CN104857534A - 叶酸盐靶向的诊断和治疗 - Google Patents
叶酸盐靶向的诊断和治疗 Download PDFInfo
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- CN104857534A CN104857534A CN201510160314.2A CN201510160314A CN104857534A CN 104857534 A CN104857534 A CN 104857534A CN 201510160314 A CN201510160314 A CN 201510160314A CN 104857534 A CN104857534 A CN 104857534A
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- G01N33/60—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances involving radioactive labelled substances
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- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
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Cited By (1)
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| CN110678204A (zh) * | 2016-03-29 | 2020-01-10 | 恩多塞特公司 | 用于靶向肿瘤相关巨噬细胞的叶酸缀合物 |
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| CA2696627C (en) | 2007-08-17 | 2016-09-27 | Purdue Research Foundation | Psma binding ligand-linker conjugates and methods for using |
| US9951324B2 (en) | 2010-02-25 | 2018-04-24 | Purdue Research Foundation | PSMA binding ligand-linker conjugates and methods for using |
| AU2011325982C1 (en) | 2010-11-12 | 2015-08-20 | Endocyte, Inc. | Methods of treating cancer |
| BR112013026352A2 (pt) * | 2011-04-12 | 2016-07-26 | Endocyte Inc | composição farmacêutica sólida |
| KR102354613B1 (ko) | 2012-11-15 | 2022-01-21 | 엔도사이트, 인코포레이티드 | Psma 발현 세포에 의해 야기되는 질병을 치료하기 위한 컨쥬게이트 |
| US20140154702A1 (en) * | 2012-11-30 | 2014-06-05 | Endocyte, Inc. | Methods For Treating Cancer Using Combination Therapies |
| WO2015055796A1 (en) | 2013-10-16 | 2015-04-23 | Université Libre de Bruxelles | Formulations useful in the treatment of proliferative diseases affecting the respiratory tract |
| HUE066137T2 (hu) | 2013-10-18 | 2024-07-28 | Novartis Ag | A prosztata-specifikus membrán antigén (PSMA) jelzett inhibitorai, alkalmazásuk képalkotásban és gyógyszerkészítmények prosztatarák kezelésére |
| JP6464166B2 (ja) | 2013-11-14 | 2019-02-06 | エンドサイト・インコーポレイテッドEndocyte, Inc. | 陽電子放出断層撮影用の化合物 |
| WO2015077303A1 (en) | 2013-11-19 | 2015-05-28 | Purdue Research Foundation | Patient selection method for inflammation |
| US10188759B2 (en) | 2015-01-07 | 2019-01-29 | Endocyte, Inc. | Conjugates for imaging |
| CA2973380A1 (en) * | 2015-01-11 | 2016-07-14 | Endocyte, Inc. | Cancer imaging agent |
| IL237525A (en) | 2015-03-03 | 2017-05-29 | Shalom Eli | Method for labeling a prostate-specific membrane antigen with a radioactive isotope |
| US10940112B2 (en) | 2016-05-04 | 2021-03-09 | L.E.A.F. Holdings Group Llc | Targeted liposomal gemcitabine compositions and methods thereof |
| US20190216935A1 (en) * | 2016-05-25 | 2019-07-18 | Purdue Research Foundation | Method of treating cancer by targeting myeloid-derived suppressor cells |
| CA3097381A1 (en) | 2018-04-17 | 2019-10-24 | Endocyte, Inc. | Methods of treating cancer |
| CN120097930A (zh) | 2019-05-20 | 2025-06-06 | 因多塞特股份有限公司 | 制备psma缀合物的方法 |
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| AR042942A1 (es) * | 2003-01-27 | 2005-07-06 | Endocyte Inc | Conjugados de administracion de drogas de union de receptores de vitaminas |
| CN101111267B (zh) * | 2004-12-21 | 2012-12-05 | 尼克塔治疗公司 | 稳定的聚合物巯基试剂 |
| JP5289935B2 (ja) * | 2005-03-16 | 2013-09-11 | エンドサイト,インコーポレイテッド | プテロイン酸およびその結合体の合成と精製 |
| WO2006105141A1 (en) * | 2005-03-30 | 2006-10-05 | Purdue Research Foundation | Method for cancer prognosis using cellular folate vitamin receptor quantification |
| JP2006316040A (ja) * | 2005-05-13 | 2006-11-24 | Genentech Inc | Herceptin(登録商標)補助療法 |
| MX2009004555A (es) * | 2006-10-25 | 2009-05-11 | Schering Corp | Metodos de tratamiento de cancer de ovario. |
| EP3569251A1 (en) * | 2007-06-25 | 2019-11-20 | Endocyte, Inc. | Conjugates containing hydrophilic spacer linkers |
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| WO2006071754A2 (en) * | 2004-12-23 | 2006-07-06 | Purdue Research Foundation | Positron emission tomography imaging method |
Non-Patent Citations (5)
| Title |
|---|
| CHRISTOPHER P. LEAMON ET AL: ""Comparative preclinical activity of the folate-targeted Vinca alkaloid conjugates EC140 and EC145"", 《INT. J. CANCER》 * |
| ENDOCYTE ET AL: "Preclinical Evaluation of EC145, a Folate-Vinca Alkaloid Conjugate", 《CANCER RES》 * |
| LEVI S. DOWNS JR ET AL: "A Prospective Randomized Trial of Thalidomide With Topotecan Compared With Topotecan Alone in Women With Recurrent Epithelial Ovarian Carcinoma", 《CANCER》 * |
| RONALD E. FISHER ET AL: "Exploratory Study of 99mTc-EC20 Imaging for Identifying Patients with Folate Receptor–Positive Solid Tumors", 《J NUCL MED》 * |
| TIMOTHY A. YAP ET AL: "Beyond chemotherapy: targeted therapies in ovarian cancer", 《CANCER》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110678204A (zh) * | 2016-03-29 | 2020-01-10 | 恩多塞特公司 | 用于靶向肿瘤相关巨噬细胞的叶酸缀合物 |
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| US20120128587A1 (en) | 2012-05-24 |
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