Drug intelligence / Profile preview

etanidazole

Development stage
Phase 2
Modality
Small Molecules
Administration
Intravenous
01

Overview

Etanidazole is a synthetic small molecule of the nitroimidazole class developed as a hypoxic radiosensitizer for use in cancer therapy. Its primary mechanism involves depleting glutathione and inhibiting glutathione S-transferase, which increases the sensitivity of hypoxic tumor cells to ionizing radiation. This effect is intended to enhance the efficacy of radiotherapy in solid tumors by targeting radioresistant hypoxic regions within tumors. Etanidazole was investigated primarily for use alongside radiotherapy in patients with advanced head and neck cancers and other solid tumors, but its development was discontinued after Phase III trials due to limited clinical benefit[1][2][3][5][7].

Brand names
Radinyl
Other names
EtanidazolEtanidazolumEthanidazole1H-Imidazole-1-acetamide, N-(2-hydroxyethyl)-2-nitro-N-(2-Hydroxyethyl)-2-nitroimidazole-1-acetamide
02

Targets

GST (Glutathione S-transferase alpha 3)

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