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National Cancer Institute
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Version: 17.06d (Release date: 2017-06-26)
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Irinotecan/P-glycoprotein Inhibitor HM30181AK Combination Tablet (Code C88280)

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Terms & Properties

Preferred Name: Irinotecan/P-glycoprotein Inhibitor HM30181AK Combination Tablet

Definition: An orally bioavailable combination tablet containing the semisynthetic camptothecin derivative irinotecan and the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181AK, with potential antineoplastic activity. HM30181A binds to P-gp and prevents the P-gp-mediated efflux of irinotecan from tumor cells, which may result in greater intracellular concentrations of irinotecan and enhanced cytotoxicity. Retained intracellularly, the prodrug irinotecan is converted, by a carboxylesterase-converting enzyme, to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters and is overexpressed by some MDR tumors, preventing the intracellular accumulation of various cytotoxic agents.

Label: Irinotecan/P-glycoprotein Inhibitor HM30181AK Combination Tablet

NCI Thesaurus Code: C88280 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL412470  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Irinotecan/P-glycoprotein Inhibitor HM30181AK Combination Tablet

External Source Codes: 
PDQ Closed Trial Search ID 656527
PDQ Open Trial Search ID 656527 (check for NCI PDQ open clinical trial info)

Other Properties:
     Name Value (qualifiers indented underneath)
code C88280
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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