Lonafarnib(Sch66336)是口服生物相容性的FPTase抑制剂,对H-ras,K-ras-4B和N-ras的IC50分别为1.9 nM,5.2 nM和2.8 nM。
Lonafarnib (SCH 66336) is a selectively FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
0.1 μM - 8 μM
50 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] Liu M, et al. Cancer Res, 1998, 58(21), 4947-4956.
分子式 C27H31Br2ClN4O2 |
分子量 638.82 |
CAS号 193275-84-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 127 mg/mL |
Water <1 mg/mL |
Ethanol 15 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00539968 | Prostate Cancer|Breast Cancer|Ovarian Cancer|Lung Cancer|Gastric Cancer | Drug: Docetaxel plus lonafarnib | Merck Sharp & Dohme Corp. | Phase 1|Phase 2 | 2007-06-01 | 2015-02-04 |
NCT02527707 | Chronic Delta Hepatitis | Drug: lonafarnib|Drug: Ritonavir | Eiger BioPharmaceuticals|Hannover Medical School | Phase 2 | 2015-09-01 | 2016-09-14 |
NCT00109538 | Myelodysplastic Syndromes|Leukemia, Myelomonocytic, Chronic|Myelodysplasia|Myelomonocytic | Drug: Lonafarnib|Other: Placebo | Merck Sharp & Dohme Corp. | Phase 3 | 2005-05-01 | 2015-04-09 |
NCT00773474 | Metastatic Breast Cancer | Drug: Lonafarnib | George Sledge|Schering-Plough|Hoosier Cancer Research Network | Phase 2 | 2008-10-01 | 2016-01-21 |
NCT00081510 | Breast Cancer | Drug: Lonafarnib|Drug: Placebo|Drug: anastrozole | Merck Sharp & Dohme Corp. | Phase 2 | 2003-12-01 | 2015-03-26 |
NCT00047502 | Chronic Myelogenous Leukemia | Drug: Lonafarnib (SCH66336)|Drug: Imatinib Mesylate (Gleevec) | M.D. Anderson Cancer Center | Phase 1 | 2002-11-01 | 2012-02-20 |
NCT01495585 | Hepatitis D | Drug: Lonafarnib|Other: Placebo | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) | Phase 2 | 2011-12-01 | 2016-07-18 |
NCT02430194 | Chronic Hepatitis D Infection | Drug: lonafarnib|Drug: Ritonavir|Drug: PEG IFN-a | Eiger BioPharmaceuticals|Ankara University | Phase 2 | 2014-12-01 | 2017-02-26 |
NCT02430181 | Chronic Hepatitis D Infection | Drug: lonafarnib|Drug: PEG IFN-a|Drug: Ritonavir | Eiger BioPharmaceuticals | Phase 2 | 2014-11-01 | 2017-01-18 |
NCT00103090 | Head and Neck Cancer | Drug: Fenretinide|Drug: Lonafarnib | M.D. Anderson Cancer Center|National Cancer Institute (NCI) | Phase 1 | 2005-01-01 | 2012-11-12 |
NCT00288444 | Lung Cancer|Soft Tissue Sarcoma|Colorectal Carcinoma|Breast Cancer|Prostate Cancer | Drug: Lonafarnib|Drug: Docetaxel | Emory University|Aventis Pharmaceuticals|Schering-Plough | Phase 1 | 2006-01-01 | 2012-12-17 |
NCT00102648 | Glioblastoma Multiforme|Gliosarcoma|Brain Tumors | Drug: Sarasar|Drug: Temodar | M.D. Anderson Cancer Center|Schering-Plough | Phase 1 | 2004-12-01 | 2016-06-07 |
NCT00015899 | Brain and Central Nervous System Tumors | Drug: lonafarnib | Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) | Phase 1 | 2002-01-01 | 2009-10-13 |
NCT02968641 | Chronic Delta Hepatitis | Drug: Lonafarnib|Drug: Ritonavir | Eiger BioPharmaceuticals | Phase 2 | 2017-03-01 | 2016-11-16 |
NCT01232881 | Breast Cancer | Procedure: Tumor Sample|Procedure: Serum Sample | Hoosier Cancer Research Network|United States Department of Defense|Indiana University School of Medicine|Emory University | 2009-08-01 | 2011-04-27 | |
NCT00281515 | Epithelial Ovarian Cancer | Drug: Lonafarnib | AGO Study Group | Phase 2 | 2006-01-01 | 2012-06-28 |
NCT00083096 | Brain and Central Nervous System Tumors | Drug: lonafarnib|Drug: temozolomide | European Organisation for Research and Treatment of Cancer - EORTC | Phase 1 | 2004-03-01 | 2015-02-09 |
NCT02511431 | Hepatitis D | Drug: Lonafarnib|Drug: Ritonavir|Other: Placebo | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) | Phase 2 | 2015-07-21 | 2017-03-10 |
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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