We evaluated the effectiveness of L-arginine mono(2-mercaptoethanesulfonate) (argimesna) to limit the extent of myocardial damage resulting from 60 minutes of severe ischemia followed by 30 minutes of reperfusion in the Langendorff-perfused rabbit heart. Argimesna is a sulfhydryl group containing molecule which has no effect on glutathione status or on the total thiol pool. The effects of 10(-6) M argimesna were compared with those of 10(-6) M L-arginine and of 10(-6) M sodium salt of 2-mercaptoethanesulfonate (mesna). Pretreatment of the hearts with 10(-6) M argimesna resulted in marked myocardial protection, measured in terms of improved recovery of developed pressure (p less than 0.01), reduced release of creatine kinase (p less than 0.01), maintenance of mitochondrial function and increased stores of ATP on reperfusion (p less than 0.01). On reperfusion less oxidative stress developed, as indicated by less accumulation of oxidized glutathione (p less than 0.01). These effects were specific for argimesna; no significant protection could be found for mesna and L-arginine. The beneficial effects of argimesna could not be explained by hemodynamic differences or effects on anaerobic metabolism. Neither is it likely that argimesna acts as a free radical scavenger at the concentrations employed. The protection may be achieved by maintenance of -SH groups during ischemia and reperfusion.

01 Apr 1992·Annals of OncologyQ1 · MEDICINE

Feasibility and efficacy of arginine 2-mercaptoethanesulfonate (ARGIMESNA) in the prevention of hemorragic cystitis from ifosfamide (IFO)

Q1 · MEDICINE

Article

Author: G. Lo Re ; D. Errante ; S. Monfardini ; R. Sorio ; S. Frustaci ; A. De Pascale ; A. Freschi ; S. Foladore

Tolerability and efficacy of the new uroprotective agent ARGIMESNA was assessed within a randomized cross-over study comparing it to sodiummercaptoethanesulfonate (MESNA), in patients treated with IFO. MESNA i.v., 20% of IFO dose, was given to all patients before chemotherapy; 4 h later, at random, they received ARGIMESNA p.o., 20% of IFO dose every 2 h x 4, or MESNA p.o., 40% of IFO dose every 4 h x 2. Overall, 78 cycles of oral uroprotection were administered: 37 for ARGIMESNA capsules; 41 for MESNA vials p.o. ARGIMESNA was subjectively better tolerated, determining gastro-intestinal discomfort in only 12 out of 37 cycles versus 34/41 of MESNA p.o. (p less than 0.001). Both preparations were equivalent for subjective and objective efficacy since no cycles were complicated by urinary symptoms (dysuria, stranguria, or hematuria). Nevertheless, 2 patients (7.7%) refused further oral assumption of both uroprotectors, whereas MESNA i.v. was added in other 7 patients because of nausea and vomiting caused by chemotherapy. In conclusion, this new oral preparation of mercaptoethanesulfonate turned out to be well tolerated, safe and active in the prevention of haemorrhagic cystitis from IFO.

01 Feb 1992·Pharmacological ResearchQ2 · MEDICINE

Serum concentrations of sodium 2-mercaptoethanesulfonate (MESNA) and its metabolite, disulfide form (DIMESNA), in volunteers after oral dosing: A comparison between mesna and argimesna.

Q2 · MEDICINE

Article

Author: Edoardo Casiglia ; F Pea ; V. Moretti ; A Pessina ; M Mazzo ; Pa Miglioli

Male volunteers were given MESNA (I) 1800 mg) or ARGIMESNA (II), the arginine salt of 2-mercaptothanesulfonate) (920 mg) and blood samples were collected at 0, 0.25, 0.5, 1, 2, 4 and 8 h after each administration.Serum levels of I were higher 2-8 h after II.AUC_(0-8h) values were greater after II administration.No differences were found in levels and AUC_(0-8h) of DIMESNA after administration of either I or II.Thus II has a better oral availability than I.

100 Deals associated with Argimesna

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Indication	Highest Phase	Country/Location	Organization	Date
Bladder Cancer	Phase 2	DE	Bayer Schering Pharma AG	-
Bladder Cancer	Phase 2	IT	Farmades	-
Bladder Cancer	Phase 2	-	Bayer AG	-
Cystitis	Phase 2	DE	Bayer Schering Pharma AG	-
Cystitis	Phase 2	IT	Farmades	-
Cystitis	Phase 2	-	Bayer AG	-
Nephritis	Phase 2	IT	Farmades	-
Nephritis	Phase 2	DE	Bayer Schering Pharma AG	-
Nephritis	Phase 2	-	Bayer AG	-

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