Delving into the Latest Updates on 13-Deoxyadriamycin hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

DNA x Top II

Action

inhibitors

Mechanism

DNA inhibitors(DNA inhibitors), Top II inhibitors(Topoisomerase II inhibitors)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Metastatic breast cancerNeoplasm Metastasis

Originator Organization

Gem Pharmaceuticals LLC

Active Organization-

Inactive Organization

Gem Pharmaceuticals LLC

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC27H31NO10

InChIKeyRGVRUQHYQSORBY-JIGXQNLBSA-N

CAS Registry628290-43-7

View All Structures (2)

The purpose of this early Phase II multicenter trial is to determine the objective clinical response to GPX-100, an anthracycline similar to doxorubicin, in up to 40 patients with newly diagnosed metastatic breast cancer. GPX-100 is unique among anthracyclines because it is not converted to doxorubicinol during metabolism in the body. This metabolite has been shown to be a major cause of damage to the heart (cardiotoxicity) in laboratory studies. Eligible patients who are enrolled in this study will receive GPX-100 as a single agent at the beginning of as many as 8 three week long cycles of chemotherapy. Objective measurements of tumor response will be made by computed tomography (CT) scans.

Start Date01 Mar 2005

Sponsor / Collaborator

Gem Pharmaceuticals LLC

NCT00003403

/ CompletedPhase 1

Phase I Safety and Efficacy Study of an Intravenous Formulation of the Anthracycline Analog, GPX-100, in the Treatment of Metastatic Breast Cancer

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase I trial to study the effectiveness of GPX-100 in treating patients who have solid tumors.

Start Date01 Aug 1999

Sponsor / Collaborator

Gem Pharmaceuticals LLC

100 Clinical Results associated with 13-Deoxyadriamycin hydrochloride

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100 Translational Medicine associated with 13-Deoxyadriamycin hydrochloride

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100 Patents (Medical) associated with 13-Deoxyadriamycin hydrochloride

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7

Literatures (Medical) associated with 13-Deoxyadriamycin hydrochloride

22 Aug 2024·Journal of Medicinal Chemistry

Novel N,N-Dimethyl-idarubicin Analogues Are Effective Cytotoxic Agents for ABCB1-Overexpressing, Doxorubicin-Resistant Cells

Article

Author: van Gelder, Merle A. ; Berlin, Ilana ; Wander, Dennis P. A. ; van der Zanden, Sabina Y. ; Overkleeft, Hermen S. ; Neefjes, Jacques J. C. ; Li, Yufeng

Anthracyclines comprise one of the most effective anticancer drug classes. Doxorubicin, daunorubicin, epirubicin, and idarubicin have been in clinical use for decades, but their application remains complicated by treatment-related toxicities and drug resistance. We previously demonstrated that the combination of DNA damage and histone eviction exerted by doxorubicin drives its associated adverse effects. However, whether the same properties dictate drug resistance is unclear. In the present study, we evaluate a library of 40 anthracyclines on their cytotoxicity, intracellular uptake, and subcellular localization in K562 wildtype versus ABCB1-transporter-overexpressing, doxorubicin-resistant cells. We identify several highly potent cytotoxic anthracyclines. Among these, N,N-dimethyl-idarubicin and anthracycline (composed of the idarubicin aglycon and the aclarubicin trisaccharide) stand out, due to their histone eviction-mediated cytotoxicity toward doxorubicin-resistant cells. Our findings thus uncover understudied anthracycline variants warranting further investigation in the quest for safer and more effective anticancer agents that circumvent cellular export by ABCB1.

01 Jun 2021·Journal of Pure and Applied Microbiology

Regulatory Action of all trans Retinoic Acid on Metastasis Induced lung Cell Metabolic Changes during Implantation of B16F10 Cancer Cells in C57BL6 Mice

Author: Saranya, S. ; Peardon, Rohit ; Wilson, D. David ; Grace, V. M. Berlin

The changes that occur during metastasis lodging is under intense research now to develop preventive new drugs to fight against the deadly metastasis. The molecular drug, all trans Retinoic Acid (ATRA) has regulatory effects on signal mediated metabolism. In this study, we have analyzed the metastasis facilitating metabolic changes in mice lung when a highly metastatic melanoma cell line (B16F10) having potency to lodge in lung was implanted via tail vein injection into C57BL/6 mice (1×106 cells/ml in PBS). One group of implanted mice were treated with 0.60 mg of ATRA per Kg body weight daily for 21 days. The alteration of protein, enzymatic and non-enzymatic antioxidants (SOD, Catalase, GPX, GSH) levels and the lipid profile with cholesterol level were evaluated in the lung tissues. The ATRA treatment caused 62.16% inhibition on metastatic nodule formation. Compared to normal mice, the cancer control mice showed an increased (p≤ 0.01**) total protein, LPO and NO and a decreased antioxidant. In ATRA treated group, all these levels were reverted to near normal levels with a high significance (p≤ 0.01**) difference from untreated cancer mice. The lipid profile and cholesterol level also were altered in cancer and were normalized in ATRA treated group with high significance (p≤ 0.01**). All these results implies that the metabolic changes induced in the lung tissue during metastatic lodging of melanoma cells were prevented and regularized by the ATRA treatment in vivo which give a scope of anti-metastatic therapy using ATRA.

01 Nov 2017·BiomaterialsQ1 · ENGINEERING & TECHNOLOGY

Poly(2-ethyl-2-oxazoline) conjugates with doxorubicin for cancer therapy: In vitro and in vivo evaluation and direct comparison to poly[N-(2-hydroxypropyl)methacrylamide] analogues

Q1 · ENGINEERING & TECHNOLOGY

Article

Author: Verbraeken, Bart ; Hocherl, Anita ; Janouskova, Olga ; Vergaelen, Maarten ; Sedlacek, Ondrej ; Monnery, Bryn D ; Hruby, Martin ; Hoogenboom, Richard ; Mattova, Jana ; Panek, Jiri ; Kucka, Jan ; Zadinova, Marie

We designed and synthesized a new delivery system for the anticancer drug doxorubicin based on a biocompatible hydrophilic poly(2-ethyl-2-oxazoline) (PEtOx) carrier with linear architecture and narrow molar mass distribution. The drug is connected to the polymer backbone via an acid-sensitive hydrazone linker, which allows its triggered release in the tumor. The in vitro studies demonstrate successful cellular uptake of conjugates followed by release of the cytostatic cargo. In vivo experiments in EL4 lymphoma bearing mice revealed prolonged blood circulation, increased tumor accumulation and enhanced antitumor efficacy of the PEtOx conjugate having higher molecular weight (40 kDa) compared to the lower molecular weight (20 kDa) polymer. Finally, the in vitro and in vivo anti-cancer properties of the prepared PEtOx conjugates were critically compared with those of the analogous system based on the well-established PHPMA carrier. Despite the relatively slower intracellular uptake of PEtOx conjugates, resulting also in their lower cytotoxicity, there are no substantial differences in in vivo biodistribution and anti-cancer efficacy of both classes of polymer-Dox conjugates. Considering the synthetic advantages of poly(2-alkyl-2-oxazoline)s, the presented study demonstrates their potential as a versatile alternative to well-known PEO- or PHPMA-based materials for construction of drug delivery systems.

100 Deals associated with 13-Deoxyadriamycin hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05706

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Metastatic breast cancer	Phase 2	United States	Gem Pharmaceuticals LLC	01 Mar 2005
Metastatic breast cancer	Phase 2	Bulgaria	Gem Pharmaceuticals LLC	01 Mar 2005
Neoplasm Metastasis	Phase 2	United States	Gem Pharmaceuticals LLC	01 Mar 2005
Neoplasm Metastasis	Phase 2	Bulgaria	Gem Pharmaceuticals LLC	01 Mar 2005