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)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
CHEBI has role CHEBI:35610 antineoplastic agent

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE TURALIO DAIICHI SANKYO INC N211810 Aug. 2, 2019 RX CAPSULE ORAL 8461169 April 19, 2028 TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 200MG BASE TURALIO DAIICHI SANKYO INC N211810 Aug. 2, 2019 RX CAPSULE ORAL 9358235 June 8, 2033 TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 200MG BASE TURALIO DAIICHI SANKYO INC N211810 Aug. 2, 2019 RX CAPSULE ORAL 10189833 May 5, 2036 TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY

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 FUNCTIONAL LIMITATIONS AND NOT AMENABLE 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
6783M2LV5X UNII
10056 INN_ID
2183102 RXNORM
018075 NDDF
d09340 MMSL
4038623 VANDF
789180004 SNOMEDCT_US
789195002 SNOMEDCT_US
25151352 PUBCHEM_CID
CHEBI:145373 CHEBI
2040295-03-0 SECONDARY_CAS_RN
D11270 KEGG_DRUG
DB12978 DRUGBANK_ID
CHEMBL3813873 ChEMBL_ID
CHEMBL3989973 ChEMBL_ID
8710 IUPHAR_LIGAND_ID
C000600259 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Turalio HUMAN PRESCRIPTION DRUG LABEL 1 65597-402 CAPSULE 200 mg ORAL NDA 20 sections