Throughout the body, the vasculature and the nervous system are fellow travelers. Renaissance physician and anatomist Andreas Vesalius described their proximity on the macroanatomical level in the 16th century, and modern microscopic techniques have shown that it extends into the micrometer range – where there is a blood vessel, there is often a nerve nearby, and vice versa.
Human lipoprotein(a) (Lp(a)) is a lipoprotein complex composed of a low-density lipoprotein (LDL) particle and a large highly polymorphic glycoprotein named apolipoprotein (a) (apo(a)). There is evidence that Lp(a) is linked to cardiovascular disorder risk.
Under pathologic conditions such as vascular injury or atherosclerosis, the hyperactivation of platelets may lead to occlusive thrombus formation, myocardial infarction or stroke. Although there are several targets for clot prevention validated clinically, these strategies may present bleeding risk as a limitation. Researchers from the University of Michigan have reported on CS-014, a histone deacetylase (HDAC) inhibitor aimed to reduce clot formation without risk of bleeding.
Both oxidative stress and inflammation are the main hallmarks in the development of heart failure. Researchers from the Hefei University of Technology have reported on the discovery and optimization of a series of pterostilbene derivatives intended to be used in heart failure.
Eli Lilly & Co. has described pyrrolidine compounds targeting apolipoprotein(a) (Apo[a]) and acting as lipoprotein(a)-lowering agents reported to be useful for the treatment of cardiovascular disorders.
Obesity is known to be associated with metabolic and cardiovascular disorders such as insulin resistance, type 2 diabetes, hypertension, or heart failure, all presenting a chronic low-grade inflammatory component. The activation of the NLRP3 inflammasome pathway appears to be linked to the development of cardio-metabolic diseases.
Protease form factor Xia (FXIa) is a therapeutic target for thrombosis prevention due to its well-known contribution to VTE and ischemic stroke in humans. Researchers from Janssen Pharmaceutica NV presented an antithrombotic target FXIa inhibitor obtained through a non-classical interactions strategy to improve the pharmacokinetic and pharmacological activity for the treatment of thrombosis. In the series, the potency was increased by using water-mediated hydrogen bonds to reduce polar hydrogen bond donors and using methyl to displace high-energy waters.
Lexeo Therapeutics Inc. has announced that its IND for LX-2020 has been cleared by the FDA. LX-2020 is an AAVrh10-based gene therapy candidate designed to intravenously deliver a functional PKP2 gene to cardiac muscle for the treatment of arrhythmogenic cardiomyopathy (ACM) caused by variants in PKP2 (PKP2-ACM).
Hangzhou Adamerck Pharmlabs Inc. has disclosed uracil derivatives reported to be useful for the treatment of cardiovascular and cerebrovascular disorders.
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