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Chlorotoxin I-131 is a synthetic version of a neurotoxin investigated in clinical trials for treating brain cancer. Chlorotoxin was originally isolated from the venom of the Israeli scorpion Leiurus quinquestriatus, and has potential as a tumor imaging agent based on its selective binding to tumor cells. Molecular targets for Chlorotoxin include voltage-gated chloride channels (GCC), calcium-dependent phospholipid-binding protein Annexin-2, and the inducible extracellular enzyme Matrix Metalloproteinase-2 (MMP-2). Chlorotoxin reduced the migration ability of glioma cells through tight extracellular spaces in the brain tissue by inhibition of the MMP2 because this prevented the cells from shrinking and releasing from the extracellular matrix. Chlorotoxin is a small 36-amino-acid peptide that selectively binds to glioma cells but not normal brain parenchyma. The synthetic version of this peptide has been manufactured and covalently linked to iodine 131 as a means of targeting radiation to tumor cells in the treatment of brain cancer.

Approval Year

PubMed

PubMed

TitleDatePubMed
Use of chlorotoxin for targeting of primary brain tumors.
1998 Nov 1
TransMolecular receives FDA approval for 131-I-TM-601 IND application.
2002 Apr
Phase I single-dose study of intracavitary-administered iodine-131-TM-601 in adults with recurrent high-grade glioma.
2006 Aug 1
Targeted delivery of antitumoral therapy to glioma and other malignancies with synthetic chlorotoxin (TM-601).
2007 Mar
Patents
Name Type Language
CHLOROTOXIN I-131
Common Name English
131-I-TM-601
Common Name English
TM-601 I-131
Common Name English
I(131)-TM-601
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 152201
Created by admin on Fri Dec 15 15:31:43 GMT 2023 , Edited by admin on Fri Dec 15 15:31:43 GMT 2023
Code System Code Type Description
DRUG BANK
DB05462
Created by admin on Fri Dec 15 15:31:43 GMT 2023 , Edited by admin on Fri Dec 15 15:31:43 GMT 2023
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FDA UNII
544WOQ7W6W
Created by admin on Fri Dec 15 15:31:43 GMT 2023 , Edited by admin on Fri Dec 15 15:31:43 GMT 2023
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