Oral chemotherapeutic agents in current use

Namsu Lee; Kyoung Ha Kim; Sang-Cheol Lee

doi:10.5124/jkma.2011.54.11.1191

J Korean Med Assoc > Volume 54(11); 2011 > Article

Lee, Kim, and Lee: Oral chemotherapeutic agents in current use

Pharmacotherapeutics

Journal of the Korean Medical Association

Journal of the Korean Medical Association 2011; 54(11): 1191-1198.

Published online: November 15, 2011

DOI: http://dx.doi.org/10.5124/jkma.2011.54.11.1191

Oral chemotherapeutic agents in current use

Namsu Lee, MD, Kyoung Ha Kim, MD, Sang-Cheol Lee, MD

Department of Internal Medicine, Soonchunhyang University College of Medicine, Seoul, Korea.

Corresponding author: Namsu Lee, mdnslee@schmc.ac.kr

Received August 29, 2011 Accepted September 13, 2011

This is an Open-Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Currently, 10% of cancer chemotherapy is provided to patients by oral formulation; however, by 2013 this percentage is predicted to increase to 25%. Chemotherapy is traditionally given by injection. Oral chemotherapy has been developed as a more convenient method for treating patients. Oral chemotherapy offers many advantages including the elimination of pain often caused by injections, the lack of fees for administering intravenous drugs, more time at home for patients, and a patient's increased sense of autonomy. The role of oral chemotherapy has been expanding because of the potential advantages in convenience and better quality of life for patients, and in the cost-effectiveness of treatment as compared to intravenous chemotherapy. A number of novel oral targeted and cytotoxic chemotherapeutic agents are entering the market or are in development. Many of the agents display significant clinical activity against various cancers. The growing availability of effective oral chemotherapy treatments, especially the new class of 'targeted biologic therapies', is one of the wonderful recent advances in cancer care. This manuscript describes the progress of clinical development and efficacy of these newly developed chemotherapeutic agents.

Neoplasms; Drug therapy; Oral administration

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Figure 1

Metabolism of capecitabine. 5'-DFCR, 5'-deoxy-5-fluorocytidine; dThdPase, thymidine phosphorylase; 5'-DFUR, 5'-deoxy-5-fluorouridine; 5-FU, 5-fluorouracil.

Figure 2

Mode of action of imatinib on BCR-ABL. ADP, adenosine diphosphate; ATP, adenosine triphosphate; P, phosphate.

Figure 3

ErbB2 cellular signaling pathways and lapatinib mechanism of action. PI3K, phosphatidylinositol 3-kinase; IGFIR, insulin-like growth factor receptor; EGFR, epidermal growth factor receptor; mTOR, mammalian target of rapamycin; PTEN, phosphatase and tensin homolog (From Vogel C, et al. Jpn J Clin Oncol 2010;40:999-1013, with permission from Oxford University Press) [14].

Figure 4

Mode of action of everolimus. PI3K, phosphatidylinositol 3-kinase; PTEN, phosphatase and tensin homolog; mTOR, mammalian target of rapamycin (From Atkins MB, et al. Nat Rev Drug Discov 2009;8:535-536, with permission from Nature) [19].

Table 1

Tyrosine kinase inhibitors

HER2/neu, human EGFR type 2; EGFR, epidermal growth factor receptor; PDGFR, plateletderived growth factor; VEGFR, vascular endothelial growth factor receptor; NET, neuroendocrine tumor; CML, chronic myelogenous leukemia; GIST, gastrointestinal stromal tumor; mTOR, mammalian target of rapamycin.