Allisartan isoproxil (ALS-3) is an orally potent, selective, non-peptide inhibitor of Angiotensin II Type 1. Allisartan isoproxil is also an antipertensive agent. Allisartan isoproxil may inhibit angiotensin-aldosterone system and oxidative stress. Allisartan isoproxil lowers blood pressure and protects the organs, preventing cerebrovascular damage. Allisartan isoproxil (80-320 mg/kg/d) has shown toxicity in rat models by targeting liver organs[1][2].
Allisartan isoproxil 的代谢途径相对简单，Allisartan isoproxil 在胃肠道吸收过程中通过酯酶完全直接转化为EXP-3174[1]。
Allisartan isoproxil (20、80和320 mg/kg；口服；26 周) 在 80-320 mg/kg/天的剂量下，会减轻 Sprague-Dawley 大鼠的体重[1]。
Allisartan isoproxil (30mg /kg/天；口服；55 周) 显著降低卒中易感肾血管性高血压大鼠 (RHR-SP) 的相关死亡，延长寿命[2]。
| Animal Model: | Femal and male Sprague-Dawley rats[1] |
| Dosage: | 20, 80 and 320 mg/kg |
| Administration: | |
| Result: | Decreased body-weight gain at 320 mg/kg/day in both sexes as well as at the 80-mg/kg/day dose in females. Decreased erythrocyte parameters in males, and decreased heart weight and exacerbation of chronic progressive nephropat (CPN) severity in males at 80 and 320 mg/kg/day. |
[1]. Liu Y, et al. A 26-week repeated-dose toxicity study of allisartan isoproxil in Sprague-Dawley rats. Drug Chem Toxicol. 2013 Oct;36(4):443-50.
[2]. Ling QS, et al. Allisartan isoproxil reduces mortality of stroke-prone rats and protects against cerebrovascular, cardiac, and aortic damage. Acta Pharmacol Sin. 2021 Jun;42(6):871-884.