奥他赛(Ortataxel) - 药物靶点：Tubulin_在研适应症：胶质母细胞瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [5]

靶点

Tubulin

作用方式

抑制剂

作用机制

微管蛋白抑制剂

治疗领域

肿瘤神经系统疾病其他疾病

在研适应症

胶质母细胞瘤

非在研适应症

晚期肾细胞癌转移性乳腺癌非霍奇金淋巴瘤+ [5]

原研机构

Indena SpA

在研机构

Indena SpA

Istituto di Ricerche Farmacologiche Mario Negri

非在研机构

Bayer AG

Theradex Systems, Inc.

Spectrum Pharmaceuticals, Inc.

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C44H57NO17

InChIKeyBWKDAMBGCPRVPI-ZQRPHVBESA-N

CAS号186348-23-2

关联

9

项与奥他赛相关的临床试验

NCT01989884

/ Completed临床2期IIT

Multicenter, Single Arm, Open-Label Phase II Trial On The Efficacy Of Ortataxel In Recurrent Glioblastoma

Italian Study On The Efficacy Of Ortataxel In Recurrent Glioblastoma

开始日期2013-11-01

申办/合作机构-

EUCTR2012-003618-15-IT

/ Not yet recruiting临床2期IIT

Multicenter, randomized, non-comparative, open-label phase II trial on the efficacy of Ortataxel and Fotemustine in recurrent glioblastoma

开始日期2013-09-17

申办/合作机构-

NCT00044525

/ Completed临床2期

An Uncontrolled Phase II Study Evaluating the Efficacy and Safety of Intravenous BAY59-8862 in Patients With Taxane-Resistant Metastatic Breast Cancer

Breast cancer is the most common form of cancer among women in developing countries, accounting for approximately one-fifth of all female cancers in the United States. Although mortality rates are declining in some countries, it remains the leading cause of death in women aged 40-55 years. The median survival for women with metastatic breast cancer is 2-3 years but there is significant variability in this population. The primary goals of treatment in patients with metastatic breast cancer are improvement or maintenance of quality of life and prolongation of survival. The taxanes, paclitaxel and docetaxel, were incorporated into the treatment of metastatic breast cancer in the 1990's. The usefulness of the taxanes is limited by the development of tumor resistance to these agents. This phase II trial with BAY59-8862 will be conducted to determine the anti-tumor efficacy of BAY59-8862 in taxane-resistant metastatic breast cancer.

开始日期2002-04-01

申办/合作机构

Bayer AG

100 项与奥他赛相关的临床结果

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100 项与奥他赛相关的转化医学

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100 项与奥他赛相关的专利（医药）

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70

项与奥他赛相关的文献（医药）

2022-10-01·Current Nutrition & Food Science

The Organic Life According to Traditional Chinese Medicine with Anticancer Approaches

作者: Shahrajabian, Mohamad Hesam ; Cheng, Qi ; Sun, Wenli

Abstract:The aim of this review was to summarize the most important traditional medinical herbs and plants that are being used in different parts of the world with a focus on a green anticancer approach. The most important impacts of medicinal plants on cancer treatments are prevention of cancer occurrence, decreased side effects, ameliorated post-operative complications, reduced post operative recurrence, reduced tumor growth, maintenance therapy, reduced symptoms and prolonged survival. Alkaloid anti-cancer compounds are pyrrolidine, pyridine, tropane, piperidine, pyrrolizidine, quinolizidine, indolizidine, isoquinoline, oxazole, isoxazole, quinazoline, quinoline, indole serine, purine, β-phenylethylamine, colchicine, benzylamine, abornin, pancratistatin and narciclasine. Anticancer phenolic compounds from plants are flavonol, flavones, kaempferol, luteolin, curcumin, apigenin, chalcone, and cafestol. Anticancer terpenoids compounds from medicinal plants are isoprene, alpha-hederin, galanal A, galanal B, carnosol, oleanane and xanthorrhizol. The most important chemical structures of anti-cancer drugs derived from plants are vincristine, vinblastine, vinorelbine, vindesine, vinflunine, paclitaxel, docetaxel, cabazitaxel, larotaxel, milataxel, ortataxel, tesetaxel, camptothecin, irinotecan, topotecan, etoposide, teniposide, harringtonine and homoharringtonine. Cancer is one of the main and primary causes of morbidity and mortality all over the world. It is a broad group of various diseases typified by unregulated cell growth. The role of plants, especially traditional herbs as a source of organic medicines has been prevalent in many societies, especially in Eastern medicinal science for thousands of years. Traditional medicinal herbs and plants which have both antiviral activity and the ability to promote immunity, would have possible inhibition ability in the initiation and promotion of virus-associated cancers. Medicinal plants should always be considered a great source of novel chemical constituents with anti-cancer effects.

2020-10-01·Cancer Letters1区 · 医学

A novel taxane, difluorovinyl-ortataxel, effectively overcomes paclitaxel-resistance in breast cancer cells

1区 · 医学

Article

作者: Liu, Daiyuan ; Farhan, Haider ; Momen Ali, Saleh Abdul ; Wang, Haihe ; Taouil, Adam ; Zhang, Xiaomei ; Wang, Changwei ; Rong, Dade ; Zhang, Mingming ; Yang, Shulan ; Wei, Yanli ; Wang, Yican ; Guo, Wanrong ; Ojima, Iwao ; Liu, Yanbin

Paclitaxel (PTX) is widely used to treat breast and ovarian cancers, but innate and acquired resistance often compromises its applications. The objective of this study was to screen new-generation taxanes for their efficiency against both PTX-sensitive and PTX-resistant breast cancer cells. From twelve compounds, difluorovinyl-ortataxel (DFV-OTX) displayed potent cytotoxic activities against both PTX-sensitive and PTX-resistant breast cancer cells. Moreover, DFV-OTX effectively induced tubulin/microtubule polymerization and G2/M phase arrest, leading to apoptosis in both PTX-sensitive and PTX-resistant cancer cells. Molecular docking analysis showed that DFV-OTX possesses unique hydrogen-bonding and van der Waals interactions with β-tubulin. LC-MS/MS analysis also demonstrated that the intracellular drug amount of DFV-OTX was lower than that of PTX, which would be critical to overcome PTX-resistance. Furthermore, DFV-OTX exhibited clear efficacy in the MCF-7R and MDA-MB-231R tumor xenografts in mouse models. Taken together, our results demonstrate that the novel taxane, DFV-OTX, can effectively overcome PTX-resistance in MDA-MB-231R cells, wherein the drug resistance was attributed to ABCB1/ABCG2 upregulation and a distinct mode of action in MCF-7R cells. Our results strongly indicate that DFV-OTX is a promising chemotherapeutic agent for the treatment of PTX-resistant cancers.

2020-06-30·Bioinformation

Molecular docking analysis of docetaxel analogues as duel lipocalin 2 inhibitors

Article

作者: Selvaraj, Jayaraman ; Vijayalakshmi, Periyasamy ; Saravanan, Radhakrishnan ; Rekha, Umapathy Vidhya ; Vishnupriya, Veeraraghavan ; Padmini, Ramakrishnan ; Perumal, Srinivasan ; Ponnulakshmi, Rajagopal

Lipocalin 2 (Lcn2, also called as neutrophil gelatinase-associated lipocalin) is a member of the lipocalin family and a known target for breast cancer. Therefore, it is of interest to use Docetaxel as a scaffold to design molecules with improved efficiency from naturally derived phytochemicals. We document 10 analogues (4Deacetyltaxol, 7Acetyltaxol, Cabazitaxel, Cephalomannine, Docetaxal, Deacetyltaxol, Docetaxeltrihydrate, Ortataxel, Paclitaxel, Taxoline) having optimal binding with Lipocalin 2 in comparison with Docetaxel. This data is highly useful for consideration in the design and development of drugs for breast cancer.

100 项与奥他赛相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	奥他赛	-	DB11669

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
胶质母细胞瘤	临床2期	-	Indena SpA	-
胶质母细胞瘤	临床2期	-	Istituto di Ricerche Farmacologiche Mario Negri	-
非小细胞肺癌	临床1期	德国	Bayer AG	2001-12-01
非小细胞肺癌	临床1期	加拿大	Bayer AG	2001-12-01
非小细胞肺癌	临床1期	意大利	Bayer AG	2001-12-01
非小细胞肺癌	临床1期	美国	Bayer AG	2001-12-01
非小细胞肺癌	临床1期	以色列	Bayer AG	2001-12-01
非霍奇金淋巴瘤	临床前	美国	Indena SpA	-
肾细胞癌	临床前	美国	Indena SpA	-
实体瘤	临床前	美国	Spectrum Pharmaceuticals, Inc.	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01989884 (Pubmed \| J Neurooncol) 人工标引	临床2期	复发性胶质母细胞瘤二线	40	ortataxel	(鏇範窪襯憲觸廠蓋繭願) = 範蓋壓窪網選簾艱鑰網鬱獵選遞簾膚獵醖醖鏇 (鹽醖繭窪窪繭壓衊壓淵 )	不佳	2019-05-01
P01.067 (EANO2018)	临床2期	复发性胶质母细胞瘤	40	Ortataxel	觸齋鑰築鹽淵製鏇願觸(遞糧製鏇構範窪遞築積) = 餘遞蓋餘選積夢繭觸鏇艱齋鏇醖膚鬱遞壓襯選 (餘衊遞獵構範築醖壓繭, 21.8 ~ 53.8) 更多	积极	2018-09-19
ASCO2008	临床2期	乳腺癌	85	Ortataxel	願製醖糧製襯鏇簾鑰獵(廠衊醖遞襯廠廠繭衊衊) = 2 deaths from liver failure 遞範餘壓壓鑰鏇構積鏇 (鹹觸齋鹽衊選築構糧憲 )	-	2008-05-20