Rosuvastatin Zinc

Pictured: AstraZeneca’s production plant in Sweden iStock, Roland Magnusson AstraZeneca on Wednesday unveiled Phase I results for its PCSK9 inhibitor, acquired from Dogma Therapeutics in 2020, which when combined with a statin reduced LDL-C levels in patients with high “bad” cholesterol. AstraZeneca announced Wednesday Phase I trial data for its PCSK9 inhibitor, AZD0708, which showed a statistically significant reduction of low-density lipoprotein cholesterol in patients with high “bad” cholesterol or hypercholesterolemia. The trial investigated the safety, tolerability and pharmacodynamics of AZD0780 in lowering low-density lipoprotein cholesterol (LDL-C) levels. The results demonstrated that the candidate reduced LDL-C levels by 52% for patients also taking rosuvastatin, a statin that helps reduce bad cholesterol and raise good cholesterol. AZD0780 also showed a 78% total reduction from the baseline in treatment-naïve patients with hypercholesterolemia. AstraZeneca said preliminary data comparing dosing with food versus fasting shows more “dosing flexibility” with food. No serious adverse events were recorded and AZD0708 was well tolerated, according to the company. “The role of PCSK9 in cholesterol management is well established, and the compelling data generated with AZD0780 demonstrate the potential of this molecule for effective inhibition of this target and a possible next generation treatment for people with cardiovascular disease,” Sharon Barr, executive vice president of biopharmaceuticals R&D at AstraZeneca, said in a statement. “AZD0780 inhibits PCSK9 via a novel, previously unexplored, mode of action that is compatible with traditional oral small molecule drug discovery.” Barr added that AstraZeneca is “progressing development” of AZD0780 as an oral medicine for patients who cannot meet LDL-C targets with statins alone to reduce the risk of cardiovascular events. The pharma picked up the candidate in 2020 from Dogma Therapeutics for an undisclosed amount, intending to treat dyslipidemia. AZD0780 moved into a Phase II clinical trial in patients with dyslipidemia earlier this year. Dyslipidemia elevates the level of fats or lipids and can increase the risk of clogged arteries, leading to further health issues such as heart attack or stroke. The PCSK9 market has attracted several big drugmakers. Novartis’ Leqvio generated $151 million in revenue in the first quarter of 2024, a 136% jump from last year, while Amgen’s Repatha raked in $517 million in Q1 2024, a 33% increase compared to the same period in 2023. However, AstraZeneca potentially faces other competition as other PCSK9 inhibitors have shown encouraging clinical trial results. Merck announced last year that a Phase IIb study evaluating its PCSK9 inhibitor MK-0616 in hypercholesterolemia patients had “significantly” reduced LDL-C levels from the placebo, with the placebo-adjusted reduction from the baseline ranging from 41.2% to 60.9%. Merck’s candidate is currently in a Phase III trial . Tyler Patchen is a staff writer at BioSpace . You can reach him at tyler.patchen@biospace.com . Follow him on LinkedIn .

8月16日，国家药监局发布要闻，信达生物申报的1类新药托莱西单抗注射液获批上市，用于治疗原发性高胆固醇血症和混合型血脂异常的成人患者，成为国内首款获批的国产抗PCSK9单抗。米内网数据显示，2022年中国三大终端六大市场（统计范围详见本文末）血脂调节剂市场规模超过220亿元，国内已获批进口的2款抗PCSK9单抗2022年合计销售额超过9亿元。 托莱西单抗注射液是信达生物自主研发的IgG2全人源单克隆抗体，能特异性结合PCSK9分子，通过减少PCSK9介导的低密度脂蛋白受体(LDLR)内吞来增加LDLR水准，继而增加低密度脂蛋白胆固醇(LDL-C)清除，降低LDL-C水准，最终达到降低血脂的目的。 此前国内已获批上市的抗PCSK9单抗 在托莱西单抗注射液之前，国内已有两款抗PCSK9单抗获批进口，分别为安进的依洛尤单抗（2018/8）、赛诺菲的阿利西尤单抗（2019/12）。2款产品2022年在中国三大终端六大市场的销售额合计超过9亿元，其中依洛尤单抗的销售额突破6亿元。 近年来中国三大终端六大市场依洛尤单抗销售情况（单位：万元） 此外，国内还有多款国产抗PCSK9单抗已报产在审，包括君实生物的重组人源化抗PCSK9单抗注射液、康方生物的伊努西单抗注射液、恒瑞医药的注射用瑞卡西单抗等。 国内报产在审的国产抗PCSK9单抗 米内网数据显示，近年来中国三大终端六大市场血脂调节剂的销售规模有所波动，但一直维持在200亿元以上。 近年来中国零售药店终端血脂调节剂销售情况（单位：万元） 从细分终端看，血脂调节剂在院内市场（公立医院+公立基层医疗）受集采影响，销售规模下滑较多，2022年虽然止跌，但离集采前仍有一定差距；零售药店不受影响，近年来销售规模逐年上涨，2022年接近59亿元。 2022年中国零售药店终端血脂调节剂TOP10产品 注：低于1亿元用-代表来源：米内网格局数据库 在2022年中国零售药店终端血脂调节剂TOP10产品中，阿托伐他汀钙片以超26亿的销售额独占鳌头，瑞舒伐他汀钙片以超15亿元的销售额紧接在后，2款抗PCSK9单抗依洛尤单抗注射液、阿利西尤单抗注射液均上榜。 资料来源：米内网数据库、国家药监局官网等 内容来源于网络，如有侵权，请联系删除。