NDA	31 sections