Drugs /

trilaciclib

Back to Drugs List
Associated Genetic Biomarkers

Overview

NCI Definition [1]:
A small molecule, competitive inhibitor of cyclin dependent kinases 4 and 6 (CDK4/6), with potential antineoplastic and chemoprotective activities. Upon intravenous administration, trilaciclib binds to and inhibits the activity of CDK4/6, thereby blocking the phosphorylation of the retinoblastoma protein (Rb) in early G1. This prevents G1/S phase transition, causes cell cycle arrest in the G1 phase, induces apoptosis, and inhibits the proliferation of CDK4/6-overexpressing tumor cells. In patients with CDK4/6-independent tumor cells, G1T28 may protect against multi-lineage chemotherapy-induced myelosuppression (CIM) by transiently and reversibly inducing G1 cell cycle arrest in hematopoietic stem and progenitor cells (HSPCs) and preventing transition to the S phase. This protects all hematopoietic lineages, including red blood cells, platelets, neutrophils and lymphocytes, from the DNA-damaging effects of certain chemotherapeutics and preserves the function of the bone marrow and the immune system. CDKs are serine/threonine kinases involved in the regulation of the cell cycle and may be overexpressed in certain cancer cell types. HSPCs are dependent upon CDK4/6 for proliferation.

Clinical Trials

View Clinical Trials for trilaciclib

Trilaciclib has been investigated in 6 clinical trials, of which 6 are open and 0 are closed. Of the trials investigating trilaciclib, 4 are phase 2 (4 open) and 2 are phase 3 (2 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for trilaciclib clinical trials.

Breast carcinoma, colorectal adenocarcinoma, and invasive breast carcinoma are the most common diseases being investigated in trilaciclib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Trilaciclib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating trilaciclib 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]:
2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'h-spiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one, spiro(cyclohexane-1,9'(6'h)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one, 7',8'-dihydro-2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-, trilaciclib, cdk4/6 inhibitor g1t28, g1t28
Drug Categories [2]:
CDK inhibitors, CDK4/6 inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
CDK4, CDK6
NCIT ID [1]:
C123281

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.