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Thalidomide and Its Analogs as Anticancer Agents

Yen-Ta Huang a, b, Chih W. Hsu a, c, Ted H. Chiu b, d

aDivision of Emergency Medicine, Buddhist Tzu Chi General Hospital, Hualien, Taiwan
bInstitute of Pharmacology and Toxicology, Tzu Chi University, Hualien, Taiwan
cInstitute of Medical Science, Tzu Chi University, Hualien, Taiwan
dDepartment of Pharmacology, Tzu Chi University, Hualien, Taiwan

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Thalidomide has reemerged as a promising anticancer and anti-inflammatory drug despite its devastating congenital birth defects. Many thalidomide derivatives with enhanced antiangiogenic and immunomodulatory effects or greater cytokine inhibition accompanied by less adverse toxicities than the parent drug have been developed. The mechanisms of action of thalidomide and its analogs are complex and not yet fully understood, but studies indicate that their antiangiogenic and immunomodulatory effects play important roles. Thalidomide and lenalidomide have been approved for the treatment of multiple myeloma and myelodysplastic syndrome. The powerful antiangiogenic, anti-inflammatory, and apoptotic effects mean that thalidomide and its immunomodulatory derivatives will continue to be explored in the treatment of a variety of cancers and inflammatory diseases.


Antiangiogenesis; Cytokines; Immunomodulatory drugs; Multiple myeloma; Thalidomide


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