TABLE 8

Doses and tebipenem formulation for each cohort

PhaseCohortNo. (active:placebo)TBPM-PI-HBr dose/formulationa
SAD18 (6:2)300 mg, 12-h ER, fasted/fed
28 (6:2)600 mg, 12-h ER, fasted/fedb
38 (6:2)900 mg, 12-h ER, fasted
68 (6:2)100 mg, 12-h ER, fasted
78 (6:2)600 mg, 12-h ER fasted/fedb
88 (6:2)300 mg, IR, fasted/fed
98 (6:2)300 mg, 2-h ER, fasted/fed
108 (6:2)300 mg, 4-h ER, fasted/fed
118 (6:2)300 mg, 6-h ER, fasted/fed
128 (8:0)300 mg (Orapenem), fasted/fedc
138 (6:2)600 mg, IR, fasted/fed
148 (6:2)600 mg, 4-h ER, fasted/fed
158 (6:2)Not used
168 (6:2)100 mg, IR, fasted
178 (6:2)900 mg, IR, fasted
MAD48 (6:2)300 mg, IR q8h for 14 days
58 (6:2)600 mg, IR q8h for 14 days
  • a TBPM-PI-HBr dosages indicate amounts of TBPM-PI; each 300-mg dose of TBPM-PI contains 231 mg of active TBPM.

  • b Initially, cohort 2 and cohort 7 were designed as receiving the same dosage of SPR994 (600-mg 12-h ER) under fasting-only and fasting/fed conditions, respectively. A protocol amendment allowed subjects in cohort 2 to return to the unit for repeated dosing in fed condition after a 5-day washout, in order to maximize the number of subjects with fed-condition dosing at this dose. Five of the 8 subjects in cohort 2 returned for this fed-condition dosing. These cohorts were combined for the fasted/fed PK analysis of the 600-mg 12-h ER dosing group.

  • c Orapenem dosage refers to 300 mg of active TBPM, or 389.1 mg of TBPM-PI granules. The Orapenem granule cohort was open label, not placebo controlled.