Sanofi/Regeneron and Amjin's PCSK9 Antibody Patent Battle Ends

2Month 25Amjin announced the verdict of a Delaware District jury, which ruled that the claims claimed in Amjin's patent were valid and rejected Sanofi/Patent claims for regenerative elements. Meanwhile, Sanofi/Regenera said in a statement that they disagreed with the ruling or could continue to appeal.

PCSK9Antibody

French pharmaceutical giant SanofieRegeneration with partners (Regeneron)The jointly developed Praluent(Alirocumab) and Amgen's Repatha(Evolocumab) are both monoclonal antibody drugs, targeting a protein called proprotein convertase subtilisin 9 (PCSK9), which can reduce the liver from the blood The ability to clear low-density lipoprotein cholesterol (LDL-C) is LDL-C recognized as a major risk factor for cardiovascular disease (CVD). PCSK9 inhibitors offer an entirely new treatment modality to combat LDL-C and are seen as the biggest advance in lipid-lowering since statins such as Lipitor and Zocor. Both were approved by the FDA in July and August 2015 for the control of LDL levels in high-risk groups (such as familial hypercholesterolemia, statin intolerance, etc.).

PCSK9considered as a lipid-lowering drug of great potential, although Repatha、PraluentSales have been slow since the launch, but this has not affected Amjin and Sanofi's fierce competition for this.

The Patent War

Tracing time back to 2014Year 10On March 17, Amjin sued Sanofi/Regenera Praluent for infringing on three of its Repatha patents (US8563698, US8829165 and US8859741).

2016Year 2Month 22On the same day, Sanofi/Regeneration admitted to infringing some of the claims claimed in Amjin's patents and turned the finger at whether the patent itself should be recognized: "The patent goes beyond Amjin's findings and makes it improperly cover a new class of therapies".

2016Year 3Month 8The two sides focused on the validity of some of the claims claimed in Amjin's patents.

2016Year 3Month 16A jury ruled that the claims claimed in the Amjin patent were valid.

2016Year 3Month 23-24The court heard evidence from the plaintiff's application for a permanent injunction against the Praluent.

2017Year 1Month 5On the same day, the court announced a permanent injunction against Praluent, unable to produce and sell Praluent in the U.S. market, and decided to postpone the execution for 30 days; Sanofi filed an emergency motion with the local court to postpone the execution of the permanent ban until the end of the appeal.

2017Year 1Month 9On the 2nd, the local court rejected the motion, but at the same time changed the 30-day delay to 45 days. The judgment stated that 45 days would give Sanofi enough time to appeal to the Federal Circuit.

This patent protracted war alarmed the entire pharmaceutical industry, and the watching melon eaters sweated for the game between the two sides, and finally reached 1Month 6On the 15th, Delaware District Judge Sue Robinson ruled that Sanofi/Regeneron had stopped selling Praluent for 12 years because the drug infringed Amgen's patents on similar drug Repatha.

Amjin's patent layout

The three patent US8563698 involved in the dispute.、US8829165And the US8859741 came from Amgen's global application through PCT on February 26, 2009 in WO2009026558. At present, the parent patent has nine authorized patents in the United States in addition to the three patents. At the same time, the parent nuclear patent is currently under application in China, and one was authorized on June 25, 2014. This series of patents protect the sequence, epitope and indication of PCSK9 antibody respectively.

Case revelation

Amjin's patent extends to the protection of epitopes, which greatly extends the scope of patent protection and creates patent obstacles for latecomers. If epitope protection becomes a trend, the difficulty of patent challenge can be imagined, and it can be expected that it will be difficult to bio-too in the market in the future.Antibodies, if any, take a lot of effort with the help of structural biology to avoid the protected epitope.

This change may change the pattern of research and development of antibody drugs and even drugs, greatly increasing the difficulty of research and development of antibody drugs with the same target, but it will also benefit the pattern of drug development based on other mechanisms, such as antisense RNA.及siRNASuch as avoiding the epitope level of drug development.