Altretamine hydrochloride

Altretamine is an antineoplastic agent with antiproliferative activity.¹ It induces cytotoxicity in an ovarian cancer cell line when used at a concentration of 10 μg/ml, with radiolabeled thymidine uptake equal to 102 and 75% of controls after 48 and 120 hours, respectively.² Altretamine (100 μg/ml) reduces colony survival in A204 human rhabdomyosarcoma cells in an NADP-dependent manner in the presence of an S-9 hepatic activating mixture.³ In vivo, altretamine (150 mg/kg) reduces tumor growth in a mouse model of M5076 murine reticulum cell sarcoma.¹ Altretamine (0.5 mM) inhibits glutathione peroxidase 4 (GPX4) and induces accumulation of lipid-reactive oxygen species (ROS) in U-2932 cells without depleting glutathione (GSH) levels, suggesting it is a class II ferroptosis-inducing compound (FIN).⁴ It also acts as a chemosterilant in houseflies, preventing hatching and pupation in male and female houseflies when used at a concentration of 0.05%.⁵ Formulations of altretamine have been used in the treatment of various cancers.

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