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Evolocumab AI simulator
(@Evolocumab_simulator)
Hub AI
Evolocumab AI simulator
(@Evolocumab_simulator)
Evolocumab
Evolocumab, sold under the brand name Repatha, is a monoclonal antibody that is an immunotherapy medication for the treatment of hyperlipidemia.
Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that targets LDL receptors for degradation; its inhibition thereby enhances the liver's ability to remove LDL-C, often colloquially referred to as "bad" cholesterol, from the blood.
In 2023, it was the 188th most commonly prescribed medication in the United States, with more than 2 million prescriptions.
Evolocumab is designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface. In the absence of PCSK9, there are more LDL receptors on the surface of liver cells to remove LDL-C from the blood.
Injection site reactions such as redness and pain are common and are reported in approximately 2.1–4.3% of cases.
Amgen submitted a biologics license application (BLA) for evolocumab to the FDA in August 2014. The FDA approved evolocumab injection on 27 August 2015, for some patients who are unable to get their LDL cholesterol under control with current treatment options. The European Commission approved it in July 2015. Evolocumab received approval from Health Canada on 10 September 2015. Amgen reported approval by Health Canada in a press release on 15 September 2015.
Results of the FOURIER trial were published in March 2017. Results from FOURIER-OLE, an open-label follow-up study of 24% of the patients in the treatment arm of FOURIER, were published by Amgen in 2022. In 2022 a reanalysis of the FOURIER trial based on regulatory data found that cardiac mortality with evolocumab was higher than had been reported in the trial publication, with the authors calling for a full independent trial restoration of FOURIER. Overall cardiovascular mortality, which had been overreported, was found to be higher on evolocumab than on placebo, but the difference was not statistically significant.
Regeneron Pharmaceuticals and Amgen each filed for patent protection on their monoclonal antibodies against PCSK9 and the companies ended up in patent litigation in the U.S. In March 2016, a district court found that Regeneron's drug alirocumab infringed Amgen's patents; Amgen then requested an injunction barring Regeneron and Sanofi from marketing alirocumab, which was granted in January 2017. The judge gave Regeneron and Sanofi 30 days to appeal before the injunction went into effect. After several years of litigation, the patent dispute between Regeneron and Amgen was docketed by the SCOTUS for March-April 2023 Numerous legal commentators were surprised by the SCOTUS decision, considering the existing trend not to review patent cases from the United States Court of Appeals for the Federal Circuit, since this court was created in 1982 to assure uniformity in patent law among all federal courts. The question before the US Supreme Court was "Whether enablement is governed by the statutory requirement, that the specification teach those skilled in the art to "make and use" the claimed invention, or whether it must instead enable those skilled in the art "to reach the full scope of claimed embodiments" without undue experimentation—i.e., to cumulatively identify and make all or nearly all embodiments of the invention without substantial "time and effort". Other commentators believe that the SCOTUS took the case because of the significance of the legal question, which was deemed comparable to the impact of KSR v. Teleflex.
Evolocumab
Evolocumab, sold under the brand name Repatha, is a monoclonal antibody that is an immunotherapy medication for the treatment of hyperlipidemia.
Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that targets LDL receptors for degradation; its inhibition thereby enhances the liver's ability to remove LDL-C, often colloquially referred to as "bad" cholesterol, from the blood.
In 2023, it was the 188th most commonly prescribed medication in the United States, with more than 2 million prescriptions.
Evolocumab is designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface. In the absence of PCSK9, there are more LDL receptors on the surface of liver cells to remove LDL-C from the blood.
Injection site reactions such as redness and pain are common and are reported in approximately 2.1–4.3% of cases.
Amgen submitted a biologics license application (BLA) for evolocumab to the FDA in August 2014. The FDA approved evolocumab injection on 27 August 2015, for some patients who are unable to get their LDL cholesterol under control with current treatment options. The European Commission approved it in July 2015. Evolocumab received approval from Health Canada on 10 September 2015. Amgen reported approval by Health Canada in a press release on 15 September 2015.
Results of the FOURIER trial were published in March 2017. Results from FOURIER-OLE, an open-label follow-up study of 24% of the patients in the treatment arm of FOURIER, were published by Amgen in 2022. In 2022 a reanalysis of the FOURIER trial based on regulatory data found that cardiac mortality with evolocumab was higher than had been reported in the trial publication, with the authors calling for a full independent trial restoration of FOURIER. Overall cardiovascular mortality, which had been overreported, was found to be higher on evolocumab than on placebo, but the difference was not statistically significant.
Regeneron Pharmaceuticals and Amgen each filed for patent protection on their monoclonal antibodies against PCSK9 and the companies ended up in patent litigation in the U.S. In March 2016, a district court found that Regeneron's drug alirocumab infringed Amgen's patents; Amgen then requested an injunction barring Regeneron and Sanofi from marketing alirocumab, which was granted in January 2017. The judge gave Regeneron and Sanofi 30 days to appeal before the injunction went into effect. After several years of litigation, the patent dispute between Regeneron and Amgen was docketed by the SCOTUS for March-April 2023 Numerous legal commentators were surprised by the SCOTUS decision, considering the existing trend not to review patent cases from the United States Court of Appeals for the Federal Circuit, since this court was created in 1982 to assure uniformity in patent law among all federal courts. The question before the US Supreme Court was "Whether enablement is governed by the statutory requirement, that the specification teach those skilled in the art to "make and use" the claimed invention, or whether it must instead enable those skilled in the art "to reach the full scope of claimed embodiments" without undue experimentation—i.e., to cumulatively identify and make all or nearly all embodiments of the invention without substantial "time and effort". Other commentators believe that the SCOTUS took the case because of the significance of the legal question, which was deemed comparable to the impact of KSR v. Teleflex.