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Supplemental Data DMD #48819 Supplemental Data Title: Application of Hybrid Approach Based on Empirical and Physiological Concept for Predicting Pharmacokinetics in Humans -Usefulness of Exponent on Prospective Evaluation of Predictability- Authors: Hiroyuki Sayama, Hiroshi Komura, Motohiro Kogayu Journal Title: Drug Metabolism and Disposition 1 DMD #48819 Supplemental Table 1 In vitro and in vivo data for allometric scaling of CL and Vss fup RB in vitro CLint (mL/min/kg) in vivo CL (mL/min/kg) in vivo Vss (mL/kg) Refference Human Human Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Acivicin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 580 500 600 -- 650 930 63 Alfentanil -- -- -- -- -- -- -- -- -- -- -- -- -- -- 800 953 -- 1069 975 -- 8 Amiodarone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 66000 4600 5110 -- 72300 -- 23 Amlodipine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 21000 25000 -- -- 32000 27000 101 Amphotericin B -- -- -- -- -- -- -- -- -- -- -- -- -- -- 4011 5025 -- 1855 2300 3121 85 Amsacrine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1560 2800 -- 1700 4500 7420 80 Antipyrine 1 1 0.28 3.95 -- 4.07 1.58 -- 0.62 a 8.18 a -- 7.32 a 3.53 a -- 584 a 738 a -- 903 a 657 a 720 5, 6, 12, 52, 76, 91, 118 Biperiden -- -- -- -- -- -- -- -- -- -- -- -- -- -- 6200 9500 3600 19300 14000 -- 23, 70 Bosentan -- -- 0.68 0.87 -- 15.89 5.71 7.91 2.00 1.3 -- 72 38.1 31.43 -- -- -- -- -- -- 49, 52 Caffeine 0.96 1 0.40 0.83 -- 1.18 2.55 -- 1.32 a 1.83 a -- 5.03 a 5.02 a -- 614 a 887 a 830 508 a 763 a 760 9, 10, 11, 17, 52, 81, 98 Cefazolin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 107 271 128 142 225 192 89 Cefmetazole -- -- -- -- -- -- -- -- -- -- -- -- -- -- 143 235 138 220 490 368 89 Cefoperazone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 144 277 126 237 287 309 89 Cefotetan -- -- -- -- -- -- -- -- -- -- -- -- -- -- 133 249 167 237 250 241 89 Cefpiramide -- -- -- -- -- -- -- -- -- -- -- -- -- -- 111 454 100 109 264 660 89 Ceftizoxime -- -- -- -- -- -- -- -- -- -- -- -- -- -- 200 239 a 268 a -- 392 a 653 a 67, 73 Chlordiazepoxide -- -- -- -- -- -- -- -- -- -- -- -- -- -- 250 2540 -- -- 1454 -- 73, 86, 102 Chlorpheniramine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 3170 4050 -- 10100 -- -- 90 Chlorpromazine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 11200 18600 8000 -- 29100 -- 23, 90 Ciprofloxacin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 2100 4014 a 1800 3093 a 4600 -- 1, 2, 73, 95 Cyclosporine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1450 1650 -- 3160 4540 2733 a 3, 27, 66, 88, 110 Diazepam 0.032 0.58 2.16 121.2 -- -- 92.23 -- 0.5 a 21.4 a -- -- 84.22 a -- 1085 a 7136 a -- 5500 4715 a -- 43, 93 Diclofenac -- -- -- -- -- -- -- -- -- -- -- -- -- -- 59 a 189 a 170 57 370 -- 64, 84, 103, 107, 117 a Recalculated from plasma concentration-time profiles reported in the reference articles. 2 DMD #48819 Supplemental Table 1 Continued fup RB in vitro CLint (mL/min/kg) in vivo CL (mL/min/kg) in vivo Vss (mL/kg) Refference Human Human Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Didanosine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 810 950 920 -- 990 900 41 Diltiazem 0.2 1.03 5.86 10.66 -- -- 191.49 -- 13.02 a 33.33 a -- -- 89.23 a -- 3110 a 3581 a 3500 -- 3400 a -- 23, 33, 54, 69, 86, 93 Dofetilide -- -- -- -- -- -- -- -- -- -- -- -- -- -- 2800 4000 -- -- 3100 6300 97 Enprofylline -- -- -- -- -- -- -- -- -- -- -- -- -- -- 510 638 -- 206 342 452 108 Epiroprim 0.11 1.1 1.85 2.76 8.45 -- 45.24 38.21 3.57 a 10.82 a 24.82 a -- 42.30 a 151.48 a 2501 a 8006 a 3151 a -- 4122 a 8356 a 60 Erythromycin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 886 2700 -- 6875 8400 4500 18 Ethosuximide -- -- -- -- -- -- -- -- -- -- -- -- -- -- 630 590 800 960 700 2000 5, 21, 79 Felodipine 0.004 23.13 56.06 -- -- 127.37 -- 8.9 a 20.73 a -- -- 90.42 a -- 3262 a 2559 a -- -- 9006 a -- 4, 20, 93, 109 Fentanyl -- -- -- -- -- -- -- -- -- -- -- -- -- -- 5207 10533 -- -- 4574 -- 8, 86 Fexofenadine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 771 -- 302 -- 4254 -- 37, 47, 75 Flindokalner -- -- -- -- -- -- -- -- -- -- -- -- -- -- 2350 3200 5400 -- 3400 -- 23 Fluconazole -- -- -- -- -- -- -- -- -- -- -- -- -- -- 710 700 -- 880 800 1100 39 Flunitrazepam -- -- -- -- -- -- -- -- -- -- -- -- -- -- 4580 13000 -- -- 3810 -- 86, 102 Fluvastatin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 420 700 3700 290 7300 1000 56, 104, 105, 106 Garenoxacin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1000 1300 1000 -- 900 -- 23 Gentamicin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 330 320 -- 338 a 398 a -- 73, 87, 99, 115 Haloperidol -- -- -- -- -- -- -- -- -- -- -- -- -- -- 18000 37000 6600 -- 10400 -- 23 Interferon-alpha A -- -- -- -- -- -- -- -- -- -- -- -- -- -- 449 190 190 130 261 233 48 Ketamine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 2700 4526 -- -- 3929 -- 8 Lamifiban -- -- -- -- -- -- -- -- -- -- -- -- -- -- 290 750 290 -- 240 -- 50 Lamivudine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1300 870 1160 -- 2700 -- 41 Lidocaine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1080 -- 706 -- 3110 -- 90, 94 Lorazepam -- -- 0.93 71.46 -- -- 16.69 -- 1.1 26.1 -- -- 27.2 -- -- -- -- -- -- -- 93 a Recalculated from plasma concentration-time profiles reported in the reference articles. 3 DMD #48819 Supplemental Table 1 Continued fup RB in vitro CLint (mL/min/kg) in vivo CL (mL/min/kg) in vivo Vss (mL/kg) Refference Human Human Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Metazosin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 426 -- -- 847 5955 7100 46 Methadone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 3800 7600 8200 -- 7580 -- 23 Methohexitone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 4664 1815 -- 1320 3871 -- 8 Methotrexate -- -- -- -- -- -- -- -- -- -- -- -- -- -- 308 377 -- 200 1095 a 2194 13, 14, 28, 36, 59 Mibefradil -- -- 2.84 24.48 -- 59.13 23.72 -- 7 36 -- 64 94 -- -- -- -- -- -- -- 52 Midazolam 0.019 0.55 28.68 130.28 -- 73.92 483.12 -- 4.4 a 48.95 a -- 14.23 a 59.62 a -- 713 a 1582 a 3350 734 a 1648 a 2000 26, 30, 52, 72, 74, 81 Mifepristone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 300 10500 32500 -- 4300 -- 23 Mofarotene -- -- 6.17 3.95 -- -- 10.1 7.25 11 5.8 -- -- 16 27 -- -- -- -- -- -- 52 Moxalactam -- -- -- -- -- -- -- -- -- -- -- -- -- -- 138 197 162 234 276 241 89 Moxifloxacin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 2000 2700 4900 -- 3600 3700 96 Naloxone -- -- 51.5 126.73 -- -- 239.8 -- 25 42.5 -- -- 48.8 -- -- -- -- -- -- -- 93 Napsagatran -- -- -- -- -- -- -- -- -- -- -- -- -- -- 343 690 263 986 615 -- 53 Nicardipine 0.068 0.71 22.51 63.17 -- -- 118.58 -- 7.68 a 38.65 a -- -- 29.77 a -- 489 a 797 a 1375 a -- 808 a -- 31, 71, 86, 93 Nifedipine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 780 1150 500 -- 127 -- 23 Nilvadipine -- -- 41.02 43.03 -- -- 130.44 -- 20 15.3 -- -- 94 -- -- -- -- -- -- -- 93 Nitrendipine 0.02 -- 37.01 31.98 -- -- 105.41 -- 19.23 a 17.17 a -- -- 11.28 a -- 5731 a 1543 a -- 377 a -- 45, 65, 93 Ofloxacin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1780 1150 1600 -- 1660 -- 23 Oleandomycin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 771 1600 -- -- 6800 5500 18 Oxazepam 0.043 -- 1.23 4.74 -- -- 5.71 -- 1.58 a 4.33 a -- -- 20.22 a -- 861 a 1418 a -- -- 1258 a -- 16, 86, 93, 100, 112 Pentobarbital -- -- -- -- -- -- -- -- -- -- -- -- -- -- 990 -- -- 1300 1640 -- 38, 91 Phencyclidine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 6200 17000 -- 23200 9000 5 Prednisolone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 860 -- -- 1370 1370 -- 24, 38, 73 Propafenone 0.024 0.7 5.52 7.80 -- -- 9.83 14.16 14.63 a 28.7 a -- -- 34.67 a 142.37 a 3492 a 2748 a -- 4500 1919 a 3130 a 34, 44, 82, 83, 86 a Recalculated from plasma concentration-time profiles reported in the reference articles. 4 DMD #48819 Supplemental Table 1 Continued fup RB in vitro CLint (mL/min/kg) in vivo CL (mL/min/kg) in vivo Vss (mL/kg) Refference Human Human Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Human Dog Monkey Rabbit Rat Mouse Propranolol 0.068 0.81 12.95 75.01 -- -- 223.99 10.15 a 40.9 a -- -- 96.8 a -- 2421 a 1544 a 5308 a -- 4720 a -- 7, 22, 29, 52, 91 Quinidine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 3500 -- 427 5030 5800 5840 40, 90, 114 Ranitidine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1200 1722 a -- -- 216 a -- 19, 35, 73 Recainam -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1400 1200 3800 3600 3200 -- 92 Remoxipride -- -- -- -- -- -- -- -- -- -- -- -- -- -- 700 1600 1100 -- 4500 3200 23, 116 Sematilide -- -- -- -- -- -- -- -- -- -- -- -- -- -- 740 1400 -- 1813 2167 -- 32 Semaxanib -- -- -- -- -- -- -- -- -- -- -- -- -- -- 980 1400 1450 -- 1600 -- 23 Sildenafil -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1200 5200 -- -- 1100 1000 113 Stavudine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 530 -- 920 -- 700 760 41 Sumatriptan -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1635 2027 -- 4143 2642 -- 15 Susalimod -- -- -- -- -- -- -- -- -- -- -- -- -- -- 120 190 80 170 1200 310 77 Tamsulosin -- -- -- -- -- -- -- -- -- -- -- -- -- -- 205 1778 -- 2711 2857 -- 111 Theophylline 0.51 0.83 0.34 0.59 -- 0.89 0.79 -- 0.82 a 1.52 a -- 3.18 a 1.9 a -- 579 a 710 a -- 923 a 857 a 840 5, 25, 42, 52, 57, 86, 119 Thiopentone -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1757 1499 -- 613 943 -- 8 Tolcapone 0.001 0.6 3.7 5.53 -- 16.26 11.42 -- 1.43 a 1.45 a -- 10.82 a 5.7 a -- 124 a 220 a -- 153 a 98 a -- 51 Tolterodine -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1800 1500 -- -- 23000 16000 78 Triazolam -- -- -- -- -- -- -- -- -- -- -- -- -- -- 1260 1400 -- -- 2240 -- 86, 102 Valproic Acid --
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