Drug intelligence / Profile preview

oxa(acfa)2

Development stage
Preclinical
Lead developer
Universität Leipzig
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

oxa(acfa)2 (also known as Oxa(AcFA)2) is a preclinical platinum(IV) prodrug derivative of oxaliplatin. It features an octahedral platinum(IV) core with a (1R,2R)-1,2-diaminocyclohexane (DACH) ligand, an oxalate ligand, and two axial acetyl-protected ferulate (AcFA) ligands. Designed to overcome the limitations of traditional platinum(II) chemotherapeutics, such as systemic toxicity and drug resistance, oxa(acfa)2 acts as a prodrug that undergoes intracellular reduction to release active oxaliplatin and the anti-inflammatory phenolic acid ligands. The incorporation of acetyl-protected ferulate ligands is intended to target the inflammatory microenvironment of tumors, which is known to promote cancer cell proliferation and survival. oxa(acfa)2 has been investigated for its antiproliferative activity against various breast cancer cell lines, both as a free complex and encapsulated within mesoporous silica nanoparticles (SBA-15) to achieve sustained drug release.

Other names
Oxa(AcFA)2trans,cis,cis-[Pt(AcFA)2(ox)(DACH)]
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DNA

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