Drug intelligence / Profile preview

motexafin gadolinium + rituximab + ibritumomab tiuxetan

Development stage
Unknown
Lead developer
Pharmacyclics
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

This is a **combination regimen** consisting of motexafin gadolinium (a redox-active metalloporphyrin and radiosensitizer), rituximab (a chimeric monoclonal antibody against CD20), and ibritumomab tiuxetan (a radiolabeled monoclonal antibody targeting CD20, typically conjugated to the radioisotope yttrium-90). Motexafin gadolinium inhibits thioredoxin reductase, depletes cellular antioxidants, and enhances tumor cell sensitivity to radiation and chemotherapy[1][7][5][9]. Rituximab mediates elimination of CD20+ B lymphocytes through complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity[8][6]. Ibritumomab tiuxetan delivers targeted radiation to CD20+ B lymphocytes, causing localized cytotoxicity, and is effective in lymphoma refractory to rituximab[6][8]. This triple regimen is investigational, with combination use explored for the treatment of certain lymphomas and brain metastases, but not as a marketed single agent or approved therapeutic combination.

Other names
motexafin gadoliniumrituximabibritumomab tiuxetan90Y-ibritumomab tiuxetan
02

Targets

TXNRD2 (Thioredoxin reductase 2)CD20 (B-lymphocyte antigen CD20)RNR (Ribonucleotide reductase)

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