Overview

NCI Definition [1]:
An inhibitor of the adenosine triphosphate (ATP)-binding cassette (ABC) transporter P-glycoprotein (P-gp), with adjuvant activity. Upon oral administration, P-gp inhibitor HM30181AK selectively binds to and inhibits the multidrug resistance (MDR) efflux pump P-gp, which prevents the efflux of various chemotherapeutic agents from intestinal epithelial cells to the gastrointestinal tract. This leads to an increase in both oral bioavailability and therapeutic efficacy. P-gp prevents the intestinal uptake and intracellular accumulation of various cytotoxic agents. HM30181AK is not systemically absorbed.

Encequidar has been investigated in 3 clinical trials, of which 2 are open and 1 is closed. Of the trials investigating encequidar, 2 are phase 1 (1 open) and 1 is phase 2 (1 open).

Malignant solid tumor and invasive breast carcinoma are the most common diseases being investigated in encequidar clinical trials [2].

Drug Details

Synonyms [2]:
4-oxo-4h-chromene-2-carboxylic acid [2-(2-4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-ethyl]-phenyl-2h-tetrazol-5-yl)-4,5-dimethoxy-phenyl]-amide, hm30181ak, p-glycoprotein inhibitor hm30181ak, 4-oxo-4h-chromene-2-carboxylic acid [2-(2-4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-ethyl]-phenyl-2h-tetrazol-5-yl)-4,5-dimethoxy-phenyl]-amide, pgp inhibitor hm30181ak, pgp inhibitor hm30181ak, hm30181a
Drug Target(s) [2]:
ABCB1
NCIT ID [1]:
C111994

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.