Pharmaceutical Raw Powder Altretamine For Anti-Cancer CAS 645-05-6
An antitumor agent which also acts as a chemosterilant for male
houseflies and other insects. Antineoplastic.
The precise mechanism by which altretamine exerts its anti-cancer
effect is unknown but it is classified by MeSH as an alkylating
antineoplastic agent. This unique structure is believed to damage
tumor cells through the production of the weakly alkylating species
formaldehyde, a product of CYP450-mediated N-demethylation.
Administered orally, altretamine is extensively metabolized on
first pass, producing primarily mono- and didemethylated
metabolites. Additional demethylation reactions occur in tumor
cells, releasing formaldehyde in situ before the drug is excreted
in the urine.
The carbinolamine (methylol) intermediates of CYP450-mediated
metabolism also can generate electrophilic iminium species that are
capable of reacting covalently with DNA guanine andcytosine
residues as well as protein. Iminium-mediated DNA cross-linking and
DNA-protein interstrand cross-linking, mediated through both the
iminium intermediate and formaldehyde, have been demonstrated,
although the significance of DNA cross-linking on altretamine
antitumor activity is uncertain.
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