Sharif‑Rad, Javad Sharopov, Farukh Ezzat, Shahira MZam, Wissam Ademiluyi, Adedayo Oluwaseun Oyeniran, Olubukola Helen Adetunji, Charles Oluwaseun Roli, Osahon Itohan Živković, Jelena Martorell, Miquel Docea, Anca Oana El Omari, Nasreddine Bouyahya, Abdelhakim Lorenzo, José MCalina, Daniela 2023-01-252023-01-252023-01https://doi.org/10.1007/s40292-023-00562-9https://bit.ly/3kJD1w4The glycoprotein (GP) IIb/IIIa receptor is found integrin present in platelet aggregations. GP IIb/IIIa antagonists interfere with platelet cross-linking and platelet-derived thrombus formation through the competition with fbrinogen and von Wille- brand factor. Currently, three parenteral GP IIb/IIIa competitors (tirofban, eptifbatide, and abciximab) are approved for clinical use in patients afected by percutaneous coronary interventions (PCI) in the location of acute coronary syndrome (ACS). GP IIb/IIIa antagonists have their mechanism of action in platelet aggregation prevention, distal thromboembolism, and thrombus formation, whereas the initial platelet binding to damage vascular areas is preserved. This work is aimed to provide a comprehensive review of the signifcance of GP IIb/IIIa inhibitors as a sort of antiplatelet agent. Their mechanism of action is based on factors that afect their efcacy. On the other hand, drugs that inhibit GP IIb/IIIa already approved by the FDA were reviewed in detail. Results from major clinical trials and regulatory practices and guidelines to deal with GP IIb/IIIa inhibitors were deeply investigated. The cardiovascular pathology and neuro-interventional surgical application of GP IIb/IIIa inhibitors as a class of antiplatelet agents were developed in detail. The therapeutic risk/beneft balance of cur- rently available GP IIb/IIa receptor antagonists is not yet well elucidated in patients with ACS who are not clinically evalu- ated regularly for early cardiovascular revascularization. On the other hand, in patients who have benefted from PCI, the antiplatelet therapy intensifcation by the addition of a GP IIb/IIIa receptor antagonist (intravenously) may be an appropriate therapeutic strategy in reducing the occurrence of risks of thrombotic complications related to the intervention. Development of GP IIb/IIIa inhibitors with oral administration has the potential to include short-term antiplatelet benefts compared with intravenous GP IIb/IIIa inhibitors for long-term secondary preventive therapy in cardiovascular disease. But studies showed that long-term oral administration of GP IIb/IIIa receptor inhibitors has been inefective in preventing ischemic events. Paradoxically, they have been linked to a high risk of side efects by producing prothrombotic and pro-infammatory events.en-USGlycoproteins IIb/IIIa ·Platelets ·Paradoxical thrombosis ·GP IIb/IIa antagonists ·Clinical trialsArticlehttps://doi.org/10.1007/s40292-023-00562-9