Drugs /

wnt974

Back to Drugs List

Overview

NCI Definition [1]:
An orally available inhibitor of porcupine (PORCN), with potential antineoplastic activity. Upon oral administration, WNT974 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational acylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine, a membrane-bound O-acyltransferase (MBOAT), is required for the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion and activity. Wnt signaling is dysregulated in a variety of cancers.

Clinical Trials

View Clinical Trials for wnt974

Wnt974 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating wnt974, 1 is phase 1 (1 open).

BRAF Mutation, BTRC Mutation, and DVL1 Mutation are the most frequent biomarker inclusion criteria for wnt974 clinical trials.

Breast carcinoma, cervical squamous cell carcinoma, and colorectal carcinoma are the most common diseases being investigated in wnt974 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Wnt974
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating wnt974 and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
porcupine inhibitor wnt974, 2-(2,3-dimethyl-[2,4-bipyridin]-5-yl)-n-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, lgk974, porcn inhibitor lgk974, 2-(2,3-dimethyl-[2,4-bipyridin]-5-yl)-n-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Drug Target(s) [2]:
PORCN
NCIT ID [1]:
C116860

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.