Thiotepa

CAS No:
52-24-4 Category:
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Product Details:

  • CAS No: 52-24-4
  • AHFC code:
  • Synonyms:
  • ATC Code: L01AC01
  • Chemical Formula: C14H14ClNS
  • Molecular Weight: 189.218
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB04572
  • SMILES: S=P(N1CC1)(N1CC1)N1CC1
  • InChl: FOCVUCIESVLUNU-UHFFFAOYSA-N
  • PubChem: 5453
  • IUPAC: tris(aziridin-1-yl)-$l^{5}-phosphanethione

Additional Details

Indication:
ThioTEPA is used a as conditioning treatment prior to allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT) in haematological diseases in adult and paediatric patients. Also, when high dose chemotherapy with HPCT support it is appropriate for the treatment of solid tumours in adult and paediatric patients.
Pharmacodynamics:
The unstable nitrogen-carbon groups alkylate with DNA causing irrepairable DNA damage. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Mode of Action:
The alkyl group is attached to the guanine base of DNA, at the number 7 nitrogen atom of the imidazole ring. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Metabolism:
Toxicity:
General Reference:
Maanen MJ, Smeets CJ, Beijnen JH: Chemistry, pharmacology and pharmacokinetics of N,Nê,N" -triethylenethiophosphoramide (ThioTEPA). Cancer Treat Rev. 2000 Aug;26(4):257-68. Pubmed Maanen MJ, Smeets CJ, Beijnen JH: Chemistry, pharmacology and pharmacokinetics of N,Nê,N" -triethylenethiophosphoramide (ThioTEPA). Cancer Treat Rev. 2000 Aug;26(4):257-68. Pubmed
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