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Papel dos inibidores da PCSK9 no tratamento da dislipidemia
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Abstract(s)
A dislipidemia, definida como a elevação dos valores de lípidos no sangue, é um dos principais fatores de risco para o desenvolvimento de doenças cardiovasculares, nomeadamente a aterosclerose. Considera-se das maiores causas de morte a nível global, tendo um impacto bastante negativo na vida humana.
O seu controlo constitui um aspeto fundamental para a prevenção da doença, existindo fatores modificáveis que podem ser controlados, como os hábitos alimentares, a prática regular de exercício físico, o tabagismo e o alcoolismo. É necessário que se adotem medidas preventivas e estratégias para o combate destas patologias, tentando desta forma atuar na redução do colesterol das lipoproteínas de baixa densidade (c-LDL).
As medidas farmacológicas existentes concentram-se maioritariamente no uso de estatinas. Porém, há indivíduos que desenvolvem efeitos adversos, o que pode resultar de uma intolerância às mesmas e um insucesso no tratamento, refletindo-se efetivamente numa necessidade de procura por uma nova terapêutica hipolipemiante.
Com base nessa procura, a evolução no âmbito da ciência permitiu incitar ao desenvolvimento dos inibidores da pró-proteína convertase subtilina quexina tipo 9 (PCSK9), que se revelaram bastante promissores no combate às dislipidemias.
Os inibidores PCSK9 são anticorpos monoclonais e a sua atuação passa por não permitirem a degradação do LDLR pela PSCK9, regulando dessa forma os níveis plasmáticos do c-LDL.
Os principais inibidores PCSK9 alvo de estudo são Evolocumab e Alirocumab. Demonstraram uma eficácia de aproximadamente 60% na redução do c-LDL como monoterapia e, quando adicionados às com estatinas, essa redução atingiu os 75%. Desta forma, consideram-se atualmente uma terapêutica muito efetiva, de segunda linha, reservada para os doentes que não toleram ou não respondem de forma cabal a outros fármacos, nomeadamente nos casos de dislipidemia de causa genética, como a hipercolesterolemia familiar.
Dyslipidemia, defined as the elevation of blood lipids, is one of the main risk factors for the development of cardiovascular diseases, namely atherosclerosis. It is considered one of the biggest causes of death globally, having a very negative impact on human life. Its control is a fundamental aspect for the prevention of the disease, with modifiable factors that can be controlled, such as eating habits, regular physical exercise, smoking and alcoholism. It is necessary to adopt preventive measures and strategies to combat these pathologies, trying in this way to act in the reduction of low-density lipoprotein cholesterol (c-LDL). Existing pharmacological measures are mostly focused on the use of statins. However, there are individuals who develop adverse effects, which may result from intolerance to them and treatment failure, effectively reflecting a need to search for a new lipid-lowering therapy. Based on this search, the evolution in the field of science allowed for the development of inhibitors of the proprotein convertase subtilin kexin type 9 (PCSK9), which proved to be very promising in combating dyslipidemia. PCSK9 inhibitors are monoclonal antibodies and their action involves not allowing the degradation of LDLR by PSCK9, thus regulating the plasma levels of c-LDL. The main PCSK9 inhibitors to be studied are Evolocumab and Alirocumab. They demonstrated an efficacy of approximately 60% in reducing c-LDL as monotherapy and when added to those with statins, this reduction reached 75%. Thus, they are currently considered a very effective second-line therapy, reserved for patients who do not tolerate or do not fully respond to other drugs, particularly in cases of genetically caused dyslipidemia, such as familial hypercholesterolemia.
Dyslipidemia, defined as the elevation of blood lipids, is one of the main risk factors for the development of cardiovascular diseases, namely atherosclerosis. It is considered one of the biggest causes of death globally, having a very negative impact on human life. Its control is a fundamental aspect for the prevention of the disease, with modifiable factors that can be controlled, such as eating habits, regular physical exercise, smoking and alcoholism. It is necessary to adopt preventive measures and strategies to combat these pathologies, trying in this way to act in the reduction of low-density lipoprotein cholesterol (c-LDL). Existing pharmacological measures are mostly focused on the use of statins. However, there are individuals who develop adverse effects, which may result from intolerance to them and treatment failure, effectively reflecting a need to search for a new lipid-lowering therapy. Based on this search, the evolution in the field of science allowed for the development of inhibitors of the proprotein convertase subtilin kexin type 9 (PCSK9), which proved to be very promising in combating dyslipidemia. PCSK9 inhibitors are monoclonal antibodies and their action involves not allowing the degradation of LDLR by PSCK9, thus regulating the plasma levels of c-LDL. The main PCSK9 inhibitors to be studied are Evolocumab and Alirocumab. They demonstrated an efficacy of approximately 60% in reducing c-LDL as monotherapy and when added to those with statins, this reduction reached 75%. Thus, they are currently considered a very effective second-line therapy, reserved for patients who do not tolerate or do not fully respond to other drugs, particularly in cases of genetically caused dyslipidemia, such as familial hypercholesterolemia.
Description
Keywords
Dislipidemias Colesterol Inibidores PCSK9 Lipoproteínas de alta e baixa densidade Tratamento das dislipidemias Hipercolesterolemia Dyslipidemia Cholesterol PCSK9 inhibitors High and low density lipoprotein Treatment of dyslipidemias Hypercholesteroleamia