100 mg/qd | 200 mg/qd | 300 mg/qd | 450 mg/qd | 600 mg/qd | 800 mg/qd | ||
---|---|---|---|---|---|---|---|
(n = 4) | (n = 3) | (n = 3) | (n = 4) | (n = 3) | (n = 3) | ||
Tmax,ss(h) | BPI-9016M | 2.00(2.00–2.00) | 2.00(1.00–5.00) | 3.00(2.00–10.0) | 3.50(2.37–6.00) | 3.00(3.00–6.00) | 6.00(4.00–6.00) |
M1 | 0.00(0.00–5.00) | 6.00(0.00–8.00) | 2.00(0.00–2.00) | 10.0(2.37–24.0) | 6.00(0.500–12.0) | 3.00(0.00–4.00) | |
M2-2 | 0.500(0.00–0.500) | 1.00(0.00–24.0) | 0.500(0.00–2.00) | 20.0(0.500–24.0) | 6.00(0.500–24.0) | 1.00(0.00–24.0) | |
Cmax,ss (ng/mL) | BPI-9016M | 256(199) | 571(341) | 678(624) | 731(150) | 986(336) | 963(210) |
M1 | 629(200) | 2010(660) | 2270(882) | 3420(919) | 3600(1540) | 5770(2700) | |
M2-2 | 563(115) | 1460(155) | 2520(1400) | 3210(1200) | 2550(1720) | 4810(2390) | |
AUClast (h*ng/mL) | BPI-9016M | 1760(949) | 8220(6500) | 5720(5480) | 11,200(3010) | 14,000(5430) | 17,600(6940) |
M1 | 17,600(5200) | 99,100(57100) | 69,300(55800) | 161,000(59300) | 147,000(63800) | 261,000(124000) | |
M2-2 | 20,700(2950) | 85,800(19000) | 87,800(71300) | 169,000(99100) | 118,000(64400) | 240,000(133000) | |
t1/2 (h) | BPI-9016M | 8.79(1.95) | 21.0(11.1) | 12.2(2.74) | 10.5(2.23) | 13.8(3.07) | 11.3(2.86) |
M1 | 12.1(0.922) | 21.7(8.11) | 17.8(7.04) | 20.8(2.14) | 25.6(2.13) | 26.2(0.694) | |
M2-2 | 20.8(4.63) | 15.9(NA) | |||||
Ke (1/h) | BPI-9016M | 0.0818(0.0197) | 0.0386(0.0159) | 0.0587(0.0119) | 0.0684(0.0137) | 0.0522(0.0122) | 0.0647(0.0185) |
M1 | 0.0573(0.00417) | 0.0344(0.0129) | 0.0445(0.0216) | 0.0335(0.00345) | 0.0272(0.00238) | 0.0265(0.000701) | |
M2-2 | 0.0341(0.00759) | 0.0437(NA) | |||||
CLss/F (L/h) | BPI-9016M | 75.0(35.0) | 55.2(39.2) | 106.0(77.0) | 56.6(10.4) | 61.8(26.9) | 65.6(24.4) |
Vz,ss/F (L) | BPI-9016M | 963(579) | 1530(872) | 2030(1840) | 841(165) | 1150(227) | 1070(499) |