Drug intelligence / Profile preview

motexafin gadolinium

Development stage
Phase 3
Lead developer
Pharmacyclics
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Motexafin gadolinium is a synthetic metalloporphyrin complex developed as an antineoplastic agent and radiosensitizer. It selectively accumulates in tumor cells due to their altered metabolism and acts primarily by inhibiting thioredoxin reductase and ribonucleotide reductase. This inhibition disrupts cellular redox balance and increases oxidative stress within cancer cells by promoting the formation of reactive oxygen species (ROS), thereby enhancing cytotoxicity from ionizing radiation and chemotherapy. Motexafin gadolinium has also been investigated as an MRI contrast agent due to its paramagnetic properties. The drug was primarily developed for use in conjunction with whole brain radiation therapy for the treatment of brain metastases arising from solid tumors such as non-small cell lung cancer[1][2][3][4][5][7].

Brand names
Xcytrin
Other names
gadolinium texaphyringadolinium texaphyrin complexGd(III) texaphyrin
02

Targets

RNR (Ribonucleotide reductase)TXNRD2 (Thioredoxin reductase 2)PRDX5 (Peroxiredoxin-5)

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