TABLE 3

Key pharmacokinetic parameters of ARBs

Data were obtained from the regulatory authority approved U.S. prescribing information except for azilsartan where the corresponding Japanese document was used. For valsartan information from the prescribing information for both the capsule and tablet formulation were used.

tmaxOral BioavailabilityVdPlasma Protein Bindingt1/2Total ClearanceRenal Clearance
h%liters%h
Azilsartan1.8–2.47521>9913130–145 ml/min2.2–2.4 ml/min
Azilsartan medoxomil1.5–3601699.511n.r.2.3 ml/min
Candesartan cilexetil3–4150.13 l/kg>9990.37 ml/min/kg0.19 ml/min/kg
Eprosartan1–213308d9820800d ml/minn.r.
Irbesartan1.5–260–8053–939011–15157–176 ml/min3.0–3.5 ml/min
Losartan1 and 3–4a3334 and 12a98.7 and 99.8a2 and 6–9a600 ml/min and 50 ml/min75 ml/min and 25 ml/min
Olmesartan medoxomil1–22617991321.7 ml/min10 ml/min
Telmisartan0.5–142–58b500>99.524>800 ml/minn.a.
Valsartanc2–4251795633.3 ml/min10.3 ml/min
  • n.r., not reported; n.a., not applicable.

  • a Values for parent compound and active metabolite EXP3174, respectively.

  • b Values for 40 and 160 mg, respectively (dose-dependent bioavailability).

  • c Values apply similarly to the tablet and capsule formulations.

  • d Values derived from population pharmacokinetic analysis, a study in healthy volunteers reported values of 12.6 liters and 132 ml/min, respectively (Tenero et al., 1998b).