Drug intelligence / Profile preview

BKM120 + folinic acid + fluorouracil + oxaliplatin

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of four agents: - **BKM120 (buparlisib):** An oral pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor that targets the PI3K/AKT/mTOR signaling pathway, which is frequently dysregulated in cancer. By inhibiting PI3K, it aims to reduce tumor cell proliferation and survival. - **Folinic acid (leucovorin):** A reduced form of folic acid used to enhance the cytotoxic effects of fluorouracil by stabilizing its binding to thymidylate synthase. - **Fluorouracil (5-FU):** A pyrimidine analog antimetabolite that inhibits thymidylate synthase and interferes with DNA synthesis in rapidly dividing cells. - **Oxaliplatin:** A platinum-based chemotherapeutic agent that forms DNA crosslinks and induces apoptosis. The combination has been investigated primarily for advanced gastrointestinal malignancies such as colorectal cancer. The rationale is to combine targeted inhibition of the PI3K pathway with standard cytotoxic chemotherapy for potential synergistic anti-tumor activity[2].

Other names
mFOLFOX6 + BKM120buparlisib + leucovorin + 5-fluorouracil + oxaliplatin
02

Targets

TS (Thymidylate synthase)Phosphatidylinositol 3-kinase class I catalytic subunitDNATUBB (Tubulin (alpha and beta subunits))

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