Table 1.
Studies included in the SC belimumab population pharmacokinetic analysis
| Study, subject population | Number of patients (n) | Dose and administration | Pharmacokinetic sampling | Ref. |
|---|---|---|---|---|
| Phase 1 US population | 19–20 subjects per treatment cohort, males and females (∼1:1), total of 118 subjects. | Cohort 1: Single-dose on Day 0, SC 240 mg belimumab (2 × 0.6 mL (2 × 120 mg)). Cohort 2: Single-dose on Day 0, SC 240 mg belimumab (1 × 1.2 mL (1 × 240 mg)). Cohort 3: Single-dose on Day 0, SC 200 mg belimumab (1 × 1.0 mL (1 × 200 mg)). Cohort 4: Single-dose on Day 0, IV 240 mg belimumab (1 h infusion). Cohort 5: Multiple-dose, weekly × 4 (qwk × 4) on Days 0, 7, 14 and 21, SC 240 mg belimumab (2 × 0.6 mL (2 × 120 mg)). Cohort 6: Multiple-dose, qwk × 4 on Days 0, 7, 14 and 21, SC 200 mg belimumab (1 × 1.0 mL (1 × 200 mg)). Randomization was stratified by weight ( < 75 kg vs ≥75 kg) and SC administration site (abdomen vs. thigh). | SC single-dose (cohorts 1, 2 and 3): Days 1–7, 10, 14, 21, 28, 42, 56, and 70. IV single-dose (cohort 4): 5 min, 1 and 3 h post-dose administration and on Days 1, 2, 4, 7, 14, 21, 28, 42, 56, and 70. SC multiple-dose (cohorts 5 and 6): Days 1–6, 7 (prior to 2nd dosing), 14 (prior to 3rd dosing), 21 (prior to 4th dosing and 6 h post-dosing), 22–28, 31, 35, 42, 49, 63, 77, 91, and 119. Serum belimumab concentrations were quantified using validated electrochemiluminescence (ECL)-based method. | 7 |
| Phase 1 Japanese population | Eight subjects per treatment cohort, males, total of 16 subjects. | Cohort 1: Single-dose, IV 200 mg (∼1 h infusion). Cohort 2: Single dose, SC 200 mg (1 × 200 mg). Randomization was stratified by weight (<65 kg vs ≥65 kg). The SC administration site was the thigh. | IV single-dose (cohort 1): Pre-dose and 5 min, 1, and 6 h after post-dose administration, and on Days 1, 2, 4, 7, 14, 21, 28, 42, 56, and 70. SC single-dose (cohort 2): Pre-dose and 6 h post-dose administration and on Days 1, 2, 3, 4, 5, 6, 7, 10, 14, 21, 28, 42, 56, and 70. Serum belimumab concentrations were quantified using validated ECL-based method. | 8 |