Overview

NCI Definition [1]:
An orally available human ribonucleotide reductase (RNR) subunits interaction inhibitor, with potential antineoplastic and immunomodulating activities. Upon oral administration, the RNR subunits interaction inhibitor TAS1553 blocks the protein-protein interaction between and interferes with the assembly of the RNR subunits R1 and R2. This prevents RNR activity and decreases the pool of deoxyribonucleotide triphosphates (dNTPs) available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may have immunomodulatory effects on the tumor microenvironment (TME), may increase the number of CD8+ T-cells and may increase the expression of interferon gamma (IFNg) in tumors. RNR, an enzyme that catalyzes the conversion of ribonucleoside diphosphate to deoxyribonucleoside diphosphate, is essential for de novo DNA synthesis and plays an important role in cell growth; it is overexpressed in many cancer cell types and is associated with increased drug resistance, cancer cell growth and metastasis.

Tas1553 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating tas1553, 1 is phase 1 (1 open).

BCR-ABL1 Fusion, PML-RARA Fusion, and t(15;17)(q22;q12) are the most frequent biomarker inclusion criteria for tas1553 clinical trials.

Acute myeloid leukemia, myelodysplastic/myeloproliferative neoplasm, and myeloproliferative neoplasm are the most common diseases being investigated in tas1553 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tas1553
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tas1553 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]:
tas-1553, rnr subunits interaction inhibitor tas1553, rnr inhibitor tas1553, ribonucleotide reductase inhibitor tas1553, protein-protein rnr subunits interaction inhibitor tas1553
NCIT ID [1]:
C176434

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.