Benznidazole

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Chemical Structure| 22994-85-0 同义名 : Ro 71051;Ro 07-1051;Rochagan.;NSC 299972;Radanil;Benznidazol
CAS号 : 22994-85-0
货号 : A398551
分子式 : C12H12N4O3
纯度 : 99%+
分子量 : 260.249
MDL号 : MFCD00243089
存储条件:

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(192.12 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Benznidazole is recommended for treatment of Chagas infection. Benznidazole monotherapy is superior to posaconazole, with high RT-PCR (real time polymerase chain reaction) conversion rates sustained at 1 year. Side effects lead to therapy discontinuation in 32%. No advantages were observed with combined therapy versus benznidazole monotherapy[3]. Benznidazole shows high bioavailability after oral administration. Benznidazole at 5 - 8 mg/kg/day and 5 - 10 mg/kg/day for 30 - 60 days are consistent clinical recommendations for children and adults, respectively[4]. The trypanocidal activity of vitamin C and benznidazole was similar for the three parasite forms. Animals treated with benznidazole presented lower parasitemia levels, as compared with those treated with vitamin C alone. Again, vitamin C did not cause any effect on the antiparasitic profile of benznidazole. The combination of vitamin C with benznidazole could be considered as an alternative treatment for Chagas' disease[5]. Patients previously treated with benznidazole had significantly reduced parasitemia, a lower prevalence of markers of severe cardiomyopathy, and lower mortality after two years of follow-up. If used in the early phases, benznidazole treatment may improve clinical and parasitological outcomes in patients with chronic ChD (chronic Chagas disease)[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02625974 Chagas Disease Phase 3 Active, not recruiting August 9, 2021 Argentina ... 展开 >> La Plata, Buenos Aires, Argentina, 1900 Buenos Aires, Ciudad Auton. De Buenos Aires, Argentina, 1281 Buenos Aires, Ciudad Auton. De Buenos Aires, Argentina, C1270AAN Buenos Aires, Ciudad Auton. De Buenos Aires, Argentina, C1425AGP Buenos Aires, Ciudad Auton. De Buenos Aires, Argentina, C1425EFD San Salvador de Jujuy, Jujuy, Argentina, 4600 Posadas, Misiones, Argentina Rosario, Santa Fe, Argentina, 2000 Corrientes, Argentina, W3400CBI Formosa, Argentina, P3600HZL La Rioja, Argentina Mendoza, Argentina, 5500 Mendoza, Argentina, 5535 Salta, Argentina, 4400 Salta, Argentina, A4400ESE San Juan, Argentina, 5400 Santiago del Estero, Argentina, 4202 Tucuman, Argentina, 4000 Bolivia Cochabamba, Bolivia Punata, Bolivia Tarija, Bolivia Colombia Barranquilla, Atlántico, Colombia Yopal, Casanare, Colombia, 0 Santa Marta, Magdalena, Colombia, 0 Floridablanca, Santander, Colombia 收起 <<
NCT01377480 Chagas Disease Phase 2 Completed - -
NCT01377480 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.84mL

0.77mL

0.38mL

19.21mL

3.84mL

1.92mL

38.42mL

7.68mL

3.84mL

参考文献

[1]Perin L, Moreira da Silva R, et al. Pharmacokinetics and Tissue Distribution of Benznidazole after Oral Administration in Mice. Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: e02410-16.

[2]Maranon C, Egui A, et al. Benznidazole treatment reduces the induction of indoleamine 2,3-dioxygenase (IDO) enzymatic activity in Chagas disease symptomatic patients. Parasite Immunol. 2013 May-Jun;35(5-6):180-7.

[3]Morillo CA, Waskin H, Sosa-Estani S, et al. Benznidazole and Posaconazole in Eliminating Parasites in Asymptomatic T. Cruzi Carriers: The STOP-CHAGAS Trial. J Am Coll Cardiol. 2017;69(8):939‐947

[4]Caldas IS, Santos EG, Novaes RD. An evaluation of benznidazole as a Chagas disease therapeutic. Expert Opin Pharmacother. 2019;20(15):1797‐1807

[5]Puente V, Demaria A, Frank FM, Batlle A, Lombardo ME. Anti-parasitic effect of vitamin C alone and in combination with benznidazole against Trypanosoma cruzi. PLoS Negl Trop Dis. 2018;12(9):e0006764. Published 2018 Sep 21

[6]Cardoso CS, Ribeiro ALP, Oliveira CDL, et al. Beneficial effects of benznidazole in Chagas disease: NIH SaMi-Trop cohort study. PLoS Negl Trop Dis. 2018;12(11):e0006814. Published 2018 Nov 1