Amonafide L-malate

Amonafide L-malate is a naphthalimide derivative that possesses both DNA intercalation activity and topoisomerase II inhibitory activity. It can hinder the binding of topoisomerase II to DNA, induce DNA damage, activate apoptotic signaling pathways, and exhibit broad-spectrum antitumor activity.

Method: Amonafide L-malate (the study used the formulation name Xanafide) was applied for 48 h to MCF-7, MDA-MB-231, SKBR-3 and T47D human breast cancer cells, and growth was measured using the sulforhodamine-B assay in three independent experiments.
Result: Xanafide concentration-dependently inhibited growth, with mean GI₅₀ values of 5, 10, 6 and 20 μM in MCF-7, MDA-MB-231, SKBR-3 and T47D cells, respectively. MCF-7 was the most sensitive model, whereas complete growth inhibition was not reached in T47D cells.^[1]

Method: Amonafide L-malate (the study used the formulation name Xanafide) was administered intraperitoneally at 30 mg/kg once daily for 5 days to NCr nude mice implanted intraperitoneally and subcutaneously with hollow fibres containing MCF-7 or MDA-MB-231 cells.
Result: Xanafide reduced MCF-7 and MDA-MB-231 growth in intraperitoneal fibres by 41% and 46% and in subcutaneous fibres by 42% and 40%, respectively; body weight decreased by 12% by day 8.^[1]