Pyrimidine, also known as 1,3-diazobenzene, is a heterocyclic compound with the chemical formula C4H4N2. Pyrimidine is formed by substituting 2 nitrogen atoms for 2 carbons in the meta-position of benzene. It is a diazine and retains its aromaticity. Derivatives of pyrimidine widely exist in organic macromolecular nucleic acids, and many drugs also contain pyrimidine rings. In nucleic acids, three nucleobases are pyrimidine derivatives: cytosine, thymine and uracil. There are a variety of pyrimidine-containing drugs on the market, most of which are kinase inhibitors.
New Phase 3 data with aprocitentan for patients with resistant hypertension has been presented at the American Society of Nephrology Kidney Week 2023.
Aprocitentan is an investigational, novel, oral, dual endothelin receptor antagonist (ERA), which potently inhibits the binding of ET-1 to ETA and ETB receptors. Aprocitentan has a low potential for drug-drug interaction and a mechanism of action that is ideally suited for the pathophysiology of resistant hypertension.
A new drug application (NDA) for aprocitentan was accepted for review by the US FDA.
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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