A new blood pressure lowering drug, alisartan axetil, will be on the market soon

The API workshop of alisartan ester, a new blood pressure lowering drug of xinlitai, has passed the new GMP certification and will soon be put into production for the production of alisartan ester tablets, which means that alisartan ester tablets will be put on the market soon According to the website of Jiangsu food and drug administration, the API workshop of Jiangsu Ellis biomedical Co., Ltd has passed the new GMP certification, which is valid until December 18, 2018 The workshop is mainly used to produce the API of alisartan ester, the latest class a new drug approved by xinlitai in October 2013 Before that, alisartan ester tablet has successfully obtained new drug certificate, production approval and GMP certificate of preparation workshop, only lacking raw material supply Yang Jianfeng, Secretary of the board of directors of xinlitai, confirmed that the company knew that the above API workshop had passed the certification, and that it was about to put into production the alisartan ester API, which was used for tablet production The product will soon be put on the market on a small scale "After the new product is put on the market, it will take time to promote, so the sales volume of alisartan ester tablets is limited in the short term." Alisartan ester tablet is a class 1.1 new drug independently developed by Shanghai ALIS, the parent company of Jiangsu ALIS, a domestic manufacturer The domestic patent protection period is until 2026 In October 2012, xinlitai purchased the preparation production technology related to alisartan ester for 340 million yuan Jiangsu ALIS is responsible for the production of alisartan ester API, and xinlitai is responsible for the production and sales of alisartan ester tablets The company expects sales of the product to be at least 1 billion yuan in the future According to the official website of xinlitai, as a new antihypertensive drug, alisartan ester tablet has a better therapeutic effect than losartan potassium It has the characteristics of early onset, better antihypertensive consistency at different treatment times, and less fluctuation It has a large market capacity in the treatment field, and is also rated as "China's top ten heavyweight prescription drugs in 2013" with this advantage, ranking second Chinese Name: alisartan ester, also known as: alisartan ester, English Name: Allisartan isoproxil, alisartan ester is an antagonist of angiotension II receptor (there are 8 kinds of such drugs on the market in China, including valsartan, irbesartan, candesartan ester, ipsartan, irbesartan Telmisartan, losartan potassium and olmesartan ester), which are non peptide prodrugs, are completely hydrolyzed by esterase into the only metabolite exp3174 during gastrointestinal absorption Exp3174 is one of the metabolites of losartan, which has been listed on the market Losartan mainly plays a pharmacological role through the prototype drugs and active metabolites According to the literature, about 14% of losartan is metabolized into active exp3174 in the human liver, the latter is more firmly bound to AT1 receptor, and its dissociation constant is 5 times that of its mother Pharmacokinetic characteristics of the product: it is well absorbed orally and rapidly generates active metabolite E3174 after ester hydrolysis The peak time of E3174 is 1.5-2.5h, and its half-life is about 10h In the dose range of 60mg to 240mg, the relationship between Cmax and drug dose was established; auclast increased with the increase of dose, the auclast of E3174 in 60mg, 120mg and 240mg was 1.33, 2.62 and 4.43 HR * mg / L, respectively; the auclast of E3174 in liver metabolism was 4.76 HR * mg / L in 100mg of losartan potassium There was no significant accumulation of active metabolites in plasma when 240 mg was taken orally once a day The binding rate of active metabolites to human plasma protein was more than 99.7% Food will reduce the absorption of this product, Cmax decreased by 38.4%, auclast decreased by 35.5% No pharmacokinetic study and drug interaction study were conducted in special population 283 hypertensive subjects were compared with losartan potassium for 8 weeks The results showed that the sitting blood pressure of 80, 160, 240mg and 50mg groups decreased by 8.18/5.84, 11.14/7.71, 12.48/8.82 and 12.22/7.89 mmHg on average compared with baseline After 8 weeks of treatment, the percentage of sitting blood pressure (SBP / DBP < 140mmHg / 90mmHg) was 39.13%, 47.06%, 50.00% and 44.29% in the 80, 160, 240mg and 50mg groups, respectively There was no statistical difference between the groups Among them, the antihypertensive effect of the 240 mg group is the closest to that of the 50 mg group No special security issues were found Two key clinical trials were conducted, one compared with losartan potassium and the other with placebo, with a study period of 12 weeks The results showed that the antihypertensive effect of 240 mg of alisartan axetil tablet was not inferior to that of 50 mg of losartan potassium, and it had earlier onset, better antihypertensive consistency and less fluctuation in different treatment time The ratio of valley to peak of 240 mg of alisartan ester was greater than 0.6, and the antihypertensive effect of the drug could be maintained for 24 hours Compared with the placebo group, the difference between the two groups was 2.6mmhg (9.98mmhg in the alisartan group and 7.40mmhg in the placebo group) after 8 weeks of treatment There was a statistical difference between the two groups (P = 0.0066) A long-term follow-up study was carried out in 124 subjects at 56 weeks after entry From 16 weeks to 64 weeks after treatment, the sitting diastolic / systolic blood pressure of each visiting point showed a steady downward trend compared with the baseline level When it dropped to a certain level, the systolic blood pressure tended to be stable about 32 weeks after treatment and the diastolic blood pressure tended to be stable about 40 weeks after treatment From the 16th week to the 64th week, the overall effective rate is more than 70% and the overall rate is more than 60% Alisartan axetil tablets (240mg) have good safety and tolerance in the treatment of moderate and low-risk essential hypertension.