deuruxolitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 5828 1513883-39-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • deuruxolitinib
  • leqselvi
  • CTP-543
  • deuruxolitinib phosphate
Deuruxolitinib is a Janus kinase (JAK) inhibitor. In an in vitro kinase activity assay, deuruxolitinib had greater inhibitory potency for JAK1, JAK2 and TYK2 relative to JAK3. The relevance of inhibition of JAK enzymes to therapeutic effectiveness is not currently known.
  • Molecular weight: 314.42
  • Formula: C17H18N6
  • CLOGP: 3.47
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 83.18
  • ALOGS:
  • ROTB: 4

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
July 25, 2024 FDA Sun Pharmaceutical

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 L04AF09 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Janus-associated kinase (JAK) inhibitors
FDA MoA N0000190111 Organic Anion Transporter 3 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190857 Janus Kinase Inhibitors
FDA EPC N0000190858 Janus Kinase Inhibitor
FDA MoA N0000193845 Bile Salt Export Pump Inhibitors
FDA MoA N0000193932 Multidrug and Toxin Extrusion Transporter 2 K Inhibitors
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L04AF Janus-associated kinase (JAK) inhibitors 7 drugs

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

DiseaseRelationSNOMED_IDDOID
Alopecia areata indication 68225006 DOID:986




🐶 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
EQ 8MG BASE LEQSELVI SUN PHARM INDS INC N217900 July 25, 2024 RX TABLET ORAL 10561659 May 4, 2037 TREATMENT OF ADULT PATIENTS WITH ALOPECIA AREATA
EQ 8MG BASE LEQSELVI SUN PHARM INDS INC N217900 July 25, 2024 RX TABLET ORAL 12076323 May 4, 2037 TREATMENT OF ADULT PATIENTS WITH ALOPECIA AREATA
EQ 8MG BASE LEQSELVI SUN PHARM INDS INC N217900 July 25, 2024 RX TABLET ORAL 11919907 May 21, 2041 TREATMENT OF ADULT PATIENTS WITH ALOPECIA AREATA
EQ 8MG BASE LEQSELVI SUN PHARM INDS INC N217900 July 25, 2024 RX TABLET ORAL 12285432 Aug. 11, 2042 TREATMENT OF ADULT PATIENTS WITH ALOPECIA AREATA
EQ 8MG BASE LEQSELVI SUN PHARM INDS INC N217900 July 25, 2024 RX TABLET ORAL 12364699 Oct. 10, 2044 TREATMENT OF ADULT PATIENTS WITH ALOPECIA AREATA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 8MG BASE LEQSELVI SUN PHARM INDS INC N217900 July 25, 2024 RX TABLET ORAL July 25, 2029 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 6.06 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 9.34 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.59 DRUG LABEL DRUG LABEL
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 7.31 DRUG LABEL

External reference:

IDSource
CHEMBL4594381 ChEMBL_ID
C000731752 MESH_SUPPLEMENTAL_RECORD_UI
4043993 VANDF
C5446729 UMLSCUI
CHEBI:757870 CHEBI
CHEMBL4594382 ChEMBL_ID
11622 INN_ID
2147706-60-1 SECONDARY_CAS_RN
72704611 PUBCHEM_CID
387949 MMSL
43013 MMSL
d10205 MMSL
019809 NDDF
11410 IUPHAR_LIGAND_ID
0CA0VSF91Y UNII
2716557 RXNORM
D11866 KEGG_DRUG
019811 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LEQSELVI HUMAN PRESCRIPTION DRUG LABEL 1 47335-108 TABLET, FILM COATED 8 mg ORAL NDA 29 sections