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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
TransMolecular receives FDA approval for 131-I-TM-601 IND application.
2002 Apr
Patents
Substance Class Protein
Created
by admin
on Fri Dec 15 15:31:43 GMT 2023
Edited
by admin
on Fri Dec 15 15:31:43 GMT 2023
Protein Type PEPTIDE
Protein Sub Type
Sequence Origin INSECT
Sequence Type COMPLETE
Record UNII
544WOQ7W6W
Record Status Validated (UNII)
Record Version
  • Download
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
PRIMARY
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
PRIMARY
From To
1_2 1_19
1_5 1_28
1_16 1_33
1_20 1_35
Related Record Type Details
TARGET->RADIOLIGAND
NON-LABELED -> LABELED
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:CALCULATED CHEMICAL
Molecular Formula CHEMICAL