Table 2.

Pharmacology of oral P2Y12 inhibitors and expected clopidogrel bioactivation frequencies within the U.S. population.

	Clopidogrel (Plavix, Bristol-Myers Squibb/Sanofi)	Prasugrel (Effient, Eli Lilly)	Ticagrelor (Brilinta, AstraZeneca)	Cangrelor (Kengreal, Chiesi)
Drug class	Thienopyridine	Thienopyridine	Cyclopentyl-triazolopyrimidine	Adenosine triphosphate analogue
Receptor blockade	Irreversible	Irreversible	Reversible	Reversible
Prodrug	Yes	Yes	No but active metabolite	No
Half-life parent drug	≈6 h	<5 min	6–12 h	3–6 min
Half-life active metabolite	30 mins	Distribution 30-60 mins Elimination 2–15 h	8–12 h	1-2 mins
Binding site1	ADP	ADP	Allosteric, non-ADP	site uncertain
Route, dosage, frequency	oral, 75- and 300-mg tablets, once daily	oral, 5- and 10-mg tablets, once daily	oral, 60- and 90-mg tablets, twice daily	10 mL vial containing 50 mg
Loading dose	300 mg or 600 mg	60 mg	180 mg	30 mcg/kg IV bolus
Maintenance dose	75 mg daily	10 mg daily(5 mg if <60 kg)	90 mg twice daily	mcg/kg/min IV for ≥2 h
Onset2-offset of action	2–8 h; 5–10 d	0.5–4 h; 7–10 d	0.5–4 h; 3–5 d	≈2 min; <1 h
CYP drug interaction3	CYP2C19	no	CYP3A	no
Use in renal/hepatic impairment	no dose adjustment	caution in moderate-to-severe renal or severe hepatic impairment	caution in moderate and avoid in severe hepatic impairment	no dose adjustment
Nonbleeding side effects	none	none	dyspnea; elevated uric acid; elevated creatinine	dyspnea
Average wholesale price 30-day supply at maintenance dose	$232 (brand) $184 (lowest generic)	$551 (brand) $495 (lowest generic)	$236 (brand) no generic	$899 (brand) for 50 mg solutionno generic

¹Bind to ADP P2Y12 receptor preventing ADP from binding and activating GPIIb/IIIa complex.

²After loading dose-bolus.

³Indicates clinically significant drug interactions.

ADP = adenosine diphosphate; CYP = cytochrome P450; IV = intravenous.