temozolomide hexadecyl ester

Temozolomide hexadecyl ester (TMZ16e) is a lipophilic prodrug derivative of the alkylating agent temozolomide (TMZ), specifically engineered to enhance membrane permeability and brain targeting for the treatment of glioblastoma multiforme (GBM). By esterifying temozolomide with a 16-carbon hexadecyl chain, the molecule achieves higher lipophilicity, which facilitates its incorporation into nanoparticle delivery systems and improves its ability to bypass the blood-brain barrier. TMZ16e has demonstrated the ability to downregulate the expression of O6-methylguanine-DNA methyltransferase (MGMT), a key enzyme involved in DNA repair that frequently mediates resistance to standard temozolomide therapy. In preclinical studies, TMZ16e delivered via targeted PLGA nanoparticles (such as those modified with anti-EphA3 antibodies) through intranasal administration has shown significant anti-glioma activity, including the induction of apoptosis and reversal of drug resistance in T98G cell models.

Other names

temozolomide hexadecyl esterTMZ-hexadecyl ester