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Introduction to Human Cytochrome P450 Superfamily
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Because of their role in thromboxane synthesis, TBXAS1 inhibitors and thromboxane A2 receptor antagonists have been a great interest for many years for their potential use in preventing platelet aggregation. Drugs with dual action, such as dual TBXAS1 inhibitors/thromboxane A2 receptor antagonist and dual COX-1/thromboxane A2 receptor antagonists, are currently in clinical development with the hope of providing a better, more complete inhibition of the thromboxane A2 pathway. For example, ifetroban is a potent and selective thromboxane A2 receptor antagonist; dipyridamole antagonizes this receptor too; picotamide has activity both as a TBXAS1 inhibitor and as a thromboxane A2 receptor antagonist. These inhibitors often contain a basic nitrogen atom that binds to the CYP5A1 heme. Terutroban is an orally active drug in clinical development for use in secondary prevention of thrombotic events in cardiovascular disease. Despite great expectations on this drug supported by a large body of preclinical and clinical evidence and pathophysiological rationale, the PERFORM trial fails to demonstrate the superiority of terutroban over aspirin in secondary prevention of cerebrovascular and cardiovascular events among ~20,000 patients with stroke (Bousser et al. 2011).
Drug treatment of varicose veins, venous edema, and ulcers
Published in Peter Gloviczki, Michael C. Dalsing, Bo Eklöf, Fedor Lurie, Thomas W. Wakefield, Monika L. Gloviczki, Handbook of Venous and Lymphatic Disorders, 2017
Effects of the oral thromboxane A2 receptor antagonist ifetroban (250 mg daily) on the healing of chronic lower extremity venous stasis ulcers has been studied in a well-designed prospective, randomized, double-blind, placebo-controlled multicenter study.43 This drug has a profound inhibitory effect on platelet activation. The results show no efficacy for influencing venous ulcer healing.
Drug development and novel therapeutics to ensure a personalized approach in the treatment of systemic sclerosis
Published in Expert Review of Clinical Immunology, 2023
N Farina, C Campochiaro, A Lescoat, G Benanti, G De Luca, D Khanna, L Dagna, M Matucci-Cerinic
Ifetroban is an oral inhibitor of TXAR with marked antithrombotic and vasodilative properties [124]. Ifetroban has shown an anti-fibrotic action in experimental models of lung fibrosis [125]. These encouraging results have prompted the design of a phase II trial evaluating the efficacy of ifetroban on SSc-related PAH and skin fibrosis, which is currently recruiting (NCT02682511).