Overview

NCI Definition [1]:
A dinucleotide antimetabolite of a decitabine linked via phosphodiester bond to a guanosine, with potential antineoplastic activity. Following metabolic activation by phosphorylation and incorporation into DNA, guadecitabine inhibits DNA methyltransferase, thereby causing genome-wide and non-specific hypomethylation, and inducing cell cycle arrest at S-phase. This agent is resistant to cytidine deaminase, hence may result in gradual release of decitabine both extra and intracellularly, leading to more prolonged exposures to decitabine.

Guadecitabine has been investigated in 16 clinical trials, of which 10 are open and 6 are closed. Of the trials investigating guadecitabine, 2 are phase 1 (2 open), 3 are phase 1/phase 2 (2 open), 8 are phase 2 (6 open), and 3 are phase 3 (0 open).

Complex karyotype, Very Complex karyotype, and EGFR A763_Y764insFQEA are the most frequent biomarker inclusion criteria for guadecitabine clinical trials.

Myelodysplastic syndromes, chronic myelomonocytic leukemia, and non-small cell lung carcinoma are the most common diseases being investigated in guadecitabine clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Guadecitabine
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Guadecitabine
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating guadecitabine 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]:
dna methyltransferase inhibitor sgi-110, dnmt inhibitor sgi-110, sgi-110, s110
Drug Categories [2]:
DNMT inhibitors
NCIT ID [1]:
C95209

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.