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Performance is gradually showing: lipid-lowering "artifact" Novartis oligonucleotide new drug PCSK9 with 2 injections a year

 Last Update: 2023-02-05
 Source: Internet
 Author: User

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This article is only an introduction to medical and health-related drugs, and non-treatment options (if involved) are recommended and do not represent the position of
the platform.

Low-density lipoprotein cholesterol (LDL-C)

According to statistics, the number of patients with cardiovascular disease in China has reached 290 million, and an average of about 3.
5 million people die of cardiovascular disease
every year.
Elevated Low Density Lipoprotein Cholesterol (LDL-C) has been identified as one of the important factors in the pathogenesis of cardiovascular disease, especially in those at very high risk of cardiovascular disease within 1 year, which may cause relapse and threaten health and life
if not effectively intervened.
Data show that 80% of patients in very high-risk patient groups are unable to adequately control their LDL-C levels with existing treatments, implying an urgent need for innovative treatments
.
This is particularly urgent for patients with acute coronary syndromes (including myocardial infarction and unstable angina) who have been treated with statin therapy but whose LDL-C levels remain substandard
.

LDL-C level

According to the China Cardiovascular Health and Disease Report 2021, cardiovascular disease (CVD) accounted for 46.
74% and 44.
26% of deaths in rural and urban areas in 2019
, respectively.
Cardiovascular
disease accounts for 2 out of every 5 deaths.
Cardiovascular disease is still the "number one killer" of our residents
.
Hyperlipidemia is one of
the main risk factors for atherosclerotic cardiovascular disease (ASCVD).
Research data show that the treatment rate and control rate of dyslipidemia in people aged 18 and above in China are only 19.
5% and 8.
9%.

Atherosclerotic cardiovascular disease (ASCVD)

Dyslipidemia, especially elevated LDL-C levels, is a key factor in the occurrence and development of
ASCVD.
PCSK9 (proprotein convertase subtilisin-kexin type 9) inhibitors have been found to promote liver clearance of LDL-C, thereby reducing LDL-C levels
.
According to the data of WuRong Cloud, www.
pharnexcloud.
com shows that PCSK9 inhibitors include monoclonal antibodies, oral cyclic peptides, small molecules, ASO, siRNA, CRISPR gene editing and other drug
candidates worldwide.

PCSK9

▲Pharmarong Cloud Data www.
pharnexcloud.
com; Some new PCSK9 drugs

Inclisiran is injected subcutaneously twice a year

On June 28, 2020, the clinical application IND of the PCSK9 small molecule interfering RNA (siRNA, Small Interfering RNA Drug) cholesterol-lowering drug inclisiran, pioneered by Novartis, was accepted
by CDE in China for the first time 。 Novartis acquired The Medicines Company in November 2019 through the acquisition of The Medicines Company for US$9.
7 billion to obtain its core product PCSK9 RNAi product Inclisiran (the first new drug discovered by Alnylam), a long-acting synthetic new drug under development, related patents: WO-2007134161, WO-2009073809, WO-2014089313
.

WO-2007134161

▲Yao Rong Cloud Data: www.
pharnexcloud.
com

In March 2020, the results of three important Phase III clinical trials of Inclisiran for the treatment of hyperlipidemia in adults were published in the New England Journal of Medicine (NEJM).

All three trials met the primary endpoint and showed that twice-yearly subcutaneous inclisiran treatment resulted in a durable and significant reduction in LDL-C
compared with placebo after receiving two initial doses.
inclisiran is well tolerated and its safety profile is similar
to placebo.
It is used in adults with ASCVD or HeFH who receive lipid-lowering therapy at the maximum tolerated dose but still have elevated LDL-C levels
.

On December 11, 2020, Inclisiran (Leqvio®) received marketing approval from the European Union (EC), becoming the first and only siRNA cholesterol-lowering drug
.

At present, this product is undergoing three phase 3 clinical trials in China (one of which began enrollment in March 2021).

On July 1, 2021, inclisiran's first injection was completed in Boao, Hainan, and it is currently used by thousands of patients (Boao Pilot Zone and Guangdong-Hong Kong-Macao Greater Bay Area).

It is worth noting that the current indications of this product are for:

After taking statins, blood lipids are not up to standard;
Inability to tolerate statin lipid-lowering drugs;
Patients
with familial hypercholesterolemia.

After taking statins, blood lipids are not up to standard;

Inability to tolerate statin lipid-lowering drugs;

Patients
with familial hypercholesterolemia.

According to the data of WuRong Cloud, www.
pharnexcloud.
com show that on December 22, 2021, the US FDA finally approved the marketing of this product; It will be launched to the US market
in January 2022.
In the third quarter of 2022, Inclisiran's performance was $34 million; The whole year 2022 may be close to $100 million
.

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This article is only for providing scientific information to healthcare professionals and does not represent the position of the platform

Reference:

NMPA/CDE；

PharmaPharma Cloud Data www.
pharnexcloud.
com;

FDA/EMA/PMDA；

Public disclosure by relevant companies;

www.
novartis.
com；

； Novartis' first small interference nucleic acid therapy Leqvio® was approved by the FDA, and two injections a year continue to effectively lower lipids;

European Heart Network.
European Cardiovascular Disease Statistics 2017 edition，，November 2020；

Novartis enters into agreement to acquire The Medicines Company，；

Ray K, Wright R, Kallend D, et al.
Two Phase 3 Trials of Inclisiran in Patients with Elevated LDL Cholesterol [published online ahead of print March 18, 2020].
N.
Engl.
J.
Med.
, ；

Raal, F, Kallend D, Ray K, et al.
Inclisiran for Heterozygous Familial Hypercholesterolemia [published online ahead of print March 18, 2020].
N.
Engl.
J.
Med.
, ； And so on
.

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