Target(s): | Oxygenase | Integrin αIIbβ3 | Collagen receptor | Thrombin receptors | |||||
Drug | Aspirin | ML355 | Abciximab | Tirofiban | Eptifabtide | GPVI-Fc | Atopaxar | Vorapaxar | BMS-986120 |
Trade name | Bayer Asprin | (Investigational) | ReoPro | Aggrastat | Integrilin | Revacept | (Investigational) | Zontivity | (Investigational) |
Molecule type | Acetylsalicylic acid | Small molecule | Humanized mouse monoclonal antibody | Nonpeptide RGD mimetic | KGD-containing heptapeptide | Soluble dimeric glycoprotein VI-Fc fusion protein | Bicyclic amidine | Tricyclic 3-phenylpyridine | Small molecule |
Binding type | Irreversible | N.D. | Irreversible | Reversible | Reversible | N.D. | Reversible | Reversible | Reversible |
Formation | Oral | Oral | IV | IV | IV | IV | Oral | Oral | Oral |
Half-life | 15–20 min (Altman et al., 2004) | 2.5 h (murine) (Adili et al., 2017) | 10–30 min (De Luca, 2012) | 1.5–2 h (De Luca, 2012) | 2–2.5 h (De Luca, 2012) | 67–137 h depending on the doses (Ungerer et al., 2011) | 22–26 h (Tello-Montoliu et al., 2011) | 7–13 days (Tello-Montoliu et al., 2011) | 4 h (Wilson et al., 2017) |
Prodrug | No | N.D. | No | No | No | No | No | No | No |
Onset of action | 1 h (Eikelboom et al., 2012) | N.D. | Within 20 min (King et al., 2016) | Within 20 min (King et al., 2016) | Within 20 min (King et al., 2016) | 2 h (Ungerer et al., 2011) | 3.5 h (Tello-Montoliu et al., 2011) | 1–2 h (Tello-Montoliu et al., 2011) | 2 h (Wilson et al., 2017) |
Offset of action | 7–10 days | N.D. | >4 h (De Luca, 2012) | >4 h (De Luca, 2012) | 4–8 h (Topol, 1999; Vorchheimer et al., 1999) | 7 days (Ungerer et al., 2013) | 3–5 days depending on the doses | 4–8 weeks (Kosoglou et al., 2012) | 24 h (Wilson et al., 2017) |
Indication(s) | Nonfatal thrombotic events; patients with STEMI (Franchi et al., 2017) | Preclinical data show reduction in thrombotic cardiovascular events and prevention of ITT (Adili et al., 2017; Yeung et al., 2014) | Prevention of ischemic complications due to PCI and patients with UA/NSTEMI pre-PCI (Amsterdam et al., 2014a; Jneid et al., 2012) | Reduction of cardiovascular events in ACS patients with UA/NSTEMI (Amsterdam et al., 2014a; Jneid et al., 2012) | Reduction of acute cardiac ischemic events (death and/or MI) for PCI, coronary stents, patients with UA/STEMI (Amsterdam et al., 2014a; Jneid et al., 2012) | Under investigation for treatment of patients with ACS and stroke | Under investigation for treatment of patients with ACS and stroke | Reduction of thrombotic cardiovascular events in patients with previous MI or peripheral arterial disease | Under investigation for reduction of thrombotic events in high risk patients |
Target(s): | PDE | ADP Receptors | GPIb-IX-V | |||||
Drug | Dipyridamole | Cilostazol | Ticlopidine | Clopidogrel | Prasugrel | Ticagrelor | Cangrelor | Anfibatide |
Trade name | Persantine | Pletal | Ticlid | Plavix | Effient | Brilinta, Brilique, Possia | Kengreal | N.D. |
Molecule type | Pyrimido-pyrimidine derivative | Quinoline derivative | Thienopyridine | Thienopyridine | Thienopyridine | CPTP | ATP analog | C-type lectin-like protein derived from venom of Agkistrodon acutus |
Binding type | Reversible | Reversible | Irreversible | Irreversible | Irreversible | Reversible | Reversible | Reversible |
Formation | Oral | Oral | Oral | Oral | Oral | Oral | IV | IP (murine); IV (humans) (Lei et al., 2014; Li et al., 2015; Zheng et al., 2016) |
Half-life | 10 h (Gregov et al., 1987) | 10–11 h (Eikelboom et al., 2012) | 24–36 h (Eikelboom et al., 2012) | 20 min (Umemura and Iwaki, 2016) | 30 min to 7.5 h (Umemura et al., 2016) | 7–9 h (Teng and Butler, 2013) | 3–5 min (Sible and Nawarskas, 2017) | 5–7 h (murine) (Zheng et al., 2016) |
Prodrug | No | Yes (CYP3A5 and CYP2C19) (Yoo et al., 2009, 2010) | Yes | Yes | Yes | No | No | No |
Onset of action | 1–2 h (Gregov et al., 1987) | N.D. | 1–3 h (Eikelboom et al., 2012) | 2–8 h (Capodanno et al., 2013) | 30 min to 4 h (Capodanno et al., 2013) | 30 min to 4 h (Capodanno et al., 2013) | Seconds (Capodanno et al., 2013) | N.D. |
Offset of action | N.D. | 12–16 h (Yamamoto et al., 2008) | 7–10 days | 7–10 days (Capodanno et al., 2013) | 7–10 days (Capodanno et al., 2013) | 3–5 days (Capodanno et al., 2013) | 1 h (Capodanno et al., 2013) | N.D. |
Indication(s) | Adjunct therapy with oral anticoagulant in the prevention of postoperative thromboembolic complications | Claudication in patients with peripheral arterial disease (Faxon et al., 2004) | Reduce risk of thrombotic stroke and prevention of coronary artery stent thrombosis in patients intolerant to aspirin | Commonly used with aspirin for dual antiplatelet therapy to reduce MI and stroke in patients with NSTEMI or acute STEMI (Franchi et al., 2017) | Reduce rate of thrombotic cardiovascular events, including stent thrombosis, in ACS patients who are undergoing PCI, with UA/NSTEMI, STEMI (Franchi et al., 2017) | Reduce rate of rate of stent thrombosis, cardiovascular death, MI, and stroke in patients with ACS or a history of MI (Franchi et al., 2017) | Used as an adjunct to PCI for reducing the risk of periprocedural MI, repeat coronary revascularization, and stent thrombosis in patients without P2Y12 inhibitor (Sible and Nawarskas, 2017) | Preclinical data support treatment of ischemic events and TTP (Zheng et al., 2016); still under investigation in patients with NSTEMI and STEMI |
CPTP, cyclopentyl-triazolo-pyrimidine; NSTEMI, non-ST elevation myocardial infarction; STEMI, ST elevation myocardial infarction.