Delving into the Latest Updates on Ortataxel with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [5]

Target

Tubulin

Action

inhibitors

Mechanism

Tubulin inhibitors

Therapeutic Areas

NeoplasmsNervous System DiseasesOther Diseases

Active Indication

Glioblastoma

Inactive Indication

Advanced Renal Cell CarcinomaMetastatic breast cancerNon-Hodgkin Lymphoma+ [5]

Originator Organization

Indena SpA

Active Organization

Indena SpA

Istituto di Ricerche Farmacologiche Mario Negri

Inactive Organization

Bayer AG

Theradex Systems, Inc.

Spectrum Pharmaceuticals, Inc.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC44H57NO17

InChIKeyBWKDAMBGCPRVPI-ZQRPHVBESA-N

CAS Registry186348-23-2

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.

Start Date01 Apr 2002

Sponsor / Collaborator

Bayer AG

100 Clinical Results associated with Ortataxel

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100 Translational Medicine associated with Ortataxel

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100 Patents (Medical) associated with Ortataxel

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70

Literatures (Medical) associated with Ortataxel

01 Oct 2022·Current Nutrition & Food Science

The Organic Life According to Traditional Chinese Medicine with Anticancer Approaches

Author: 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.

01 Oct 2020·Cancer LettersQ1 · MEDICINE

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

Q1 · MEDICINE

Article

Author: 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.

30 Jun 2020·Bioinformation

Molecular docking analysis of docetaxel analogues as duel lipocalin 2 inhibitors

Article

Author: 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 Deals associated with Ortataxel

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Ortataxel	-	DB11669

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Glioblastoma	Phase 2	-	Indena SpA	-
Glioblastoma	Phase 2	-	Istituto di Ricerche Farmacologiche Mario Negri	-
Non-Small Cell Lung Cancer	Phase 1	Germany	Bayer AG	01 Dec 2001
Non-Small Cell Lung Cancer	Phase 1	Canada	Bayer AG	01 Dec 2001
Non-Small Cell Lung Cancer	Phase 1	Italy	Bayer AG	01 Dec 2001
Non-Small Cell Lung Cancer	Phase 1	United States	Bayer AG	01 Dec 2001
Non-Small Cell Lung Cancer	Phase 1	Israel	Bayer AG	01 Dec 2001
Non-Hodgkin Lymphoma	Preclinical	United States	Indena SpA	-
Renal Cell Carcinoma	Preclinical	United States	Indena SpA	-
Solid tumor	Preclinical	United States	Spectrum Pharmaceuticals, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01989884 (Pubmed \| J Neurooncol) Manual	Phase 2	Recurrent Glioblastoma Second line	40	ortataxel	(jblxgqxxzu) = lydlrsttpb qtpvlsgatj (prodkwtcxb )	Negative	01 May 2019
P01.067 (EANO2018)	Phase 2	Recurrent Glioblastoma	40	Ortataxel	chxdhwmmoe(ccvshrynlz) = okdykoayeu sadgjrxmoz (buagzgqfof, 21.8 - 53.8) View more	Positive	19 Sep 2018
ASCO2008	Phase 2	Breast Cancer	85	Ortataxel	jpafihvvuo(epkeqrobjs) = 2 deaths from liver failure zfbgyogclk (dpoxlfzpgo )	-	20 May 2008