阿霉素（INNO-206）的白蛋白结合前药与阿霉素联合治疗在卵巢A2780异种移植模型中实现了完全缓解并提高了耐受性。 - Suppr

Combination therapy with the albumin-binding prodrug of doxorubicin (INNO-206) and doxorubicin achieves complete remissions and improves tolerability in an ovarian A2780 xenograft model.

作者信息

Kratz Felix, Fichtner Iduna, Graeser Ralph

机构信息

Tumor Biology Center, Department of Medical Oncology, Clinical Research, Breisacher Strasse 117, 79106 Freiburg, Germany.

出版信息

Invest New Drugs. 2012 Aug;30(4):1743-9. doi: 10.1007/s10637-011-9686-5. Epub 2011 May 18.

DOI:10.1007/s10637-011-9686-5

PMID:21590366

Abstract

摘要

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Combination therapy with the albumin-binding prodrug of doxorubicin (INNO-206) and doxorubicin achieves complete remissions and improves tolerability in an ovarian A2780 xenograft model.阿霉素（INNO-206）的白蛋白结合前药与阿霉素联合治疗在卵巢A2780异种移植模型中实现了完全缓解并提高了耐受性。

Invest New Drugs. 2012 Aug;30(4):1743-9. doi: 10.1007/s10637-011-9686-5. Epub 2011 May 18.

Evaluation of combination therapy schedules of doxorubicin and an acid-sensitive albumin-binding prodrug of doxorubicin in the MIA PaCa-2 pancreatic xenograft model.多柔比星与多柔比星酸敏白蛋白结合前药联合治疗方案在 MIA PaCa-2 胰腺异种移植模型中的评价。

Int J Pharm. 2013 Jan 30;441(1-2):499-506. doi: 10.1016/j.ijpharm.2012.11.003. Epub 2012 Nov 10.

INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model.INNO-206（多柔比星的 6-马来酰亚胺己酰肼衍生物）在不同的肿瘤异种移植模型和原位胰腺癌模型中显示出比多柔比星更高的抗肿瘤疗效。

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DOXO-EMCH (INNO-206): the first albumin-binding prodrug of doxorubicin to enter clinical trials.多柔比星-乙磺半胱氨酸（INNO-206）：首个进入临床试验阶段的多柔比星白蛋白结合型前体药物。

Expert Opin Investig Drugs. 2007 Jun;16(6):855-66. doi: 10.1517/13543784.16.6.855.

Pronounced antitumor efficacy of doxorubicin when given as the prodrug DOX-GA3 in combination with a monoclonal antibody beta-glucuronidase conjugate.当多柔比星作为前药DOX-GA3与单克隆抗体β-葡萄糖醛酸酶缀合物联合使用时，具有显著的抗肿瘤功效。

Int J Cancer. 2001 Feb 15;91(4):550-4. doi: 10.1002/1097-0215(200002)9999:9999<::aid-ijc1075>3.0.co;2-l.

Synthesis and biological evaluation of an albumin-binding prodrug of doxorubicin that is cleaved by prostate-specific antigen (PSA) in a PSA-positive orthotopic prostate carcinoma model (LNCaP).在前列腺特异性抗原（PSA）阳性原位前列腺癌模型（LNCaP）中被PSA裂解的阿霉素白蛋白结合前药的合成及生物学评价

Int J Cancer. 2008 Mar 1;122(5):1145-54. doi: 10.1002/ijc.23050.

Development of albumin-binding doxorubicin prodrugs that are cleaved by prostate-specific antigen.由前列腺特异性抗原裂解的白蛋白结合阿霉素前药的开发。

Arch Pharm (Weinheim). 2005 Oct;338(10):462-72. doi: 10.1002/ardp.200500130.

Albumin-binding prodrugs of camptothecin and doxorubicin with an Ala-Leu-Ala-Leu-linker that are cleaved by cathepsin B: synthesis and antitumor efficacy.具有丙氨酸-亮氨酸-丙氨酸-亮氨酸连接子、可被组织蛋白酶B裂解的喜树碱和阿霉素白蛋白结合前药：合成与抗肿瘤疗效

Bioconjug Chem. 2007 May-Jun;18(3):702-16. doi: 10.1021/bc0602735. Epub 2007 Mar 23.

The anti-tumour effects of the prodrugs N-l-leucyl-doxorubicin and vinblastine-isoleucinate in human ovarian cancer xenografts.前体药物N-1-亮氨酰阿霉素和长春碱异亮氨酸酯对人卵巢癌异种移植瘤的抗肿瘤作用。

Br J Cancer. 1992 Dec;66(6):1044-7. doi: 10.1038/bjc.1992.407.

Determination of the optimal combination chemotherapy regimen for treatment of platinum-resistant ovarian cancer in nude mouse model.在裸鼠模型中确定治疗铂耐药卵巢癌的最佳联合化疗方案。

J Oncol Pharm Pract. 2007 Mar;13(1):39-45. doi: 10.1177/1078155207077948.

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Morphine modulates doxorubicin uptake and improves efficacy of chemotherapy in an intracranial xenograft model of human glioblastoma.吗啡调节阿霉素摄取并提高人胶质母细胞瘤颅内异种移植模型中的化疗疗效。

Am J Cancer Res. 2016 Feb 15;6(3):639-48. eCollection 2016.

Simple bioconjugate chemistry serves great clinical advances: albumin as a versatile platform for diagnosis and precision therapy.简单的生物共轭化学推动了重大的临床进展：白蛋白作为诊断和精准治疗的通用平台。

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Therapeutic efficacy of aldoxorubicin in an intracranial xenograft mouse model of human glioblastoma.阿霉素在人胶质母细胞瘤颅内异种移植小鼠模型中的治疗效果。

Neoplasia. 2014 Oct 23;16(10):874-82. doi: 10.1016/j.neo.2014.08.015. eCollection 2014 Oct.

Anti-cancer effects of novel doxorubicin prodrug PDOX in MCF-7 breast cancer cells.新型阿霉素前药PDOX对MCF-7乳腺癌细胞的抗癌作用。

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本文引用的文献

Enhanced albumin uptake by rat tumors.大鼠肿瘤对白蛋白摄取的增强。

Int J Oncol. 1997 Sep;11(3):497-507. doi: 10.3892/ijo.11.3.497.

The EPR effect: Unique features of tumor blood vessels for drug delivery, factors involved, and limitations and augmentation of the effect.EPR 效应：用于药物输送的肿瘤血管的独特特征、涉及的因素以及该效应的局限性和增强。

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Drug combination studies and their synergy quantification using the Chou-Talalay method.药物联合研究及其协同作用的定量分析——Chou-Talalay 法

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Albumin as a drug carrier: design of prodrugs, drug conjugates and nanoparticles.白蛋白作为药物载体：前药、药物偶联物及纳米颗粒的设计

J Control Release. 2008 Dec 18;132(3):171-83. doi: 10.1016/j.jconrel.2008.05.010. Epub 2008 May 17.

Phase I and pharmacokinetic study of the (6-maleimidocaproyl)hydrazone derivative of doxorubicin.阿霉素（6-马来酰亚胺己酰基）腙衍生物的I期及药代动力学研究

Clin Cancer Res. 2007 Aug 15;13(16):4858-66. doi: 10.1158/1078-0432.CCR-06-2776.

Expert Opin Investig Drugs. 2007 Jun;16(6):855-66. doi: 10.1517/13543784.16.6.855.

Acute and repeat-dose toxicity studies of the (6-maleimidocaproyl)hydrazone derivative of doxorubicin (DOXO-EMCH), an albumin-binding prodrug of the anticancer agent doxorubicin.阿霉素（DOXO-EMCH）的（6-马来酰亚胺己酰基）腙衍生物的急性和重复给药毒性研究，阿霉素是一种白蛋白结合型抗癌前药。

Hum Exp Toxicol. 2007 Jan;26(1):19-35. doi: 10.1177/0960327107073825.

Imaging tumors with an albumin-binding Fab, a novel tumor-targeting agent.使用一种新型肿瘤靶向剂——白蛋白结合Fab片段对肿瘤进行成像。

Cancer Res. 2007 Jan 1;67(1):254-61. doi: 10.1158/0008-5472.CAN-06-2531.

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Combination therapy with the albumin-binding prodrug of doxorubicin (INNO-206) and doxorubicin achieves complete remissions and improves tolerability in an ovarian A2780 xenograft model.

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