Drug intelligence / Profile preview

pexidartinib + paclitaxel

Development stage
Phase 1
Lead developer
Daiichi Sankyo
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of **pexidartinib**, a small molecule tyrosine kinase inhibitor of colony-stimulating factor 1 receptor (CSF-1R), FMS-like tyrosine kinase 3 (FLT3), and c-Kit (KIT), and **paclitaxel**, a microtubule-stabilizing chemotherapeutic agent. The combination has been studied in clinical trials for advanced solid tumors and high-risk early-stage breast cancer. Pexidartinib blocks CSF-1R signaling, reducing tumor-associated macrophage infiltration, which may help mitigate tumor growth and immune evasion. Paclitaxel disrupts cell division by stabilizing microtubules, leading to apoptosis of rapidly dividing cells. The pairing is based on preclinical evidence that CSF-1R inhibition can decrease immunosuppressive macrophages and enhance cytotoxic chemotherapy effects. In phase Ib/II studies, the combination showed manageable toxicity, notable hematologic and hepatic adverse events, and some partial and complete responses in advanced solid tumor patients. However, a trial in high-risk early-stage breast cancer found limited efficacy and concerns regarding serious hepatic toxicity[1][3][4][5].

Other names
pexidartinib and paclitaxelPLX3397 and paclitaxelPLX-3397 and paclitaxelPLX 3397 and paclitaxel
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)FLT3-ITD (Fms-like tyrosine kinase 3 with internal tandem duplication)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))FLT3 (Fms related receptor tyrosine kinase 3)

Beyond the preview

Go deeper on pexidartinib + paclitaxel.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on pexidartinib + paclitaxel.

Gosset Free

Get started with Gosset.

Enter your corporate email.

Work email preferred.

Book a call