Ribociclib是一种可口服的,高度特异性CDK4/6抑制剂。
LEE011 is a novel, orally available, potent and selective CDK4/6 inhibitor.
10 μM
~200mg/kg 每天口服
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] Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182.
分子式 C23H30N8O |
分子量 434.54 |
CAS号 1211441-98-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 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 |
NCT02754011 | Breast Cancer | Drug: Combination of ribociclib + capecitabine | UNICANCER|Novartis | Phase 1 | 2017-01-01 | 2017-02-09 |
NCT02933736 | Glioblastoma Multiforme|Meningioma | Drug: Ribociclib | St. Joseph's Hospital and Medical Center, Phoenix|Novartis | Early Phase 1 | 2016-10-01 | 2017-01-04 |
NCT02345824 | Glioblastoma|Glioma | Drug: Ribociclib | University of Virginia|Novartis Pharmaceuticals | Phase 1 | 2016-03-01 | 2016-10-27 |
NCT02571829 | Liposarcoma|Soft Tissue Sarcoma | Drug: ribociclib | Hadassah Medical Organization | Phase 2 | 2016-05-01 | 2016-11-22 |
NCT02712723 | Breast Cancer | Drug: Letrozole|Drug: Ribociclib|Drug: Placebo | University of Kansas Medical Center|Novartis Pharmaceuticals | Phase 2 | 2016-02-01 | 2017-02-17 |
NCT03008408 | Malignant Neoplasms of Female Genital Organs|Endometrial Carcinoma | Drug: Ribociclib|Drug: Everolimus|Drug: Letrozole | M.D. Anderson Cancer Center|Novartis | Phase 2 | 2017-04-01 | 2017-02-14 |
NCT02934568 | Continued Access to Study Treatment(s)|Cancers With a Mass, Bulky Tumor, Nodule, Lump, Advanced Cancer, Advanced Solid Tumors, Advanced Solid Malignancies | Drug: LEE011 | Novartis Pharmaceuticals|Novartis | Phase 2 | 2016-12-15 | 2017-02-27 |
NCT03056833 | Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Carcinoma | Drug: ribociclib|Drug: Paclitaxel|Drug: Carboplatin | University of Michigan Cancer Center | Phase 1 | 2017-05-01 | 2017-03-16 |
NCT02555189 | Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Prostate Carcinoma Metastatic in the Bone|Stage IV Prostate Cancer | Drug: Enzalutamide|Drug: Ribociclib | Sidney Kimmel Cancer Center at Thomas Jefferson University|Novartis|Prostate Cancer Clinical Trials Consortium|Thomas Jefferson University | Phase 1|Phase 2 | 2015-12-01 | 2016-12-20 |
NCT03050398 | Breast Cancer | Drug: Ribociclib|Drug: letrozole | Novartis Pharmaceuticals|Novartis | Phase 3 | 2017-05-15 | 2017-03-21 |
NCT03078751 | Breast Cancer | Drug: Ribociclib|Drug: Placebo|Drug: Adjuvant endocrine therapy | Novartis Pharmaceuticals|Novartis | Phase 3 | 2017-05-11 | 2017-03-08 |
NCT03081234 | Breast Cancer | Drug: Ribociclib|Drug: Placebo|Drug: Adjuvant endocrine therapy | Novartis Pharmaceuticals|Novartis | Phase 3 | 2017-05-25 | 2017-03-10 |
NCT03009201 | Metastatic Angiosarcoma|Metastatic Epithelioid Sarcoma|Metastatic Fibrosarcoma|Metastatic Leiomyosarcoma|Metastatic Liposarcoma|Metastatic Malignant Peripheral Nerve Sheath Tumor|Metastatic Synovial Sarcoma|Metastatic Undifferentiated Pleomorphic Sarcoma|Myxofibrosarcoma|Pleomorphic Rhabdomyosarcoma|Stage III Soft Tissue Sarcoma|Stage IV Soft Tissue Sarcoma|Undifferentiated (Embryonal) Sarcoma | Drug: Doxorubicin Hydrochloride|Drug: Ribociclib | OHSU Knight Cancer Institute|National Cancer Institute (NCI) | Phase 1 | 2017-01-01 | 2016-12-30 |
NCT02414724 | Lymphoma|Solid Neoplasm | Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Ribociclib | Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis | Phase 1 | 2015-05-01 | 2016-09-09 |
NCT03090165 | Triple Negative Breast Cancer | Drug: ribociclib|Drug: ribociclib|Drug: Bicalutamide | Ruth O'Regan, M.D.|Novartis|Big Ten Cancer Research Consortium | Phase 1|Phase 2 | 2017-03-01 | 2017-03-23 |
NCT02607124 | High Grade Glioma|Diffuse Intrinsic Pontine Glioma|Bithalamic High Grade Glioma | Drug: Ribociclib | Children's Hospital Medical Center, Cincinnati|Novartis | Phase 1|Phase 2 | 2016-04-01 | 2017-02-28 |
NCT02586675 | Breast Cancer|Breast Cancer - Female|Breast Cancer - Male | Drug: Tamoxifen|Drug: Ribociclib|Drug: Goserelin | H. Lee Moffitt Cancer Center and Research Institute|Novartis | Phase 1 | 2016-02-01 | 2016-12-27 |
NCT02657928 | Estrogen Receptor Positive|Postmenopausal|RB1 Positive|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma | Other: Laboratory Biomarker Analysis|Drug: Letrozole|Drug: Ribociclib | Mayo Clinic|National Cancer Institute (NCI) | Phase 2 | 2016-07-01 | 2017-01-26 |
NCT02732119 | Breast Cancer | Drug: Ribociclib|Drug: Everolimus|Drug: Exemestane | Novartis Pharmaceuticals|Novartis | Phase 1|Phase 2 | 2016-06-14 | 2017-02-23 |
NCT02632045 | Metastatic Breast Cancer|Breast Carcinoma | Drug: LEE-011|Drug: Fulvestrant|Drug: Placebo | Kevin Kalinsky|Novartis Pharmaceuticals|Columbia University | Phase 2 | 2016-03-01 | 2017-03-03 |
NCT02420691 | Gastrointestinal Cancer | Drug: LEE011 | M.D. Anderson Cancer Center|Novartis | Phase 2 | 2015-08-01 | 2016-09-19 |
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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