Fluorine is the most electronegative element in the periodic table, and the fluorine atom has a small atomic radius, so fluorine-containing organic compounds have many wonderful properties. For example, the introduction of fluorine atoms or fluorine-containing groups into drug molecules can improve the permeability to cell membranes, metabolic stability and bioavailability; in addition, the introduction of fluorine atoms will improve the lipid solubility of the compound and promote its absorption in the body. The speed of delivery changes the physiological effect. In the field of medicinal chemistry, the introduction of fluorine atoms into organic molecules is an important direction for the development of new anticancer drugs, antitumor drugs, antiviral agents, anti-inflammatory drugs, and central nervous system drugs.
The elevated low-density lipoprotein cholesterol (LDL-C) is a causal risk factor for atherosclerotic cardiovascular disease (ASCVD), and heterozygous familial hypercholesterolemia (HeFH). Cholesteryl ester transfer protein (CETP) transports cholesterol from good high-density lipoprotein cholesterol (HDL-C) to low-density lipoprotein cholesterol (LDL-C). NewAmsterdam’s Obicetrapib is a novel, selective CETP inhibitor to address the limitations of current treatments.
Obicetrapib is under investigation in phase III clinical trials as a monotherapy product, and in phase II studies as a fixed dose combination with Ezetimibe.
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