Overview

NCI Definition [1]:
An orally available inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR inhibitor RP-3500 selectively targets and inhibits ATR activity and blocks the downstream phosphorylation of the serine/threonine protein kinase checkpoint kinase 1 (CHK1). This prevents ATR-mediated signaling, which results in the inhibition of DNA damage checkpoint activation, the disruption of DNA damage repair, and the induction of tumor cell apoptosis. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression and survival. It is activated by DNA damage caused during DNA replication-associated stress.

Rp-3500 has been investigated in 2 clinical trials, of which 2 are open and 0 are closed. Of the trials investigating rp-3500, 2 are phase 1/phase 2 (2 open).

ATR Loss and ATR Mutation are the most frequent biomarker inclusion criteria for rp-3500 clinical trials.

Malignant solid tumor is the most common disease being investigated in rp-3500 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Rp-3500
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating rp-3500 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]:
rp 3500, atr inhibitor rp-3500, rp3500
Drug Target(s) [2]:
ATR
NCIT ID [1]:
C174206

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.