Dimesna

Dimesna (BNP-7787), the disulfide form of Mesna (HY-13679), is a platinum-related toxicity protective agent. Dimesna converts to Mesna, which in turn inactivates toxic platinum substances. Dimesna does not interfere with the antitumor activity of platinum compounds. Dimesna does not affect the antiproliferative effects of Cisplatin (HY-17394) or Carboplatin (HY-17393). Dimesna counteracts Cisplatin-induced nephrotoxicity. Dimesna exerts selective protective effects on the kidneys. Dimesna can be used in studies related to ovarian cancer and Cisplatin-induced nephrotoxicity^[2][3]. In Vitro:Dimesna (0-5.0 mmol/L; 1-24 h) alone exerts no effect on total protein, thymidine incorporation or uridine incorporation in LLC-PK1 cells, and fails to protect LLC-PK1 cells from toxicity induced by ifosfamide, cyclophosphamide, 4-hydroperoxyifosfamide, chloroacetaldehyde or acrolein^[1].
Dimesna (≥2.0×10³ μM; 96 h) does not reduce the antiproliferative effects of cisplatin or carboplatin on A2780 or OVCAR-3 ovarian cancer cells, and only inhibits the growth of these cells when exposed for 96 h at a concentration of ≥2.0×10³ μM^[2]. In Vivo:Dimesna (BNP-7787) (1000 mg/kg; i.v.) does not interfere with the antitumour activity of cisplatin or carboplatin in OVCAR-3 ovarian cancer xenografts, and co-administration with 60 mg/kg carboplatin results in significantly greater tumour growth inhibition than carboplatin alone (specific growth delay of 4.72 vs. 4.01 for carboplatin alone)^[2].
Dimesna (BNP-7787) (1000 mg/kg; i.v.; bolus injection) administered to tumour-bearing Fischer rats results in preferential accumulation of its metabolite mesna in the kidney, with kidney mesna AUC_0-t 4.5-fold higher than plasma mesna AUC_0-t, while maintaining low mesna levels in plasma and tumour tissue relative to mesna administration^[3].