Cilengitide是一种有效的integrin(整合素)抑制剂,作用于αvβ3受体和αvβ5受体,IC50分别为4.1 nM和79 nM,比作用于gpIIbIIIa选择性高10倍左右。
Cilengitide (EMD 121974, NSC 707544) is a selective inhibitor of αvβ3 integrin and αvβ5 integrin with IC50 of 1 nM and 140 nM, respectively.
30% propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)
1-50 μg/mL
100μg每天腹腔注射
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] Reardon DA, et al. Genes Cancer, 2011, 2(12):1159-1165.
[2] Alghisi et al (2009) The integrin antagonist cilengitide activates αvβ3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells. PLoS One 4 e4449.
[3] Monnier et al (2008) CYR61 and αvβ5 integrin cooperate to promote invasion and metastasis of tumors growing in preirradiated stroma. Cancer Res. 68 7323.
分子式 C27H40N8O7 |
分子量 588.66 |
CAS号 188968-51-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO |
Water 10 mg/mL |
Ethanol |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01118676 | Locally Advanced Non Small Cell Lung Cancer (NSCLC)* | Drug: cilengitide, radiochemotherapy | Institut Claudius Regaud|Merck KGaA | Phase 1 | 2010-03-01 | 2015-09-03 |
NCT00063973 | Childhood Central Nervous System Germ Cell Tumor|Childhood Choroid Plexus Tumor|Childhood Craniopharyngioma|Childhood Ependymoblastoma|Childhood Grade I Meningioma|Childhood Grade II Meningioma|Childhood Grade III Meningioma|Childhood High-grade Cerebellar Astrocytoma|Childhood High-grade Cerebral Astrocytoma|Childhood Infratentorial Ependymoma|Childhood Low-grade Cerebellar Astrocytoma|Childhood Low-grade Cerebral Astrocytoma|Childhood Medulloepithelioma|Childhood Mixed Glioma|Childhood Oligodendroglioma|Childhood Supratentorial Ependymoma|Recurrent Childhood Brain Stem Glioma|Recurrent Childhood Brain Tumor|Recurrent Childhood Cerebellar Astrocytoma|Recurrent Childhood Cerebral Astrocytoma|Recurrent Childhood Ependymoma|Recurrent Childhood Medulloblastoma|Recurrent Childhood Pineoblastoma|Recurrent Childhood Subependymal Giant Cell Astrocytoma|Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor|Recurrent Childhood Visual Pathway and Hypothalamic Glioma | Drug: cilengitide|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 1 | 2003-07-01 | 2013-09-27 |
NCT00679354 | Childhood High-grade Cerebellar Astrocytoma|Childhood High-grade Cerebral Astrocytoma|Recurrent Childhood Anaplastic Astrocytoma|Recurrent Childhood Anaplastic Oligoastrocytoma|Recurrent Childhood Anaplastic Oligodendroglioma|Recurrent Childhood Brain Tumor|Recurrent Childhood Cerebellar Astrocytoma|Recurrent Childhood Cerebral Astrocytoma|Recurrent Childhood Glioblastoma|Recurrent Childhood Visual Pathway and Hypothalamic Glioma | Drug: cilengitide|Other: laboratory biomarker analysis|Other: pharmacological study | National Cancer Institute (NCI) | Phase 2 | 2008-06-01 | 2014-05-05 |
NCT00121238 | Recurrent Prostate Cancer|Stage I Prostate Cancer|Stage IIA Prostate Cancer|Stage IIB Prostate Cancer|Stage III Prostate Cancer | Drug: cilengitide | National Cancer Institute (NCI) | Phase 2 | 2005-01-01 | 2016-03-28 |
NCT01165333 | Diffuse Intrinsic Pontine Glioma | Drug: Cilengitide dose escalation|Drug: Cilengitide|Radiation: Concomitant radiotherapy|Biological: Pharmacokinetic|Biological: Pharmacogenetic|Biological: Exploratory investigation | Centre Oscar Lambret | Phase 1 | 2010-08-01 | 2016-02-15 |
NCT00103337 | Recurrent Prostate Cancer|Stage IV Prostate Cancer | Drug: cilengitide|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2005-01-01 | 2013-02-27 |
NCT00089388 | Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia in Remission|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b) | Drug: cilengitide | National Cancer Institute (NCI) | Phase 2 | 2004-07-01 | 2013-01-23 |
NCT01782976 | Glioblastoma | Drug: Cilengitide|Drug: Bevacizumab|Behavioral: Questionnaire | M.D. Anderson Cancer Center|Brain Tumor Trials Collaborative|EMD Serono | Phase 2 | 2013-06-01 | 2013-09-03 |
NCT00979862 | Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Neoplasm | Drug: Cediranib Maleate|Drug: Cilengitide|Other: Laboratory Biomarker Analysis | National Cancer Institute (NCI) | Phase 1 | 2010-03-01 | 2015-04-14 |
NCT01124240 | Newly Diagnosed Non Methylated Glioblastoma Multiforme Grade 4 | Drug: Cilengitide | Northern Sydney and Central Coast Area Health Service|Merck KGaA | Phase 2 | 2009-11-01 | 2011-07-25 |
NCT01276496 | Adult Solid Neoplasm|Estrogen Receptor Negative|HER2/Neu Negative|Male Breast Carcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma | Drug: Cilengitide|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Other: Pharmacological Study | National Cancer Institute (NCI) | Phase 1 | 2010-12-01 | 2016-03-14 |
NCT00689221 | Glioblastoma | Drug: Cilengitide|Drug: Temozolomide|Radiation: Radiotherapy | EMD Serono|European Organisation for Research and Treatment of Cancer - EORTC|Merck KGaA | Phase 3 | 2008-09-01 | 2014-10-28 |
NCT01558687 | Supratentorial Newly Diagnosed Inoperable Gliobastoma | Drug: Drug (including placebo)|Other: Standard therapy | Merck KGaA | Phase 1 | 2012-08-01 | 2014-02-03 |
NCT00813943 | Glioblastoma | Drug: Cilengitide (2-times weekly)|Drug: cilengitide (5-times weekly)|Drug: Temozolomide|Radiation: Radiotherapy | EMD Serono|Merck KGaA | Phase 2 | 2009-03-01 | 2017-01-12 |
NCT00082875 | Stage III Melanoma|Stage IV Melanoma | Drug: cilengitide|Other: pharmacological study|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2004-03-01 | 2013-06-04 |
NCT00077155 | AIDS-related Peripheral/Systemic Lymphoma|AIDS-related Primary CNS Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma|Stage III Adult Burkitt Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Mixed Cell Lymphoma|Stage III Adult Diffuse Small Cleaved Cell Lymphoma|Stage III Adult Hodgkin Lymphoma|Stage III Adult Immunoblastic Large Cell Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Cutaneous T-cell Non-Hodgkin Lymphoma|Stage III Grade 1 Follicular Lymphoma|Stage III Grade 2 Follicular Lymphoma|Stage III Grade 3 Follicular Lymphoma|Stage III Mantle Cell Lymphoma|Stage III Marginal Zone Lymphoma|Stage III Mycosis Fungoides/Sezary Syndrome|Stage III Small Lymphocytic Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Mycosis Fungoides/Sezary Syndrome|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific | Drug: cilengitide | National Cancer Institute (NCI) | Phase 1 | 2003-12-01 | 2013-01-23 |
NCT01122888 | Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Solid Neoplasm|Recurrent Adult Brain Neoplasm | Drug: Cilengitide|Other: Clinical Observation|Other: Laboratory Biomarker Analysis | National Cancer Institute (NCI) | Phase 1 | 2009-12-01 | 2015-04-27 |
NCT01044225 | Glioblastoma | Drug: Cetuximab|Drug: Cilengitide EMD 121974 | Bart Neyns|Universitair Ziekenhuis Brussel | Phase 2 | 2009-09-01 | 2012-03-21 |
NCT00705016 | Squamous Cell Cancer | Drug: Cilengitide 2000 mg once weekly|Drug: Cilengitide 2000 mg twice weekly|Drug: Cetuximab|Drug: 5-fluorouracil (5-FU)|Drug: Cisplatin | Merck KGaA | Phase 1|Phase 2 | 2008-10-01 | 2014-03-28 |
NCT00884598 | Brain and Central Nervous System Tumors|Lung Cancer | Drug: cilengitide|Other: pharmacological study|Radiation: radiation therapy | Universit盲tsmedizin Mannheim|Heidelberg University | Phase 1 | 2008-12-01 | 2010-04-27 |
NCT00112866 | Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor | Drug: cilengitide|Procedure: therapeutic conventional surgery|Other: pharmacological study|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2005-01-01 | 2013-10-25 |
NCT01504165 | Renal Impairment | Drug: cilengitide 2000mg|Drug: cilengitide 2000mg|Drug: cilengitide 2000mg|Drug: cilengitide 1000mg|Drug: cilengitide > 1000mg and up to 2000mg | Merck KGaA | Phase 1 | 2012-01-01 | 2014-02-03 |
NCT00842712 | Carcinoma, Non-Small-Cell Lung | Drug: Cilengitide|Drug: Cilengitide|Drug: Cetuximab|Drug: Cisplatin|Drug: Cisplatin|Drug: Gemcitabine|Drug: Vinorelbine|Drug: Cilengitide|Drug: Cilengitide|Drug: Cetuximab|Drug: Chemotherapy | Merck KGaA | Phase 2 | 2009-02-01 | 2017-01-12 |
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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