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. 2017 Aug 23;58(1):57–63. doi: 10.1002/jcph.974

Table 2.

Mirogabalin Plasma and Urinary Pharmacokinetic Parameters

Renal Classification According to CrCla
Normal (n = 6) Mild (n = 6) Moderate (n = 6) Severe (n = 6) ESRD (n = 6)
Plasma parametersb
AUClast, ng·h/mL 341.9 (16.5) 452.9 (32.6) 650.6 (10.9) 1244 (24.4) 1796 (55.5)
AUC0–inf, ng·h/mL 358.6 (16.1) 474.7 (30.0) 671.6 (11.3) 1266 (23.6) 2989 (51.8)c
Cmax, ng/mL 73.7 (35.9) 73.4 (36.8) 74.8 (20.0) 109.3 (24.5) 96.8 (31.9)
Tmax, h 1.3 (1.0, 2.0) 2.0 (1.0, 4.0) 1.7 (1.0, 5.0) 2.0 (1.5, 5.0) 4.0 (1.9, 5.0)
t1/2, h 2.8 (36.2) 3.4 (24.4) 5.6 (9.5) 7.5 (14.5) 39.8 (62.9)c
CL/F, L/h 13.9 (16.1) 10.5 (30.0) 7.4 (11.3) 3.9 (23.6) 1.7 (51.8)c
Vz/F, L 56.0 (47.8) 52.3 (18.1) 59.8 (19.2) 42.7 (32.4) 96.2 (29.1)c
Urinary parametersb
Fe0–48 h, % 75.2 (6.6) 64.3 (6.8) 57.0 (10.3) 46.1 (31.4)
CLr, L/h 10.2 (15.1) 6.7 (30.0) 4.3 (8.7) 1.8 (20.6)

AUC0–inf, area under the plasma concentration–time curve up to infinity; AUClast, area under the plasma concentration–time curve up to the last quantifiable time; CL/F, apparent total body clearance; Cmax, maximum plasma concentration; CLr, renal clearance; CrCl, creatinine clearance; CV, coefficient of variance; ESRD, end‐stage renal disease (4‐hour hemodialysis 24 hours after drug administration); Fe0–48 h, cumulative percentage of dose excreted into urine up to 48 hours; Tmax, time to reach maximum plasma concentration; t1/2, terminal elimination half‐life; Vz/F, apparent volume of distribution based on the terminal phase.

a

Renal function groups, based on the Cockcroft‐Gault formula,12 were normal (estimated creatinine clearance [CrCl] > 80 mL/min/1.73 m2), mild impairment (50 mL/min/1.73 m2 ≤ CrCl ≤ 80 mL/min/1.73 m2), moderate impairment (30 mL/min/1.73 m2 ≤ CrCl < 50 mL/min/1.73 m2), severe impairment (CrCl < 30 mL/min/1.73 m2), and ESRD (patients undergoing hemodialysis, regardless of CrCl).

b

Geometric mean (geometric CV%) values are presented for parameters excluding Tmax. Median (minimum, maximum) values are presented for Tmax.

c

n = 5. One subject had 3 unusable PK sampling points.