Miltefosine作用于癌细胞系A431和HeLa,抑制PI3K/Akt活性,ED50分别为17.2 μM和8.1 μM,是第一个用于治疗内脏利什曼病的口服药物,有效对抗前鞭毛体和无鞭毛体。
Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.
10,20,30,40,, 50μM
50 mg/kgi.p.
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] Uberall F, et al. Cancer Res, 1991, 51(3), 807-812.
分子式 C21H46NO4P |
分子量 407.57 |
CAS号 58066-85-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO <1 mg/mL |
Water 80 mg/mL |
Ethanol 80 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01462500 | Cutaneous Leishmaniasis | Drug: Miltefosine | Centro Internacional de Entrenamiento e Investigaciones Mdicas|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) | Phase 4 | 2011-10-01 | 2016-08-18 |
NCT02687971 | Cutaneous Leishmaniasis | Drug: Miltefosine | Drugs for Neglected Diseases | Phase 2 | 2016-12-01 | 2017-03-14 |
NCT02427308 | Leishmaniasis or Other Uses of Miltefosine | Drug: Miltefosine | Knight Therapeutics (USA) Inc | 2015-07-01 | 2017-02-28 | |
NCT02193022 | Post Kala Azar Dermal Leishmaniasis | Drug: Miltefosine | International Centre for Diarrhoeal Disease Research, Bangladesh|Thrasher Research Fund | Phase 3 | 2014-07-01 | 2016-03-24 |
NCT02429518 | Mucocutaneous Leishmaniasis | Drug: Miltefosine | Knight Therapeutics (USA) Inc | 2015-12-01 | 2017-02-28 | |
NCT02431429 | Mucocutaneous Leishmaniasis | Drug: Miltefosine | Knight Therapeutics (USA) Inc | 2015-07-01 | 2017-02-28 | |
NCT00371995 | Visceral Leishmaniasis | Drug: Liposomal amphotericin B and Miltefosine | Banaras Hindu University|Rajendra Memorial Research Institute of Medical Sciences | Phase 2 | 2007-10-01 | 2011-06-21 |
NCT00487253 | Cutaneous Leishmaniasis | Drug: Miltefosine|Drug: Meglumine antimoniate | Centro Internacional de Entrenamiento e Investigaciones Mdicas|Instituto Colombiano para el Desarrollo de la Ciencia y la Tecnologa (COLCIENCIAS)|INS|Instituto Nacional de Dermatologa Centro dermatolgico Federico Lleras Acosta | Phase 3 | 2007-07-01 | 2010-02-13 |
NCT01380301 | Cutaneous Leishmaniasis | Drug: Miltefosine and antimony|Drug: Miltefosine alone | Foundation Fader|AB Foundation | Phase 2 | 2007-03-01 | 2011-06-22 |
NCT03023111 | Cutaneous Leishmaniasis | Drug: Sbv|Drug: Miltefosine plus placebo|Drug: Miltefosine plus GM-CSF | Hospital Universitrio Professor Edgard Santos|Oswaldo Cruz Foundation | Phase 3 | 2017-03-01 | 2017-01-18 |
NCT02429505 | Leishmaniasis | Drug: Miltefosine | Knight Therapeutics (USA) Inc | 2015-07-01 | 2017-02-28 | |
NCT01050907 | Mucosal Leishmaniasis|Cutaneous Leishmaniasis | Drug: miltefosine | Knight Therapeutics (USA) Inc | Phase 2 | 2010-05-01 | 2015-03-24 |
NCT02011958 | Visceral Leishmaniasis | Drug: Liposomal Amphotericin B|Drug: Miltefosine | Drugs for Neglected Diseases|Medecins Sans Frontieres, Netherlands|London School of Hygiene and Tropical Medicine|Addis Ababa University|Institute of Tropical Medicine, Belgium|Slotervaart Hospital|University of Gondar | Phase 3 | 2014-07-01 | 2016-10-06 |
NCT00471705 | Cutaneous Leishmaniasis | Drug: Miltefosine|Device: Thermotherapy|Drug: Glucantime | Universidad de Antioquia | Phase 3 | 2006-06-01 | 2010-07-15 |
NCT01377974 | Leishmaniasis|Leishmaniasis, Mucocutaneous | Drug: Miltefosine|Drug: Standard Treatment Meglumine antimoniate | Brasilia University Hospital | Phase 2 | 2009-07-01 | 2015-06-08 |
NCT00600548 | Treatment of Cutaneous Leishmaniasis in Brazil. | Drug: Miltefosine.|Drug: Meglumine antimoniate.|Drug: Miltefosine.|Drug: Meglumine antimoniate. | Hospital Universitrio Professor Edgard Santos|Conselho Nacional de Desenvolvimento Cientfico e Tecnolgico|Ministerio de Ciencia e Innovacin, Spain|Ministrio da Sade|AEterna Zentaris | Phase 2 | 2007-07-01 | 2010-04-14 |
NCT00373568 | Leishmaniasis | Drug: miltefosine: 2.5 mg/kg/day for 42 days | AB Foundation | Phase 1|Phase 2 | 2005-04-01 | 2010-05-29 |
NCT02431143 | Visceral Leishmaniasis | Drug: Miltefosine | Drugs for Neglected Diseases | Phase 2 | 2015-05-01 | 2016-10-10 |
NCT02530697 | Leishmaniasis | Drug: Meglumine antimoniate|Drug: Miltefosine|Drug: Pentoxifylline | University of Brasilia | Phase 2 | 2015-08-01 | 2016-05-22 |
NCT01380314 | Cutaneous Leishmaniasis | Drug: Miltefosine + Imiquimod|Drug: Miltefosine 150 mg x day + Placebo | Foundation Fader | Phase 2 | 2008-03-01 | 2011-06-22 |
NCT01122771 | Visceral Leishmaniasis | Drug: Liposomal amphotericin B|Drug: liposomal amphotericin B + miltefosine|Drug: liposomal amphotericin B + paromomycin|Drug: Miltefosine + Paromomycin | Drugs for Neglected Diseases|Shaheed Surhawardy Medical College and Hospital|International Centre for Diarrhoeal Disease Research, Bangladesh | Phase 3 | 2010-05-01 | 2016-01-20 |
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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