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TGR-1202 + nab-paclitaxel + gemcitabine

Development stage
Preclinical
Lead developer
TG Therapeutics
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

TGR-1202 + nab-paclitaxel + gemcitabine is a combination drug regimen that includes three distinct agents: **TGR-1202** (umbralisib), **nab-paclitaxel** (albumin-bound paclitaxel, branded as Abraxane), and **gemcitabine**. - **TGR-1202 (umbralisib)** is a small molecule inhibitor of phosphoinositide 3-kinase delta (PI3Kδ)[1][7]. Inhibition of PI3Kδ disrupts cellular signaling crucial for survival and proliferation of certain hematologic malignancies. - **Nab-paclitaxel** is a nanoparticle, albumin-bound formulation of paclitaxel (a microtubule inhibitor) that targets cell division by stabilizing microtubules, preventing normal mitotic function[4][8]. - **Gemcitabine** is a nucleoside analog (antimetabolite) that is incorporated into DNA, resulting in inhibition of DNA synthesis and ultimately cell death[8]. Taken together, the triple combination would potentially act through inhibition of PI3Kδ-mediated survival signaling, disruption of microtubule dynamics, and interference with DNA replication. TGR-1202 is developed by TG Therapeutics. Nab-paclitaxel (Abraxane) and gemcitabine are standard chemotherapy agents, commonly used in pancreatic cancer[2][4][6][8][10]. The combination of nab-paclitaxel and gemcitabine is FDA-approved for metastatic pancreatic cancer, but the triple combination with TGR-1202 is investigational and has not reached widespread clinical use or regulatory approval.

Brand names
Abraxane (nab-paclitaxel)
Other names
nab-P/Gemgemcitabine plus nab-paclitaxel
02

Targets

RNR (Ribonucleotide reductase)DNA polymerase familyTUBB (Tubulin (alpha and beta subunits))PIK3CD (Phosphatidylinositol 3-kinase delta)

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