Temozolomide

Temozolomide is a prodrug form of the DNA alkylating agent MTIC (Item No. 18863).¹ It is converted to MTIC in a non-enzymatic manner under physiological conditions. Temozolomide is selectively cytotoxic to U87 and D54 glioblastoma cells, which do not express O⁶-methylguanine-DNA methyltransferase (MGMT), over MGMT-expressing T98G and U3054MG glioblastoma cells (IC₅₀s = 51, 12, 660, and 370 µM, respectively).² It increases survival in a Br23c glioblastoma orthotopic mouse xenograft model when administered at a dose of 15 mg/kg. Temozolomide, in combination with antibodies targeting CD47, decreases tumor volume and increases the number of tumor-infiltrating CD4⁺ and CD8⁺ T cells in a GL261 murine glioma model.³ Formulations containing temozolomide have been used in the treatment of glioblastoma multiforme (GBM) and refractory anaplastic astrocytoma.

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1. Tsang, L.L.H., Quarterman, C.P., Gescher, A., et al. Comparison of the cytotoxicity in vitro of temozolomide and dacarbazine, prodrugs of 3-methyl-(triazen-1-yl)imidazole-4-carboxamide. Cancer Chemother. Pharmacol. 27(5), 342-346 (1991).

2. Svec, R.L., Furiassi, L., Skibinski, C.G., et al. Tunable stability of imidazotetrazines leads to a potent compound for glioblastoma. ACS Chem. Biol. 13(11), 3206-3216 (2018).

3. von Roemeling, C.A., Wang, Y., Qie, Y., et al. Therapeutic modulation of phagocytosis in glioblastoma can activate both innate and adaptive antitumour immunity. Nat. Commun. 11(1), 1508 (2020).

Zhang, P., Rashidi, A., Zhao, J., et al. STING agonist-loaded, CD47/PD-L1-targeting nanoparticles potentiate antitumor immunity and radiotherapy for glioblastoma. Nat. Commun. 14(1), 1610 (2023).

von Roemeling, C.A., Wang, Y., Qie, Y., et al. Therapeutic modulation of phagocytosis in glioblastoma can activate both innate and adaptive antitumour immunity. Nat. Commun. 11(1), 1508 (2020).