[Anti-angiogenesis targeting drugs: a review]

Ka Jia1, Jin Li

  • 1Department of Medical Oncology, Cancer Hospital, Fudan University, Shanghai, 200032, PR China. 0256277@fudan.edu.cn

Insights

Targeting tumor angiogenesis, driven by vascular endothelial growth factor (VEGF), offers a promising cancer therapy strategy. This review covers anti-VEGF/VEGFR agents and clinical data for novel anticancer treatments.

Area of Science:

  • Oncology
  • Molecular Biology
  • Vascular Biology

Context:

  • Tumor growth and metastasis rely on neovascularization.
  • Vascular Endothelial Growth Factor (VEGF) is a critical regulator of angiogenesis.
  • Targeting the VEGF pathway presents a rational approach for cancer treatment.

Purpose:

  • To review the development of anti-VEGF/VEGFR agents.
  • To discuss the latest clinical data on these targeted therapies.
  • To highlight key therapeutic strategies in angiogenesis inhibition.

Summary:

  • The review examines anti-VEGF/VEGFR agents, including bevacizumab (anti-VEGF monoclonal antibody), sunitinib and sorafenib (VEGFR tyrosine kinase inhibitors), and IMC-1C11 (VEGFR monoclonal antibody).
  • Clinical data for these agents are presented, underscoring their role in cancer therapy.
  • The dependence of tumor progression on angiogenesis makes VEGF a significant therapeutic target.

Impact:

  • Provides an overview of current anti-angiogenesis therapies targeting VEGF/VEGFR.
  • Informs on the clinical efficacy and development of targeted cancer treatments.
  • Highlights the therapeutic potential of inhibiting tumor neovascularization.

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Mechanism of Angiogenesis01:10

Mechanism of Angiogenesis

Blood vessel formation starts early during embryonic development, around day 7. In the extraembryonic yolk sac, mesodermal precursor cells called hemangioblast proliferate and differentiate into angioblast. Angioblasts express vascular endothelial growth factor receptor 2 or VEGFR2, which binds VEGF-A, a proangiogenic factor, guiding blood vessel formation. VEGF signaling promotes angioblasts to form a blood island in the developing embryo. Angioblasts further differentiate, giving rise to...
Regulation of Angiogenesis and Blood Supply01:24

Regulation of Angiogenesis and Blood Supply

Rapidly dividing tumors, embryos, and wounded tissues require more oxygen than usual, lowering the oxygen concentration in the blood. At low oxygen or hypoxic conditions, an oxygen-sensitive transcription factor called the hypoxia-inducible factor 1 or HIF1 is activated. HIF1 is a dimeric protein of alpha (ɑ) and beta (β) subunits.  Under optimal oxygen conditions, HIF1β is present in the nucleus while HIF1ɑ remains in the cytosol. HIF1ɑ is hydroxylated by prolyl hydroxylase and factor...
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...
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...