Members of the family of eucaryotic, subtilisin-like endoproteases that reside in the constitutive secretory pathway, which include furin, Paired Basic Amino Acid Cleaving Enzyme 4 (PACE4), Prohormone Convertase
5 (PC5), and Prohormone Convertase
7 (PC7), are prime candidates for the endoproteolytic maturation of pro-BACE.
Repatha (evolocumab) is a human monoclonal antibody that binds to proprotein convertase
subtilisin/kexin type 9 (PCSK9) and inhibits circulating PCSK9 from binding to the low-density lipoprotein receptor, preventing PCSK9-mediated LDLR degradation and permitting LDLR to recycle back to the liver cell surface.
Praluent is a human monoclonal antibody targeting PCSK9 (proprotein convertase
subtilisin/kexin type 9).
The company said Praluent is a PCSK9 (proprotein convertase
subtilisin/kexin type 9) inhibitor indicated as adjunct to diet and maximally tolerated statin therapy for the treatment of adults with HeFH or clinical atherosclerotic CVD, who require additional lowering of LDL cholesterol.
They are human monoclonal antibodies that bind to proprotein convertase
subtilisin kexin type 9 (PCSK9), a serine protease that is involved in the regulation of LDL receptor (LDR-R).
It is clear that these proprotein convertase
subtilisin/kexin type 9 (PCSK9) inhibitors provide a powerful therapy for reducing LDL cholesterol, with a reported decrease of about 60% after only 12 or 52 weeks of treatment.
In the past 2 and a half decades, 9 members of the proprotein convertase
subtilisin/kexin (PCSK)  have been identified in mammals, with broad substrate specificities.
Both SPIRE-HR and SPIRE-FH continued for 52 weeks to assess the longer-term efficacy and safety of bococizumab, an investigational Proprotein Convertase
Subtilisin Kexin type 9 inhibitor (PCSK9i), in patients at high and very high risk for cardiovascular events.
According to the companies, Praluent (alirocumab) is the only EC-approved PCSK9 (proprotein convertase
subtilisin/kexin type 9) inhibitor that is available in two starting doses as a single 1-milliter (mL) injection (75 mg and 150 mg) once every two weeks, offering two levels of efficacy.
Lipids: All eyes are on ongoing pivotal phase III randomized clinical outcome trials of three monoclonal antibodies that inhibit proprotein convertase
subtilisin kexin type 9 (PCSK9): the 22,500-patient FOURIER trial of evolocumab, which includes 9,000 patients older than 65 years; the 18,000-patient ODYSSEY Outcomes trial of alirocumab; and the SPIRE-1 and SPIRE-2 trials of bococizumab totaling 18,300 patients.