Drug intelligence / Profile preview

temozolomide

Development stage
Approved
Lead developer
Merck
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Temozolomide is an oral alkylating agent used primarily to treat certain types of brain tumors, including glioblastoma multiforme and anaplastic astrocytoma. It is also sometimes used for other tumors such as neuroendocrine tumors and adrenal gland cancer. The drug works by methylating DNA at the O6 and N7 positions of guanine, leading to DNA damage that inhibits replication and triggers apoptosis in rapidly dividing tumor cells. Temozolomide is a prodrug that undergoes spontaneous hydrolysis to form the active compound MTIC (monomethyl triazeno imidazole carboxamide), which exerts its cytotoxic effects on tumor cells. It was first developed in the early 1980s at Aston University in Great Britain[1][2][4][6][8].

Brand names
TemodarTemodal
Other names
temozolomide
02

Targets

DNA

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