THERAPY DOSSIER · th-fce5d9f2b69a

PLX3397 (pexidartinib)

Drug · CSF1R/FLT3/KIT tyrosine kinase inhibitor

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This record is classified as “NO TRAUMA TRANSLATION”. Read the indication and notes below for the specific context.

Evidence & regulatory context

Mechanism: CSF1R/FLT3/KIT tyrosine kinase inhibitor
Target: CSF1R (CHEMBL1844); FLT3 (CHEMBL1974); KIT (CHEMBL1936)
Injury models: TBI
Reported indication: Not recorded
First approval: 2019
Development stage: Not recorded
ChEMBL record: CHEMBL3813873 ↗
ChEMBL max phase: 4 / 4 (development scale, not regulatory approval)
Synonyms: Pexidartinib; PLX3397; PLX-3397; Turalio; CML-261
Note: Not recorded

Clinical trials 10

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

NCT02371369 ↗PHASE3completed

Phase 3 of PLX3397 in Pigmented Villonodular Synovitis or Giant Cell Tumor of Tendon Sheath

Tenosynovial Giant Cell Tumor

Enrolment: 120 · Results not recorded

NCT04488822 ↗PHASE3active not recruiting

Pexidartinib in Adult Subjects With Tenosynovial Giant Cell Tumor

Tenosynovial Giant Cell Tumor

Enrolment: 40 · Results not recorded

NCT01349049 ↗PHASE2completed

PLX3397 in Relapsed/Refractory FLT3-ITD Positive Acute Myeloid Leukemia

Acute Myeloid Leukemia

Enrolment: 90 · Results not recorded

NCT04703322 ↗PHASE2completed

Pexidartinib in Adult Subjects With Tenosynovial Giant Cell Tumor in Japan

Tenosynovial Giant Cell Tumor

Enrolment: 9 · Results not recorded

NCT01596751 ↗PHASE2completed

PLX3397 and Eribulin in Metastatic Breast Cancer

Metastatic Breast Cancer

Enrolment: 67 · Results not recorded

NCT02734433 ↗PHASE1completed

Single Agent Pexidartinib in Asian Subjects With Advanced Solid Tumors

Advanced Solid Tumors

Enrolment: 12 · Results not recorded

NCT03138759 ↗PHASE1completed

Effect of Probenecid on Pharmacokinetics of Pexidartinib in Healthy Subjects

Pharmacokinetics in Healthy Volunteers

Enrolment: 16 · Results not recorded

NCT02777710 ↗PHASE1completed

Anti-PDL1 (Durvalumab) Combined With Pexidartinib in Metastatic Pancreatic or Colorectal Cancers

Colorectal Cancer · Pancreatic Cancer

Enrolment: 48 · Results not recorded

NCT04635111 ↗Phase not recordedrecruiting

Long-term Study of Hepatotoxicity Risk Associated With TURALIO (Pexidartinib)

Hepatotoxicity · Tenosynovial Giant Cell Tumor

Enrolment: 30 · Results not recorded

NCT02975700 ↗Phase not recordedcompleted

PLX3397 in Unresectable or Metastatic KIT-mutated Melanoma

Melanoma

Enrolment: 6 · Results not recorded

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 31397209 ↗2019Reported benefit

Depletion of Microglia Attenuates Dendritic Spine Loss and Neuronal Apoptosis in the Acute Stage of Moderate Traumatic Brain Injury in Mice.

MouseTBIFluid percussionthy-1 GFPMaleGiven for 21 consecutive days before injury

Model: Moderate lateral fluid percussion injury

Microglial depletion with PLX3397 reduced resident microglia and infiltrating immune cells, promoted neurite outgrowth, preserved dendritic spines and lowered neuronal apoptosis and endoplasmic reticulum stress markers at 1 and 3 days after injury.

Extraction: extract · Subtype source: rule · Supplied extraction confidence: 0.65. Machine-extracted fields require source verification.

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