Malignant Neoplasms of the Small Intestine Medication

Updated: May 18, 2022
  • Author: Ponnandai S Somasundar, MD, MPH, FACS; Chief Editor: N Joseph Espat, MD, MS, FACS  more...
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Medication Summary

No standard regimen demonstrates benefit in an adjuvant or metastatic setting for small-bowel adenocarcinoma. Because of the similarity to colorectal adenocarcinoma, a regimen containing 5-FU with leucovorin (ie, Roswell Park, Mayo Clinic) may be used. Newer agents active in colorectal carcinoma, such as irinotecan and oxaliplatin, may also be considered, in combination with 5-FU. Small-bowel sarcomas, most of which are c-kit –positive GISTs, are resistant to cytotoxic chemotherapy. However, patients with advanced disease may be treated with imatinib.


Chemotherapeutic agents

Class Summary

Chemical substances or drugs that treat neoplastic diseases by interfering with DNA synthesis.

Fluorouracil (Adrucil)

Fluorinated pyrimidine analog. Metabolite, FdUMP, inhibits thymidylate synthase that is essential in folate metabolism. 5-FU metabolites FUTP and FdUTP inhibit RNA and DNA synthesis by incorporating into RNA and DNA, respectively.

Leucovorin (Wellcovorin)

Racemic mixture of 5-formyltetrahydrofolate. Metabolized to reduced folate 5,10-methylenetetrahydrofolate, which forms ternary complex with FdUMP and thymidylate synthase, enhancing inhibition of the latter.

Irinotecan (Camptosar)

Camptothecin derivative that inhibits topoisomerase I, resulting in double-stranded DNA damage. Approved as first-line therapy in combination with 5-FU and leucovorin or as second-line, single-agent therapy after 5-FU for advanced colorectal cancer.

Oxaliplatin (Eloxatin)

Organoplatinum complex that acts as an alkylating agent. Metabolites cross-link with DNA, inhibiting DNA synthesis and function. Combination with 5-FU and leucovorin (FOLFOX 4 regimen) is approved for treatment of advanced colorectal cancer.


Tyrosine kinase inhibitors

Class Summary

Inhibit tyrosine kinase activity of c-kit,bcr-abl, and PDGFR oncogenes.

Imatinib mesylate (Gleevec)

Small molecule that selectively inhibits tyrosine kinase activity of c-kit,bcr-abl, and PDGFR. Available in 100-mg caps.


Multikinase inhibitors

Class Summary

Elicit actions via multiple tyrosine kinase inhibitors implicated in tumor growth, pathologic angiogenesis, and metastatic progression.

Sunitinib (Sutent)

Mulitkinase inhibitor that targets several tyrosine kinase inhibitors implicated in tumor growth, pathologic angiogenesis, and metastatic progression. Inhibits platelet-derived growth factor receptors (ie, PDGFR-alpha, PDGFR-beta), vascular endothelial growth factor receptors (ie, VEGFR1, VEGFR2, VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony-stimulating factor receptor type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET).

Indicated for persons with gastrointestinal stromal tumors (GISTs) whose disease has progressed or who are unable to tolerate treatment with imatinib (Gleevec). Delays median time to tumor progression.