TABLE 3

Plasma PK parameters for tebipenem during the fed state in SAD phase (PK analysis population)

Drug and doseMedian
(range) for
Tmax (h)
Arithmetic mean (% CV)
Cmax
(ng/ml)
AUClast
(h·ng/ml)
AUC0–∞
(h·ng/ml)
t1/2 (h)Nominal dose
CL (liters/h)V (liters)
TBPM-PI-HBr
    12 h, 300 mg (n = 6)5.0 (2.0–8.0)1,892 (51.0)7,175 (38.5)aaaa
    12 h, 600 mg (n = 6)4.0 (4.0–12.0)3,014 (37.5)14,213 (32.0)14,727b (37.0)1.3b (25.9)35.3b (44.9)70.6b (71.6)
    2 h, 300 mg (n = 6)4.0 (4.0–8.0)1,852 (37.7)5,528 (23.8)6,215b (14.8)1.1b (5.3)37.8b (16.1)59.1b (11.3)
    4 h, 300 mg (n = 6)4.0 (2.0–6.0)1,677 (50.5)5,417 (31.2)6,549b (0.2)0.9b (17.5)35.3b (0.2)43.9b (17.7)
    4 h, 600 mg (n = 6)4.0 (1.5–6.0)5,830 (56.4)15,363 (39.3)16,547c (39.9)1.1c (31.3)31.9c (43.4)53.6c (74.4)
    6 h, 300 mg (n = 6)4.0 (2.0–4.0)2,288 (32.7)6,579 (16.0)dddd
    IR, 300 mg (n = 6)2.0 (0.5–4.0)2,058 (31.8)6,169 (21.3)6,137e (23.7)0.9e (9.3)39.5e (24.5)49.0e (32.6)
    IR, 600 mg (n = 6)1.5 (0.5–4.0)6,451 (73.7)14,160 (42.4)14,200 (42.4)0.9 (15.8)37.7 (43.2)44.9 (34.1)
Orapenem, 300 mg (n = 7)0.5 (0.5–1.0)8,718 (40.3)11,321 (29.6)11,352 (29.7)0.8 (17.1)28.7 (32.3)32.6 (26.4)
  • a —, n = 0.

  • b n = 3.

  • c n = 4.

  • d —, n = 2.

  • e n = 5.