An Update on Novel Antiplatelets in Vascular Patients

Abstract

Background: Acetylsalicylic acid, clopidogrel and cilostazol are well-established agents inhibiting the normal function of platelets with known advantages and limitations. The development of novel antiplatelet agents aims to provide equal or superior outcomes for patients and simultaneously minimize side effects. Objective: The aim of this manuscript is to review the latest data on the use of novel antiplatelet agents in vascular patients. Method: Based on our 2016 review, a further search in the English medical literature has yielded a number of publications on cangrelor, prasugrel, ticagrelor, vorapaxar and a number of other – still experimental – agents (Ir- 6, UBO-QIC, W1, revacept and YM-254890). Results: Recently published data have not altered the use and indications of cangrelor, prasugrel and vorapaxar; all of them now approved by both FDA and EMA. The EUCLID trial has recently provided valuable data on the clinical use of ticagrelor, although results regarding vascular patients and administration of ticagrelor are still under scrutiny. Vorapaxar remains the only novel antiplatelet that is approved for PAD. Randomized control trials that focus on vascular patients are necessary to establish the safety and efficacy of these novel agents. Despite their positive initial results, most novel experimental antiplatelets are still in early development, thus in preclinical or early clinical phases of their trials. Research on three novel antiplatelets is currently discontinued (atopaxar, darexaban and elinogrel). Conclusion: Vorapaxar remains the only novel antiplatelet that is approved for PAD. Other novel antiplatelets demonstrate positive results, but further studies focused on vascular patients are necessary. Novel experimental antiplatelets are still in the early phases of the clinical and preclinical studies.

Cell type‐specific mechanisms coupling protease‐activated receptor‐1 to infectious colitis pathogenesis

“…The novel animals presented here are likely to be important tools in the study of PAR-1 signaling in other inflammatory pathologies, models of infection, and cancer pathogenesis. Given that a PAR-1 antagonist is now approved by United States Food and Drug Administration for clinical use in humans [53], understanding the role of this receptor in disease pathogenesis in cell type-specific mechanistic detail is of significant importance.…”

Involvement of P2 receptors in hematopoiesis and hematopoietic disorders, and as pharmacological targets

“…Cangrelor, an inhibitor of the P2Y12 receptor that does not require metabolic activation, was recently approved for use by the FDA [175]. This inhibitor has a similar structure to ATP, and ticagrelor binds directly and reversibly to the P2Y12 receptor [176,177].…”

“…Elinogrel is also an intravenous drug that acts on the P2Y12 receptor but is still under clinical testing [171,175]. It is also available in oral form and binds reversibly and directly to the P2Y12 receptor [171].…”