Anti-Angiogenesis Drug Discovery and Development

Anti-Angiogenesis Drug Discovery and Development

Volume: 4

The inhibition of angiogenesis is an effective mechanism of slowing down tumor growth and malignancies. The process of induction or pro-angiogenesis is highly desirable for the treatment of ...
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Angiogenesis in Cancer Treatment: 60 Years’ Swing Between Promising Trials and Disappointing Tribulations

Pp. 34-96 (63)

Khalid Alhazzani, Ali Alaseem, Mohammad Algahtani, Sivanesan Dhandayuthapani, Thiagarajan Venkatesan, Appu and Rathinavelu


Pathological angiogenesis plays essential role in tumor progression, invasiveness, and metastasis. This process is highly stimulated by VEGF/VEGFR signaling pathway(s). Additional players such as Ang/Tie-2, FGF/FGFR, and Notch signals are also involved in this complex process by stabilization and maturation of blood vessels. As a result of the identification of molecular pathways and various targets driving angiogenesis, several agents have been developed for cancer treatment. Among various pathways, targeting VEGF/VEGFR2 has been proven to be the most effective to inhibit tumor angiogenesis and subsequent tumor growth in preclinical and clinical settings. This chapter highlights on the ramification of some of the crucial events that leads to the maturation of angiogenesis, explore the perplex process of angiogenesis and discuss the amenable strategies for intervention. We will discuss about the myriad number of current therapeutic agents based the target selectivity, preclinical findings, clinical application, and toxicity profile.


Ang/Tie-2, Notch Signals, Pathological Angiogenesis, Toxicity profile, Tumor Growth, Tumor Progression.


Rumbaugh-Goodwin Institute for Cancer Research, Nova Southeastern University, Fort Lauderdale, Florida, USA.