Cholesterol: new oral drug reduces 70%


More solutions are on the way for those who do not respond to hypercholesterolemia therapy, i.e. the prescription of a statin that reduces blood cholesterol levels. With the statin, many patients fail to achieve the desired results or are intolerant, so PCSK9 protein inhibitors have been invented . These are monoclonal antibodies that help the body to decrease plasma levels of LDL cholesterol by up to 70%. If statins are oral drugs, these new drugs are given by injection only. Since 2015 there are two Alirocumab and Evolocumab. Researchers recently devised the first oral small-molecule drug that reduces PCSK9 levels and lowers LDL by 70%.


Blood cholesterol levels are regulated by LDL receptors found on liver cells by removing cholesterol from the blood. This is regulated by the PCSK9 protein, which inhibits the functioning of the LDLReceptors, which promote the absorption of cholesterol by the liver. This also brings advantages in reducing cardiovascular pathologies . PCSK9 inhibitors reduce LDL cholesterol levels by 50-70%. Today there are many therapeutic approaches attested or under development for the inhibition of the PCSK9 protein. PCSK9 short interfering RNAs (siRNAs) that work by reducing PCSK9 synthesis (such as Inclisiran), anti-PCSK9 monoclonal antibodies, and the anti-PCSK9 vaccine.

The researchers used nitric oxide , a molecule that prevents heart attacks by dilating blood vessels. With nitric oxide they developed a new PCSK9 inhibitor that lowered cholesterol levels. Finally, they created an oral small-molecule drug that works by increasing the nitric oxide inactivation of PCSK9. For now, the test has been done on mice by decreasing LDL cholesterol by 70%. It seems that these drugs are also effective against cancer. PCSK9 inhibitors appear to improve the results of immunotherapy.

  • How the new oral drug that reduces cholesterol by 70% works


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