Drug intelligence / Profile preview

PF-03084014 + gemcitabine + nab-paclitaxel

Development stage
Discontinued
Lead developer
Pfizer
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination regimen** consisting of PF-03084014, gemcitabine, and nab-paclitaxel. **PF-03084014** is a selective, orally bioavailable γ-secretase inhibitor that suppresses Notch signaling, which is implicated in tumor progression and maintenance of cancer stem cells. **Gemcitabine** is a nucleoside analog (antimetabolite) used as chemotherapy, primarily inhibiting DNA synthesis. **Nab-paclitaxel** (albumin-bound paclitaxel, marketed as Abraxane) is a nanoparticle formulation of paclitaxel, a mitotic inhibitor. The combination is being investigated for synergistic or additive anti-tumor activity in pancreatic ductal adenocarcinoma, showing preclinical efficacy by promoting tumor apoptosis, inhibiting proliferation, reducing stem cell populations, and blocking angiogenesis.

Other names
nirogacestatnab-paclitaxelgemcitabine
02

Targets

GSEC (Gamma-Secretase Complex)TUBB (Tubulin (alpha and beta subunits))

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