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Motexafin Gadolinium

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Name: Motexafin Gadolinium
Generic Names: NSC 695238[1], [2],[3]
originally called as gadolinium texaphyrin[4], [3]
gadolinium(III) texaphyrin,[5]
PCI 0120, [6], [7],[5], Gd-Tex2+[7]
Trade Names: Xcytrin®[8],[9], [6],[10],[7]
IUPAC name: Gadolinium, bis(acetato-O)-(9, 10 diethyl-20, 21-bis(3-hydroxypropoxy)-4,15-dimethyl-8,11-imino-3,6:16, 13-dinitrilo-1, 18-benzodiazacycloeicosine-5, 14-dipropanolato-N1 N18, N23, N24,N25)[5]
[11], [9], [12], [6], [13], [14],[15],[10],[21]
it has five nitrogen ring resulting in large core to accomodate element gadolinium(Gd+3).[9],[16], [3]
synthetic aromatic macrocycle[9]
Functional Group/
chemical constitution:
radiosensitizing property is not attributed to inserted metal but is a function of ligand.[11]
it is expanded porphyrin ring in which iron is substituted by gadolinium[4]
the central metal composition is said to be an important determinant of effect of MGd on tumor oxygenation[17]
water soluble, kinetically stable[11]
member of texapyrin class of compounds[9],metalloporphyrin[12]
easily reduced[12]
paramagnetic, MRI-detectable[3]
soluble in water and also in organic solvents like alcohol, chlorocarbons, hence is amphiphilic[18]
Actions & Indications: Pharmcological Action-
redox modulator[9], [6]
anticancer agent[9]
radical formation agonist[12].
It is reported to be a promising radiosensitizing-agent in the treatment of brain tumors, especially in specific patient subsets, in a review[19]
ROS generator[6]
Therapeutic benefits:
The drug has shown effecicacy in improving neurocognitive quality of life in patients with brain metastasis from primary lung cancer in clinical setting[6],[15]
Preclinical Data:
MGd is a suitable candidate to be used in neutron capture therapy[12] ,[3],[15],[20]
Notes: MGd is not FDA approved radiation sensitizer[12]
1. Rosenthal DI et al, Reversible renal toxicity resulting from high single doses of the new radiosensitizer gadolinium texaphyrin. Am J Clin Oncol. 2000;23(6):593-8.
2. Ramanathan RK et al, Phase I and pharmacokinetic study of the novel redox-active agent, motexafin gadolinium, with concurrent radiation therapy in patients with locally advanced pancreatic or biliary cancers. Cancer Chemother Pharmacol 2006;57: 465–474.
3. Richards GM, Mehta MP, Motexafin gadolinium in the treatment of brain metastases. Expert Opin. Pharmacother. 2007;8(3):351-359.
4. Wu GN, Ford JM, Alger JR, MRI measurement of the uptake and retention of motexafin gadolinium in glioblastoma multiforme and uninvolved normal human brain. J Neurooncol. 2006;77(1):95-103.
5. Adis R&D profile, Motexafin gadolinium: gadolinium (III) texaphyrin, gadolinium texaphyrin, Gd-Tex, GdT2B2, PCI 0120. Drugs R&D 2004; 5 (1): 52-57.
6. Rodrigus P, Motexafin gadolinium: a possible new radiosensitiser. Expert Opinion on Investigational Drugs 2003; 12(7):1205-1210.
7. Sessler JL et al, One-electron reduction and oxidation studies of the radiation sensitizer Gadolinium(III) Texaphyrin (PCI-0120) and other water soluble metallotexaphyrins. J. Phys. Chem. A 1999;103:787-794.
8. Suh J et al, Phase II trial of Motexafin Gadolinium (MGd, Xcytrin®) and cranial radiation in newly diagnosed Glioblastoma Multiforme (GBM). Int. J. Radiat. Oncol. Biol. Phy. Supplement, 1 ,2002;54(2):246.
9. Forouzannia A et al, Motexafin gadolinium: a novel radiosensitizer for brain tumors. Expert Rev Anticancer Ther. 2007;7(6):785-94.
10. Thomas SR, Khuntia D, Motexafin gadolinium injection for the treatment of brain metastases in patients with non-small cell lung cancer. Int J Nanomedicine. 2007;2(1):79-87.
11. Viala J et al, Phases IB and II multidose trial of gadolinium texaphyrin, a radiation sensitizer detectable at MR imaging: preliminary results in brain metastases. Radiology. 1999;212(3):755-9.
12. Francis D et al, Motexafin gadolinium: a novel radiosensitizer for brain tumors. Expert Opin Pharmacother. 2009;10(13):2171-80.
13. Young SW et al, Gadolinium(III) texaphyrin: a tumor selective radiation sensitizer that is detectable by MRI. Proc. Natl. Acad. Sci. USA 1996;93(13):6610-6615.
14. Parise RA, Miles DR, Egorin MJ, Sensitive high-performance liquid chromatographic assay for motexafin gadolinium and motexafin lutetium in human plasma. Journal of Chromatography B, 2000;749(2):145–152.
15. Khuntia D, Mehta M, Motexafin gadolinium: a clinical review of a novel radioenhancer for brain tumors. Expert Rev Anticancer Ther. 2004;4(6):981-9.
16. Biaglow JE, Miller RA, The thioredoxin reductase/thioredoxin system: Novel redox targets for cancer therapy. Cancer Biol Ther. 2005;4(1):6-13.
17. Donnelly ET et al, Effects of texaphyrins on the oxygenation of EMT6 mouse mammary tumors. Int J Radiat Oncol Biol Phys. 2004;58(5):1570-6.
18. Magda D, Miller RA, Motexafin gadolinium: a novel redox active drug for cancer therapy. Semin Cancer Biol. 2006;16(6):466-76.
19. Mehta MP, Khuntia D, Current strategies in whole-brain radiation therapy for brain metastases. Neurosurgery 2005;57:S4-33-S4-44.
20. De Stasio G et al, Gadolinium in human glioblastoma cells for gadolinium neutron capture therapy. Cancer Res. 2001; 61: 4272.
21. Evans JP et al, Motexafin Gadolinium-induced cell death correlates with Heme oxygenase-1 expression and inhibition of P450 reductase-dependent activities. Mol Pharmacol. 2007;71:193–200.