Rilpivirine (利匹韦林; R278474, TMC 278) 是HIV的非核苷逆转录酶抑制剂。
Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.
4 mg/kg(大鼠);1.25 mg/kg(另一物种)静脉注射,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] Janssen PA, et al. J Med Chem. 2005, 48(6), 1901-1909.
分子式 C22H18N6 |
分子量 366.42 |
CAS号 500287-72-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 70 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01562886 | HIV | Drug: Rilpivirine | Imperial College London|Janssen-Cilag Ltd. | Phase 1 | 2012-03-01 | 2014-05-19 |
NCT02494986 | Human Immunodeficiency Virus Type 1 | Drug: Rilpivirine | Janssen Sciences Ireland UC | Phase 2 | 2015-07-01 | 2016-08-25 |
NCT02547870 | Human Immunodeficiency Virus Type 1 | Drug: Rilpivirine (RPV)|Drug: Rilpivirine Long-Acting Parenteral Formulation (RPVA)|Drug: Aged RPVA | Janssen Infectious Diseases BVBA | Phase 1 | 2015-08-01 | 2016-07-05 |
NCT02404233 | HIV Positive | Drug: darunavir/cobicistat|Drug: rilpivirine | Therapeutic Concepts|Janssen Scientific Affairs, LLC | Phase 4 | 2015-03-01 | 2015-03-30 |
NCT01719614 | Healthy Participants | Drug: Metformin|Drug: Rilpivirine | Janssen R&D Ireland | Phase 1 | 2012-10-01 | 2014-03-05 |
NCT02530060 | Healthy | Drug: Rilpivirine/Tenofovir Disoproxil Fumarate/Emtricitabine FDC | Janssen Pharmaceutical K.K. | Phase 4 | 2015-08-01 | 2016-12-30 |
NCT01615614 | Healthy | Drug: Rilpivirine|Drug: Rifabutin | Janssen R&D Ireland | Phase 1 | 2012-04-01 | 2014-03-27 |
NCT03033368 | HIV | Drug: Rilpivirine | Mahidol University|amfAR, The Foundation for AIDS Research | Phase 2|Phase 3 | 2015-07-01 | 2017-01-24 |
NCT01692470 | Human Immunodeficiency Virus Type 1 (HIV-1) Infection | Drug: No intervention | Janssen Pharmaceutica | Phase 4 | 2013-06-01 | 2015-11-30 |
NCT01585038 | Cardiovascular Disease | Drug: Efavirenz|Drug: Rilpivirine | Indiana University|Janssen Services, LLC | Phase 4 | 2012-07-01 | 2015-07-27 |
NCT02165202 | Human Immunodeficiency Virus (HIV) | Drug: Rilpivirine|Drug: Placebo | PATH|Bill and Melinda Gates Foundation|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) | Phase 2 | 2014-10-01 | 2016-03-14 |
NCT01268839 | HIV | Drug: TMC278|Drug: TMC278|Drug: Efavirenz | Tibotec, Inc|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA | Phase 1 | 2010-01-01 | 2013-09-02 |
NCT02104700 | HIV | Drug: Rilpivirine/Emtricitabine/Tenofovir | Philip Grant|Rwanda Biomedical Center|Gilead Sciences|Stanford University | Phase 2|Phase 3 | 2014-04-01 | 2015-07-15 |
NCT02561936 | Healthy | Drug: Rilpivirine Oral Tablet|Drug: Rilpivirine formulation G007|Drug: Rilpivirine formulation G009-01|Drug: Rilpivirine formulation G002|Dietary Supplement: Standardized Breakfast | Janssen Sciences Ireland UC | Phase 1 | 2015-10-01 | 2016-06-09 |
NCT01049932 | HIV Infections | Drug: TMC278LA | St Stephens Aids Trust | Phase 1|Phase 2 | 2010-03-01 | 2010-08-13 |
NCT01656018 | Healthy | Drug: TMC278, Long acting (LA) | Janssen Research & Development, LLC | Phase 1 | 2012-11-01 | 2016-04-06 |
NCT01266902 | HIV-1 Infection | Drug: Rilpivirine | Janssen R&D Ireland | Phase 3 | 2011-02-25 | 2017-03-14 |
NCT00799864 | Human Immuno Deficiency (HIV) Infection | Drug: Rilpivirine|Drug: Zidovudine|Drug: Abacavir|Drug: Tenofovir disoproxil fumarate|Drug: Lamivudine|Drug: Emtricitabine | Janssen Sciences Ireland UC | Phase 2 | 2011-01-07 | 2017-03-21 |
NCT01975012 | HIV Infections | Drug: Rilpivirine | National Institute of Allergy and Infectious Diseases (NIAID)|National Institute of Mental Health (NIMH) | Phase 1|Phase 2 | 2014-09-01 | 2015-08-31 |
NCT01804244 | Healthy | Drug: TMC278 | Janssen Pharmaceutical K.K. | Phase 4 | 2013-03-01 | 2014-03-18 |
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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