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Published in V.K. Kapoor, Hans G. Beger, Acute Pancreatitis, 2017
Gabexate mesilate—an inhibitor of protease—has NOT been found to be of use in acute pancreatitis. It may, however, help to reduce the incidence of acute pancreatitis induced by endoscopic retrograde cholangiography (ERC).
Biliary endoscopy
Published in Nizar Zein, Bret Lashner, The Year in Gastroenterology and Hepatology, 2005
This is another multicentre Italian study with an exceedingly low rate of ERCPinduced pancreatitis. The slightly higher rate of pancreatitis in the shorter gabexate infusion was not clinically or statistically significant. The shorter infusion duration of gabexate is a reasonable method of reducing the incidence of ERCP-induced pancreatitis. The main barrier to gabexate seemed to be the cost associated with infusion of the drug, and these authors are to be commended for addressing these issues by examining the optimal duration of treatment. Gabexate is not widely available but these studies should prompt other investigators to examine the drug for use in other countries.
Trends and recent developments in pharmacotherapy of acute pancreatitis
Published in Postgraduate Medicine, 2023
Juliana Hey-Hadavi, Prasad Velisetty, Swapnali Mhatre
Gabexate is a synthetic serine protease inhibitor, reported to improve the microcirculatory environment in acute experimental pancreatitis model in rats [73]. Moreover, gabexate is also known to regulate inflammatory cytokines [67]. In a prospective and double-blind study, the efficacy of somatostatin with or without ulinastatin and gabexate for the treatment of SAP was evaluated. Inflammatory cytokines including TNFα, IL-6, and IL-8 levels decreased significantly and immunosuppressive cytokine IL-10 levels increased significantly after the treatment with somatostatin, ulinastatin, and/or gabexate compared with somatostatin alone. In contrast, significant decrease in frequency of MODS, mortality, and complication was observed only in the somatostatin, ulinastatin, and/or gabexate as compared with somatostatin alone. There were no statistical differences between somatostatin and gabexate compared with somatostatin alone, and between somatostatin, ulinastatin, and gabexate compared with somatostatin and ulinastatin. Thus, gabexate could alleviate clinical symptoms and shorten the course of the disease, however, could not improve the effective ratio or decrease MODS, mortality, and complication [74].
The discovery and development of transmembrane serine protease 2 (TMPRSS2) inhibitors as candidate drugs for the treatment of COVID-19
Published in Expert Opinion on Drug Discovery, 2022
Christiana Mantzourani, Sofia Vasilakaki, Velisaria-Eleni Gerogianni, George Kokotos
Gabexate mesilate (8, Figure 3) is a TMPRSS2 inhibitor, which has been approved for use in Italy and Japan for the treatment of pancreatitis and disseminated intravascular coagulation [91]. It has been established that gabexate mesilate can inhibit influenza virus A and B in vitro in MDCK and human tracheal epithelial cells [57,76], and in vivo in a murine model [92]. This inhibitor is similar to camostat and nafamostat in structure, but less effective in most cases. Recently, in an enzymatic TMPRSS2 assay, Shrimp et al. reported that gabexate mesilate inhibited TMPRSS2 with an IC50 value of 130 nM and was the least potent compound compared to nafamostat mesilate (IC50 0.27 nM), camostat mesilate (IC50 6.2 nM) and FOY-251 (IC50 33.3 nM), while bromhexine hydrochloride showed no inhibition of TMPRSS2 [93].
The effectiveness of Hemopatch™ in preventing postoperative distal pancreatectomy fistulas
Published in Expert Review of Medical Devices, 2019
Anna Pisapia, Enrico Crolla, Michele Saracco, Alessandro Saglioccolo, Pasquale Dolce, Carlo Molino
We analyzed all patients who underwent DP from January 2014 to December 2017. Hemopatch™ started to be applied to pancreatic stumps in all cases after January 2016. During that period, 57 (30 male) patients underwent DP. Taking device availability into account, the sample was divided into two different groups: group A (treated without Hemopatch™, 18 patients) and group B (treated with Hemopatch™, 39 patients). Patients included men and women aged from 34 to 75 years with a body mass index (BMI) ranging from 18 to 28 kg/m2. All patients underwent preoperative staging evaluation, standard prophylaxis for pulmonary embolism according to American guidelines [3], and received postoperative prophylactic treatment with gabexate mesylate. A postoperative drain was placed in all patients, and an evaluation of fluid amylase (DFA) at postoperative days (POD) 1 and 3 was performed. Drain removal occurred when DFA at POD 3 was lower than two times the upper amylase serum standard level. Demographic, surgical (technique, time, associated splenectomy, collagen pad usage), blood transfusion, and postoperative complication data were collected.