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TGR-1202 + oxaliplatin + folinic acid + fluorouracil

Development stage
Preclinical
Lead developer
TG Therapeutics
Modality
Recombinant Proteins and Enzymes, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral (TGR-1202), Intravenous (oxaliplatin, Folinic Acid, Fluorouracil)
01

Overview

This drug regimen is an **experimental combination** of four agents: - **TGR-1202 (umbralisib):** a next-generation, oral small molecule inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), primarily developed for B-cell malignancies. It selectively inhibits PI3Kδ, disrupting survival and proliferation signaling in malignant B cells[4][5][7]. - **Oxaliplatin:** a platinum-based chemotherapy agent that forms DNA crosslinks, inhibiting DNA replication and transcription, primarily used in gastrointestinal cancers. - **Folinic acid (leucovorin):** a reduced form of folic acid used to enhance the effects and decrease the toxicity of fluorouracil. - **Fluorouracil (5-FU):** a pyrimidine analog antimetabolite that inhibits thymidylate synthase, interfering with DNA and RNA synthesis, commonly used in many solid tumors. This combination is designed to provide **multi-modal targeting**, combining a targeted PI3Kδ inhibitor with a standard cytotoxic regimen frequently used in the treatment of gastrointestinal malignancies (FOLFOX). Its main indication would likely be for clinical investigation in refractory or relapsed solid tumors or lymphomas, although at this time, there is no publicly available evidence of this exact 4-drug combination being tested in officially registered trials[4][5][7]. Umbralisib was developed by TG Therapeutics and has shown efficacy both as monotherapy and in combination with other agents in hematologic cancers.

Other names
umbralisib + oxaliplatin + folinic acid + fluorouracil
02

Targets

TS (Thymidylate synthase)DNAPIK3CD (Phosphatidylinositol 3-kinase delta)

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