Overview

Generic Name(s):
ribociclib
Trade Name(s):
Kisqali
NCI Definition [1]:
An orally available cyclin-dependent kinase (CDK) inhibitor targets at cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. Ribociclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.

Biomarker-Directed Therapies

Ribociclib has been investigated in 65 clinical trials, of which 53 are open and 12 are closed. Of the trials investigating ribociclib, 2 are early phase 1 (2 open), 21 are phase 1 (17 open), 9 are phase 1/phase 2 (8 open), 23 are phase 2 (19 open), and 10 are phase 3 (7 open).

ER Positive, HER2 Deficient Expression, and HER2 Negative are the most frequent biomarker inclusion criteria for ribociclib clinical trials.

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

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Ribociclib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Ribociclib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating ribociclib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,931 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
lee011, Kisqali, 1211441-98-3, ribociclib, 7-cyclopentyl-n,n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxamide, cdk4/6 inhibitor lee011, 7-cyclopentyl-n,n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxamide, lee-011
Drug Categories [2]:
CDK inhibitors, CDK4/6 inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
CDK4, CDK6
NCIT ID [1]:
C95701

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.