Drug Detail

Information about Pexidartinib

Generic Name
 Pexidartinib
IND
 PLX3397
Brand Name (US)
Manufacturer
 Plexxicon
Drug Type
 Tyrosine Kinase Inhibitor
Delivery
 Oral
Approval Status
 Phase 2
Indications
Overall Strategy
 KIT Protein Based
Strategy
 Block KIT
Drug Category
 KIT/PDGFRA inhibitor

PLX3397 is a KIT inhibitor that is being explored for potential use in cancer and several immune-mediated diseases.
It is currently in phase II trials for solid tumors including GIST.

May also be called PLX108-01.

Links

 

 Adis Insight (Springer)
   

 

 Selleckchem
   

 

 Sarcoma response to targeted therapy dynamically polarizes tumor-associated macrophages
   

 

 KIT oncogene inhibition drives intratumoral macrophage M2 polarization.
   

 

 Increased KIT inhibition enhances therapeutic efficacy in gastrointestinal stromal tumor
   

 

 NCI Drug Dictionary
   

 

 Plexxikon oncology page
   

 

 Sustained inhibition of receptor tyrosine kinases and macrophage depletion by PLX3397 and rapamycin as a potential new approach for the treatment of MPNSTs.
   

 

 Plexxikon Advances Novel Targeted Treatment PLX3397 in Blood Cancer
   

 

 Oncology - Osteolytic metastatic disease fact sheet (PDF)
   

 

 Clinical Cancer Research 2014: Sustained inhibition of receptor tyrosine kinases and macrophage depletion by PLX3397 and rapamycin as a potential new approach for the treatment of MPNSTs.
   

 

 Abstract A246: Blockade of CSF-1R/CSF-1 signaling by PLX3397 attenuates prostate cancer cell growth in bone, prostate cancer-induced skeletal pain, and pathological bone remodeling.
   

Trials of this drug

  

 Safety Study of PLX108-01 in Patients With Solid Tumors
   

Trial results
  ASCO 2014: A pilot study of PLX3397, a selective colony-stimulating factor 1 receptor (CSF1R) kinase inhibitor, in pigmented villonodular synovitis (PVNS).
   
  ASCO 2014: A phase 1b study to assess the safety of PLX3397, a CSF-1 receptor inhibitor, and paclitaxel in patients with advanced solid tumors.
   
  ASCO 2014: A phase 2 study of orally administered PLX3397 in patients with recurrent glioblastoma.
   
 
   
  2011 ASCO phase I - Pharmacodynamic activity demonstrated in phase I for PLX3397, a selective inhibitor of FMS and Kit.
   

Search for this drug/combination in:

ClinicalTrials.gov

ASCO

Pubmed