Lopinavir是一种有效的HIV protease(HIV蛋白酶)抑制剂, Ki为1.3 pM。
Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
10 mg/kg 口服
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Sham HL, et al. Antimicrob Agents Chemother, 1998, 42(12), 3218-3224.
[2] Weemhoff, J.L., et al., Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol, 2003. 55(3): p. 381-6.
[3] Vishnuvardhan, D., et al., Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. AIDS, 2003. 17(7): p. 1092-4.
分子式 C37H48N4O5 |
分子量 628.8 |
CAS号 192725-17-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 125 mg/mL |
Water <1 mg/mL |
Ethanol 125 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00771498 | HIV Infection|Tuberculosis | Drug: Lopinavir | Oswaldo Cruz Foundation|Abbott | Phase 4 | 2008-11-01 | 2015-05-15 |
NCT01074931 | HIV-1 Infections | Drug: Lopinavir/ritonavir (Kaletra) | Abbott | 2008-04-01 | 2011-07-07 | |
NCT01700790 | AIDS|Tuberculosis | Drug: Lopinavir/ritonavir and ritonavir | University of Miami|Oswaldo Cruz Foundation | Phase 4 | 2016-01-01 | 2016-12-06 |
NCT01172535 | HIV | Drug: Lopinavir/ritonavir | National Institute of Allergy and Infectious Diseases (NIAID) | Phase 2|Phase 3 | 2010-11-01 | 2015-11-16 |
NCT01581853 | HIV | Drug: Lopinavir/ritonavir 800 mg / 200mg | Daniel Podzamczer|Hospital Universitari de Bellvitge | Phase 4 | 2012-05-01 | 2016-10-05 |
NCT01002898 | HIV | Drug: lopinavir/ritonavir soft gel capsule | Bamrasnaradura Infectious Diseases Institute | Phase 3 | 2007-04-01 | 2011-11-10 |
NCT00605098 | HIV Infections|Pregnancy | Drug: Lopinavir / ritonavir|Drug: Lopinavir/ritonavir | Oswaldo Cruz Foundation|Ministry of Health, Brazil | Phase 4 | 2008-02-01 | 2013-10-25 |
NCT00621166 | HIV Infections | Drug: generic lopinavir/ritonavir | The HIV Netherlands Australia Thailand Research Collaboration | Phase 2 | 2008-06-01 | 2012-04-03 |
NCT00752037 | HIV Infections | Drug: lopinavir/ritonavir and raltegravir | Saint Michael's Medical Center|Abbott | Phase 4 | 2008-09-01 | 2011-07-19 |
NCT01660477 | Pharmacokinetics of Isavuconazole|Pharmacokinetics of Lopinavir/Ritonavir|Healthy Volunteers | Drug: Isavuconazole|Drug: Lopinavir/ritonavir | Astellas Pharma Global Development, Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc | Phase 1 | 2012-06-01 | 2015-02-20 |
NCT01139905 | HIV-1 Infections | Other: lopinavir/ritonavir | The HIV Netherlands Australia Thailand Research Collaboration|Chulalongkorn University|UMC St. Radboud, Nijmegen, The Netherlands | Phase 2 | 2010-04-01 | 2015-03-24 |
NCT00619944 | HIV Infections | Drug: Lumefantrine - lopinavir/ritonavir drug interaction|Drug: Lumefantrine only arm | Makerere University|University of Liverpool | Phase 4 | 2008-02-01 | 2010-12-03 |
NCT01237444 | HIV Infection | Drug: lopinavir/ritonavir plus one nucleoside|Drug: lopinavir /ritonavir plus two nucleosides | Pedro Cahn|Abbott|The Huesped Foundation | Phase 3 | 2010-12-01 | 2012-06-08 |
NCT01076972 | Human Immunodeficiency Virus | Drug: Lopinavir/ritonavir (Kaletra) | Abbott | 2000-12-01 | 2012-01-31 | |
NCT00985543 | Acquired Immunodeficiency Syndrome | Drug: lopinavir/ritonavir | Kirby Institute | Phase 1 | 2009-10-01 | 2011-03-02 |
NCT01076985 | Human Immunodeficiency Virus | Drug: Lopinavir/ritonavir (Kaletra) | Abbott | 2000-12-01 | 2011-12-09 | |
NCT00344487 | HIV | Drug: Lopinavir/Ritonavir | University of Maryland | 2005-12-01 | 2014-12-17 | |
NCT00762320 | HIV Infections | Drug: Low dose Kaletra tablets | Phoenix Children's Hospital|Abbott | 2008-10-01 | 2014-02-05 | |
NCT02348177 | Acquired Immunodeficiency Syndrome|Tuberculosis | Drug: lopinavir with ritonavir in 1:1 ratio|Drug: Lopinavir/ritonavir 4:1 | Drugs for Neglected Diseases|University of Cape Town|Medecins Sans Frontieres, Netherlands|French Development Agency|UBS Optimus Foundation | Phase 4 | 2013-01-01 | 2015-01-22 |
NCT00981318 | HIV Infections|Acquired Immunodeficiency Syndrome | Drug: lopinavir/ritonavir plus maraviroc | Rodwick, Barry M., M.D.|Abbott | Phase 4 | 2009-12-01 | 2015-06-20 |
NCT00159224 | HIV Infections | Drug: Lopinavir/ritonavir simplification strategy | The Huesped Foundation|Abbott | Phase 4 | 2005-04-01 | 2015-09-04 |
NCT00866021 | HIV/HCV Co-infection|HIV Infections | Drug: Lopinavir/ritonavir|Drug: Lopinavir/ritonavir with two nucleoside analogs | Fundacion SEIMC-GESIDA|Abbott | Phase 4 | 2008-02-01 | 2013-03-21 |
NCT01088516 | HIV | Drug: Lopinavir/Ritonavir (200/50 mg) Tablets + Zidovudine + 3TC | University of Zambia|University of Toronto|Abbott | Phase 4 | 2008-12-01 | 2015-06-22 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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