Overview

NCI Definition [1]:
An orally bioavailable, small molecule reactivator of the p53 Y220C mutant, with potential antineoplastic activity. Upon oral administration, p53 Y220C mutant reactivator PC14586 selectively targets and binds to the crevice created by the p53 Y220C mutation, which normalizes and restores wild-type p53 protein structure and activity. This blocks tumor cell cycle progression and induces apoptosis in tumor cells expressing the p53 Y220C mutant. The p53 gene, a tumor suppressor gene, is mutated in many tumor types. The p53 protein plays a key role in the regulation of apoptosis and cellular proliferation.

Pc14586 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating pc14586, 1 is phase 1/phase 2 (1 open).

TP53 Y220C is the most frequent biomarker inclusion criterion for pc14586 clinical trials.

Malignant solid tumor is the most common disease being investigated in pc14586 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Pc14586
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating pc14586 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]:
mutant p53 activator pc14586, p53 y220c mutant reactivator pc14586, pc 14586, pc-14586
Drug Target(s) [2]:
TP53
NCIT ID [1]:
C175961

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.