U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
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
Targeted delivery of antitumoral therapy to glioma and other malignancies with synthetic chlorotoxin (TM-601).
2007-03
Phase I single-dose study of intracavitary-administered iodine-131-TM-601 in adults with recurrent high-grade glioma.
2006-08-01
TransMolecular receives FDA approval for 131-I-TM-601 IND application.
2002-04
Use of chlorotoxin for targeting of primary brain tumors.
1998-11-01
Patents
Substance Class Protein
Created
by admin
on Mon Mar 31 18:00:07 GMT 2025
Edited
by admin
on Mon Mar 31 18:00:07 GMT 2025
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
I(131)-TM-601
Preferred Name English
131-I-TM-601
Common Name English
TM-601 I-131
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 152201
Created by admin on Mon Mar 31 18:00:08 GMT 2025 , Edited by admin on Mon Mar 31 18:00:08 GMT 2025
Code System Code Type Description
DRUG BANK
DB05462
Created by admin on Mon Mar 31 18:00:08 GMT 2025 , Edited by admin on Mon Mar 31 18:00:08 GMT 2025
PRIMARY
SMS_ID
100000183818
Created by admin on Mon Mar 31 18:00:08 GMT 2025 , Edited by admin on Mon Mar 31 18:00:08 GMT 2025
PRIMARY
FDA UNII
544WOQ7W6W
Created by admin on Mon Mar 31 18:00:08 GMT 2025 , Edited by admin on Mon Mar 31 18:00:08 GMT 2025
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

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID SUBSTITUTION [1_29] TYROSINE IOTYROSINE I-131 Q1M94GA18P
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:CALCULATED CHEMICAL
Molecular Formula CHEMICAL