Pharmacokinetics, Safety, and Tolerability of Tenapanor in Healthy Chinese and Caucasian Volunteers: A Randomized, Open-Label, Single-Center, Placebo-Controlled Phase 1 Study
Table 2
Main PK parameters of tenapanor-M1 following single and repeated dose administration of tenapanor in healthy subjects.
10 mg, Chinese subjects (n = 12)
30 mg, Chinese subjects (n = 12)
50 mg, Chinese subjects (n = 12)
50 mg, Caucasian subjects (n = 11)
Geometric mean
Geo CV%
Geometric mean
Geo CV%
Geometric mean
Geo CV%
Geometric mean
Geo CV%
Single dose
(h)a
7.508 (4.00 to 10.00)
8.458 (2.00 to 9.95)
8.008 (3.97 to 10.05)
7.000 (4.00 to 10.00)
(ng/mL)
1.7294
36.84
3.4924
38.18
5.5194
36.30
5.2455
49.07
AUC0-t (hour ng/mL)
34.1165
57.46
90.9420
52.73
169.6988
40.29
129.4200
63.81
AUC0-∞ (hour ng/mL)
63.4915b
40.56
116.0119
44.11
195.0912
36.61
152.4630
51.84
(hour)
20.61b
30.40
18.82
26.47
18.54
24.65
16.37
22.36
CL/F (L/hour)
157.5015b
40.56
258.5942
44.11
256.2904
36.61
327.9484
51.84
/F (L)
4682.8820b
43.80
7021.5237
43.92
6855.9845
40.79
7745.8242
55.13
Repeated dose
(h)a
1.975 (0.98 to 6.97)
4.000 (0.00 to 9.00)
(ng/mL)
13.4617
29.89
12.1614
38.69
(ng/mL)
19.1772
26.31
17.6014
33.31
(ng/mL)
13.3380
30.11
12.1614
38.69
(ng/mL)
16.8094
26.05
15.2140
35.09
AUC0-τ (hour ng/mL)
201.7129
26.05
182.5681
35.09
DF (%)
33.7463
23.97
34.8939
23.18
(hour)
19.32
20.26
16.77
24.02
CLss/F (L/hour)
247.8770
26.05
273.8704
35.09
AUC area under curve, CV coefficient of variation, DF degree of fluctuation, SD standard deviation. aMedian (range). bn = 10.
