Related Experiment Video

Updated: Apr 18, 2026

Chemotherapy-induced Vascular Toxicity - Real-time In vivo Imaging of Vessel Impairment
04:48

Chemotherapy-induced Vascular Toxicity - Real-time In vivo Imaging of Vessel Impairment

Published on: January 7, 2015

7.9K

Tubulin colchicine binding site inhibitors as vascular disrupting agents in clinical developments

Ya-Ting Ji, Yan-Na Liu, Zhao-Peng Liu1

  • 1Institute of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China. liuzhaop@sdu.edu.cn.

Current Medicinal Chemistry
|January 27, 2015
PubMed

Insights

Vascular disrupting agents (VDAs) offer novel cancer therapies by targeting tumor blood vessels. This review summarizes small-molecule VDAs in clinical development, highlighting promising candidates for tumor treatment.

Area of Science:

  • Oncology
  • Vascular Biology
  • Medicinal Chemistry

Background:

  • Tumor vasculature is a critical target for cancer therapy, with antiangiogenic and antivascular strategies.
  • Vascular disrupting agents (VDAs) selectively target established tumor blood vessels, leading to tumor cell death.
  • Small-molecule VDAs, particularly tubulin colchicine binding site inhibitors, show significant clinical potential.

Purpose of the Study:

  • To review the clinical development of small-molecule vascular disrupting agents (VDAs).
  • To highlight potential VDA leads and candidates for cancer treatment.

Main Methods:

  • Literature review of small-molecule VDAs targeting tumor vasculature.
  • Summary of compounds in clinical trials, including tubulin colchicine binding site inhibitors.
  • Identification of potential VDA candidates based on efficacy and selectivity.

Main Results:

  • Numerous small-molecule VDAs have been developed, with many entering clinical trials.
  • Tubulin colchicine binding site inhibitors represent a well-studied class of VDAs.
  • Several compounds like CA-4P, AVE8062, and OXi4503 are among those in clinical development.

Conclusions:

  • Small-molecule VDAs are a promising therapeutic strategy for cancer.
  • Continued research and development of VDAs could lead to new effective cancer treatments.
  • Targeting tumor vasculature remains a key area for novel oncology drug discovery.

More Related Videos

Author Spotlight: Purifying High-Quality Tubulin to Study Protein Dynamics and Therapeutic Applications06:30

Author Spotlight: Purifying High-Quality Tubulin to Study Protein Dynamics and Therapeutic Applications

Published on: October 11, 2024

2.4K
Spatiotemporal Subcellular Manipulation of the Microtubule Cytoskeleton in the Living Preimplantation Mouse Embryo using Photostatins08:13

Spatiotemporal Subcellular Manipulation of the Microtubule Cytoskeleton in the Living Preimplantation Mouse Embryo using Photostatins

Published on: November 30, 2021

2.9K

Related Concept Videos

Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
4.4K
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.9K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
11.9K
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
1.6K
Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants01:18

Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants

Oral anticoagulants are vital tools in preventing and treating blood clotting disorders. This diverse class of medications can be categorized as vitamin K antagonists, exemplified by warfarin, and direct thrombin inhibitors (DTIs), such as dabigatran, as well as factor Xa inhibitors, including rivaroxaban.
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
2.9K
Venous Thrombosis III: Interprofessional Care01:29

Venous Thrombosis III: Interprofessional Care

Venous thrombosis requires effective prevention and treatment strategies to improve patient outcomes and reduce potential complications.Prevention StrategiesHealthcare providers must prioritize preventing venous thromboembolism (VTE) for all adult patients upon admission. Interventions depend on bleeding and thrombosis risk, medical history, current medications, diagnoses, planned procedures, and patient preferences. Patients on bed rest should change positions every two hours and, if not...
473