The Ultimate Showdown in Lipid-Lowering Drugs: Domestic Chinese Pharma Companies Accelerate Entry into the PCSK9 Arena

Globally, the number of patients with hyperlipidemia is enormous, and the situation is similar in China.

According to data from Zhiyan Consulting, the number of people with dyslipidemia in China reached 200 million in 2022, and the population is still expanding. Moreover, hyperlipidemia is a chronic condition requiring long-term medication.

These two factors determine that the future potential in China's lipid-lowering track is enormous. Therefore, lipid-lowering drugs have always been a must-contend area for major pharmaceutical companies.

In such a situation, the new mechanism lipid-lowering drug PCSK9 target is regarded as a rising star by major pharmaceutical companies. However, it is precisely due to the high expectations of pharmaceutical companies that the competition for the PCSK9 target has gradually intensified.

On December 25, Ribo Life Science announced a collaboration with Qilu Pharmaceutical to grant the China rights of the PCSK9 small nucleic acid drug RBD7022 to Qilu Pharmaceutical.

This also indicates that domestic pharmaceutical companies, including Qilu Pharmaceutical, are fiercely competing for a leading position in the PCSK9 small nucleic acid drug field.

/ 01 / More imaginative drugs

In the treatment of hyperlipidemia, the PCSK9 target has always been highly anticipated.

As early as 2003, this target was discovered. Studies have shown that PCSK9 can bind to LDL-R, leading to the latter's accelerated degradation. The lack of LDL receptors means that the LDL-C they carry cannot be cleared by the liver, naturally increasing the level of "bad cholesterol" in the body. With a clear mechanism, the approach for developing drugs targeting PCSK9 becomes very straightforward.

In the race to target PCSK9, monoclonal antibody drugs were the first to appear. In July and August 2015, the FDA approved two monoclonal antibody products: Repatha, jointly developed by Sanofi/Regeneron, and Praluent, developed by Amgen.

However, due to previous patent disputes, Amgen's Praluent sales have not been particularly high, reaching only $527 million in the seven years since its launch, whereas Repatha's sales have already reached $1.296 billion.

Although Repatha has become a blockbuster drug, its performance is actually somewhat below what Wall Street analysts predicted in the past.

The core reason behind this is that hyperlipidemia is a chronic disease medication, which requires patients to take it over the long term. However, PCSK9 monoclonal antibodies may need to be injected every 2-3 weeks to maintain the inhibition of plasma-free PCSK9 activity, so patient compliance is not high.

For this issue, small nucleic acid drugs might be the solution.

Currently, a breakthrough in compliance has been achieved with Novartis' PCSK9 siRNA therapy, Leqvio.

Leqvio achieves long-lasting therapeutic effects by directly inhibiting the liver's production of PCSK9 protein through gene silencing. Specifically, after two injections within the first three months, patients only need to receive a single injection of Leqvio every six months to maintain its lipid-lowering effects.

In December 2021, this drug was approved for marketing by the FDA. As its first full year on the market in 2022, Leqvio's sales reached $112 million.

/ 02 / Chinese pharmaceutical companies accelerate layout

The potential shown by the PCSK9 target is attracting domestic players to accelerate their布局.

Currently, Innovent Biologics' PCSK9 monoclonal antibody has been approved for marketing in China. Other domestic pharmaceutical companies such as Hengrui Medicine, Akeso Biopharma, and Junshi Biosciences are also preparing to apply for market entry.

However, beyond monoclonal antibodies, some new players are focusing on PCSK9 small nucleic acid drugs with better compliance.

On October 7, SinoBiologics' self-developed PCSK9 siRNA drug SGB-3403 was approved for clinical trials; on November 30, CSPC's self-developed PCSK9 siRNA drug SYH2053 was just approved for clinical trials for the treatment of hypercholesterolemia.

The latest pharmaceutical company to join the PCSK9 competition is Qilu Pharmaceutical. On December 25, Ribo Life Science announced that it had reached a collaboration with Qilu Pharmaceutical, granting the domestic rights of the PCSK9 small nucleic acid drug RBD7022 to Qilu Pharmaceutical. In return, Ribo Life Science will receive an upfront payment and milestone payments totaling over 700 million yuan.

It appears that the competition in China's lipid-lowering drug market around PCSK9 has gradually shifted from monoclonal antibodies to the small nucleic acid field.

Of course, domestic pharmaceutical companies in this field are still in the early stages of research and development, and will continue to face significant uncertainties.

Who will be the first to win the game in the PCSK9 small nucleic acid field? We wait and see.

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