Delving into the Latest Updates on Demethylcantharidin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Mechanism-

Therapeutic Areas

NeoplasmsDigestive System DisordersRespiratory Diseases+ [1]

Active Indication

Breast CancerEsophageal CarcinomaLung Cancer

Inactive Indication-

Originator Organization-

Active Organization

Shenyang Pharmaceutical University

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC8H8O4

InChIKeyJAABVEXCGCXWRR-FBXFSONDSA-N

CAS Registry29745-04-8

主要目的：观察去甲斑蝥素脂质微球注射液在人体中的安全性，确定其剂量限制性毒性（DLT）、最大耐受剂量（MTD），为后期临床研究推荐剂量。次要目的：评价去甲斑蝥素脂质微球注射液在人体的药代动力学特征，并与已上市的注射用去甲斑蝥酸钠进行对比，探讨脂质微球剂型所引起的药代及初步安全性变化。

[Translation]

The primary objective is to observe the safety of norcantharidin lipid microsphere injection in humans, determine its dose-limiting toxicity (DLT) and maximum tolerated dose (MTD), and recommend the dose for later clinical studies. The secondary objective is to evaluate the pharmacokinetic characteristics of norcantharidin lipid microsphere injection in humans, and compare it with the marketed norcantharidin sodium for injection to explore the pharmacokinetic and preliminary safety changes caused by the lipid microsphere dosage form.

Start Date22 Sep 2020

Sponsor / Collaborator

Shenyang Pharmaceutical University

NCT04673396 / Unknown statusPhase 1

Phase I Clinical Study for Evaluation of Pharmacokinetic, Safety, Tolerance of Norcantharidin Lipid Microsphere for Injection in Patients With Solid Tumor

This study was designed as a single-center, open, non-randomized trial.

Start Date22 Sep 2020

Sponsor / Collaborator

Beijing Nuokangda Pharmaceutical Technology Co., Ltd.

100 Clinical Results associated with Demethylcantharidin

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100 Translational Medicine associated with Demethylcantharidin

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100 Patents (Medical) associated with Demethylcantharidin

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28

Literatures (Medical) associated with Demethylcantharidin

01 Aug 2024·Advanced Materials

Immunoregulatory Engineering of Semiconducting Charge‐Reversal Nanoantioxidant for Ameliorating Cancer Radioimmunotheranostics

Article

Author: Wen, Peiye ; Luo, Haifen ; Yu, Zhiqiang ; Liu, Gang ; Huang, Wei ; Yang, Zhen ; Lv, Jingqi ; Ma, Wen

AbstractRadiotherapy (RT) is a crucial clinical modality for cancer. However, nonselectivity, toxicity to normal tissues, and radio‐resistance severely limit RT applications. This study develops a versatile X‐ray theranostic nano‐antioxidant (XTN) to prevent normal tissues from oxidative damage and induce systematic and robust anticancer immunity. XTN owns NIR‐II photoacoustic (PA) imaging properties for precise discrimination of the tumor margin through, thereby improving the accuracy of RT. Additionally, XTN is a nano‐antioxidant to enhance the cell viability of normal cells after irradiation. Most importantly, XTN scavenges reactive oxygen species (ROS) in the TME to preserve the stimulatory activity of released high mobility group protein B1 to dendritic cells (DCs) and recover T cells’ immune function. Meanwhile, XTN achieves charge‐reversal specifically releasing an immunomodulator (demethylcantharidin, DMC) in the acidic TME. Moreover, the specifically released DMC inhibits protein phosphatase‐2A activity and reduces regulatory T cell (Treg) differentiation. In the bilateral 4T1 tumor model, XTN‐mediated radioimmunotherapy remarkably boosts a systemic antitumor immune response and induces durable immunological memory against tumor growth.

01 Aug 2024·Chemical Biology & Drug Design

Correction to “Nanoemulsion Based Lipid Nanoparticles for Effective Demethylcantharidin Delivery to Cure Liver Cancer”

01 Jul 2024·Chemical Biology & Drug Design

Nanoemulsion based lipid nanoparticles for effective demethylcantharidin delivery to cure liver cancer

Article

Author: Xia, Die ; Yu, Ting ; Wu, Xiaoping ; Yan, Zijun ; Zhang, Liangming ; Ding, Yuzhen ; Deng, Mengyue ; Su, Ning ; Wei, Panpan ; Chen, Tong ; Zhang, Yuehui

AbstractDemethylcantharidin (DEM) is a widely used antitumor drug; however, its poor tumor targeting and serious organotoxicity limit its application. The aim of this study was to develop a new drug delivery system for efficient delivery of DEM. Nanoemulsion based lipid nanoparticles containing demethylcantharidin (DNLNs) were prepared by loading nanoemulsions into lipid nanoparticles. The cells proliferation, apoptosis, cycle, and uptake were investigated by Cell counting kit‐8 (CCK‐8), flow cytometry, and in situ fluorescence assays, respectively. Then, we established the H22 tumor‐bearing mouse model to evaluate the antitumor efficacy of DNLNs and further studied its organ toxicity and distribution. DNLNs significantly inhibited the proliferation and promoted apoptosis of H22 cells, and H22 cells could take up more DNLNs. Compared with DEM, DNLNs had certain tumor‐targeting properties, and the tumor inhibition rate increased by 23.24%. Moreover, DNLNs can increase white blood cell count and reduce organ toxicity. This study paves the way for nanoemulsion‐based lipid nanoparticle (NLNs)‐efficient DEM delivery to treat liver cancer.

100 Deals associated with Demethylcantharidin

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Phase 1	CN	Shenyang Pharmaceutical University	22 Sep 2020
Esophageal Carcinoma	Phase 1	CN	Shenyang Pharmaceutical University	22 Sep 2020
Lung Cancer	Phase 1	CN	Shenyang Pharmaceutical University	22 Sep 2020