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.

阿斯利康周三宣布了其PCSK9抑制剂AZD0708的I期临床试验数据，该数据显示高“坏”胆固醇或高胆固醇血症患者的低密度脂蛋白胆固醇有统计学显着降低。

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.

该试验调查了AZD0780降低低密度脂蛋白胆固醇（LDL-C）水平的安全性，耐受性和药效学。结果表明，对于同时服用瑞舒伐他汀（一种他汀类药物，有助于降低坏胆固醇和提高好胆固醇）的患者，候选人将LDL-C水平降低了52%。

AZD0780 also showed a 78% total reduction from the baseline in treatment-naïve patients with hypercholesterolemia..

AZD0780在未接受治疗的高胆固醇血症患者中也显示出比基线总减少78%。。

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.

阿斯利康表示，比较食物与禁食给药的初步数据显示，食物的“给药灵活性”更高。据该公司称，没有记录到严重的不良事件，AZD0708的耐受性良好。

“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.

阿斯利康生物制药研发执行副总裁莎伦·巴尔（SharonBarr）在一份声明中表示：“PCSK9在胆固醇管理中的作用已经确立，AZD0780产生的令人信服的数据表明，这种分子具有有效抑制这一靶点的潜力，并可能成为心血管疾病患者的下一代治疗方法。”。

“AZD0780 inhibits PCSK9 via a novel, previously unexplored, mode of action that is compatible with traditional oral small molecule drug discovery.”.

“AZD0780通过一种与传统口服小分子药物发现兼容的新型，以前未被探索的作用模式抑制PCSK9。”。

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.

巴尔补充说，阿斯利康正在“逐步开发”AZD0780，作为一种口服药物，用于单独使用他汀类药物无法达到LDL-C目标的患者，以降低心血管事件的风险。

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..

该制药公司于2020年从Dogma Therapeutics公司（Dogma Therapeutics）获得了该候选人，但金额未透露，旨在治疗血脂异常。今年早些时候，AZD0780进入了血脂异常患者的II期临床试验。血脂异常会升高脂肪或脂质的水平，并可能增加动脉阻塞的风险，从而导致心脏病发作或中风等进一步的健康问题。。

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.

PCSK9市场吸引了几家大型制药商。诺华的Leqvio在2024年第一季度实现了1.51亿美元的收入，比去年增长了136%，而安进的Repatha在2024年第一季度实现了5.17亿美元的收入，比2023年同期增长了33%。

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%.

然而，阿斯利康可能面临其他竞争，因为其他PCSK9抑制剂已显示出令人鼓舞的临床试验结果。默克公司去年宣布，一项评估其PCSK9抑制剂MK-0616在高胆固醇血症患者中的IIb期研究显示，安慰剂组的LDL-C水平“显着”降低，安慰剂组的基线水平从41.2%降至60.9%。

Merck’s candidate is currently in a Phase III trial..

默克公司的候选人目前正在进行III期试验。。