Overview

Generic Name(s):
seliciclib
NCI Definition [1]:
An orally available small molecule and cyclin-dependent kinase (CDK) inhibitor with potential apoptotic and antineoplastic activity. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Seliciclib primarily inhibits CDK 2, 7, and 9 by competing for the ATP binding sites on these kinases, leading to a disruption of cell cycle progression. In addition, this agent seems to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, thereby inhibiting RNA polymerase II-dependent transcription. This may lead to the down-regulation of anti-apoptotic factors, such as myeloid cell leukemia sequence 1 (Mcl-1), a protein crucial for the survival of a range of tumor cell types. The down-regulation of anti-apoptotic factors may lead to an induction of apoptosis, thereby further contributing to seliciclib's antiproliferative effects.

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

BRCA1 Loss (germline), BRCA1 Mutation (germline), and BRCA2 Loss (germline) are the most frequent biomarker inclusion criteria for seliciclib clinical trials.

Breast carcinoma and malignant solid tumor are the most common diseases being investigated in seliciclib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Seliciclib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating seliciclib 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]:
cyc202, r-roscovitine, cyc 202, seliciclib, seliciclib, 2-(r)-(1-ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, cyc-202
Drug Categories [2]:
CDK inhibitors, CDK2 inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
CDK1, CDK2, CDK7, CDK9
NCIT ID [1]:
C62783

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.