Hogwood, John; Mulloy, Barbara; Lever, Rebecca; Gray, Elaine; Page, Clive P; (2023) Pharmacology of Heparin and Related Drugs: An Update. Pharmacological Reviews , 75 (2) pp. 328-379. 10.1124/pharmrev.122.000684.

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Abstract

Heparin has been used extensively as an antithrombotic and anticoagulant for close to 100 years. This anticoagulant activity is attributed to the pentasaccharide sequence which potentiates the inhibitory action of antithrombin, a major inhibitor of the coagulation cascade. More recently it has been determined that heparin also has antithrombotic action through interference of the formation of neutrophil extracellular traps which have been determined to play a role in thrombosis. This demonstrated a well-known observation that heparin, given it is a highly negatively charged polysaccharide, interacts with a broad range of biomolecules demonstrating attenuating effect. Since our previous review, there has been an increased interest in these non-anticoagulant effects of heparin, with the beneficial role in patients infected with sars2-coronavirus a highly topical example. This article provides an update on our previous review with more recent developments and observations made for these novel uses of heparin and an overview of the development status of heparin-based drugs. Significance Statement This state of the art review covers recent developments in the use of heparin and heparin-like materials as anticoagulant, now including immuno-thrombosis observations, and as non-anticoagulant including a role in the treatment of sars-coronavirus and inflammatory conditions.

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