Table 3.

Comparison of the Pharmacologic characteristics of Low-molecular-weight heparin with those of available direct oral anticoagulants.

Characteristics	LMWH	Dabigatran	Rivaroxaban	Apixaban	Edoxaban
Prodrug	No	Yes	No	No	No
Bioavailability (%)	90	3–7 (pH dependent-Tartaric acid added into the dabigatran capsule)	≥80 when taken with food (for 15 and 20 mg dosing)	50 (Food independent)	62 (Food independent)
Tmax (h)	3–4	1–3	2–4	3–4	1–2
Half-life (h)	4–6	12–17	5–13 (age dependent)	9–14	10–14
Excretion	Renal excretion	Urine (80%)	Urine (66% (~36% as unchanged drug; 30% as inactive metabolites)); feces (28% (7% as unchanged drug; 21% as inactive metabolites))	Urine (~27% as parent drug); feces (biliary and direct intestinal excretion)	Urine (primarily unchanged); renal clearance: ~50% of total clearance
Metabolism	Partially metabolized by desulphatation and depolymerization	Hepatic; dabigatran etexilate rapidly and completely hydrolyzed to dabigatran (active form) by plasma and hepatic esterases; dabigatran undergoes hepatic glucuronidation to active acylglucuronide isomers	Hepatic via CYP3A4/5 and CYP2J2	Hepatic predominantly via CYP3A4/5 and to a lesser extent via CYP1A2, 2C8, 2C9, 2C19, and 2J2 to inactive metabolites; -demethylation and hydroxylation are the major sites of transformation; substrate of P-gp and BCRP	Minimal via hydrolysis, conjugation and oxidation by CYP3A4; predominant metabolite (M-4) is active (<10% of parent compound)
Transporter involved	-	P-gp (dabigatran etexilate only)	P-gp, BCRP	P-gp, BCRP	P-gp
Specific antidot	Protamine (partial)	Idarucizumab Aripazin	Andexanet alfa * Aripazin	Andexanet alfa * Aripazin	Andexanet alfa * Aripazin

LMWH, low molecular weight heparin; CYP, cytochrome P450; P-gp, P-glycoprotein (ABCB1); BCRP, breast cancer resistance protein (ABCG2); * Andexanet alfa (PRT064445 or PRT4445) is a modified recombinant FXa protein targeting oral FXa inhibitors.