pexidartinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5343 1029044-16-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pexidartinib
  • pexidartinib hydrochloride
  • PLX3397
  • CML-261
  • turalio
Pexidartinib is a small molecule tyrosine kinase inhibitor that targets colony stimulating factor 1 receptor (CSF1R), KIT proto-oncogene receptor tyrosine kinase (KIT), and FMS-like tyrosine kinase 3 (FLT3) harboring an internal tandem duplication (ITD) mutation. Overexpression of the CSF1R ligand promotes cell proliferation and accumulation in the synovium. In vitro, pexidartinib inhibited proliferation of cell lines dependent on CSF1R and ligand-induced autophosphorylation of CSF1R. Pexidartinib also inhibited the proliferation of a CSF1R dependent cell line in vivo.
  • Molecular weight: 417.82
  • Formula: C20H15ClF3N5
  • CLOGP: 3.99
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 66.49
  • ALOGS: -5.19
  • ROTB: 6

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 2, 2019 FDA DAIICHI SANKYO INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hair colour changes 213.74 44.05 34 590 1758 46683680
Product dose omission issue 61.37 44.05 34 590 168486 46516952

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hair colour changes 171.21 51.82 26 240 1539 29950673

Pharmacologic Action:

SourceCodeDescription
ATC L01EX15 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:62434 alk inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Tenosynovial giant cell tumor indication 128777004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.65 acidic
pKa2 6.1 Basic
pKa3 2.77 Basic
pKa4 0.39 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 200MG BASE TURALIO DAIICHI SANKYO INC N211810 Aug. 2, 2019 RX CAPSULE ORAL Aug. 2, 2024 NEW CHEMICAL ENTITY
EQ 200MG BASE TURALIO DAIICHI SANKYO INC N211810 Aug. 2, 2019 RX CAPSULE ORAL Aug. 2, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONULLL LIMITATIONS AND NOT AMENULLBLE TO IMPROVEMENT WITH SURGERY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Macrophage colony-stimulating factor 1 receptor Kinase INHIBITOR IC50 7.88 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 7.56 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 6.79 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
2040295-03-0 SECONDARY_CAS_RN
4038623 VANDF
C5418120 UMLSCUI
CHEBI:145373 CHEBI
P31 PDB_CHEM_ID
CHEMBL3813873 ChEMBL_ID
CHEMBL3989973 ChEMBL_ID
D11270 KEGG_DRUG
DB12978 DRUGBANK_ID
25151352 PUBCHEM_CID
8710 IUPHAR_LIGAND_ID
C000600259 MESH_SUPPLEMENTAL_RECORD_UI
10056 INN_ID
6783M2LV5X UNII
2183102 RXNORM
321181 MMSL
37252 MMSL
d09340 MMSL
018075 NDDF
018076 NDDF
789180004 SNOMEDCT_US
789195002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Turalio HUMAN PRESCRIPTION DRUG LABEL 1 65597-402 CAPSULE 200 mg ORAL NDA 33 sections