Overview

Generic Name(s):
abemaciclib
NCI Definition [1]:
An orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. Abemaciclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. 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 the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.

Biomarker-Directed Therapies

Abemaciclib has been investigated in 100 clinical trials, of which 85 are open and 15 are closed. Of the trials investigating abemaciclib, 7 are early phase 1 (5 open), 21 are phase 1 (19 open), 13 are phase 1/phase 2 (10 open), 49 are phase 2 (43 open), 1 is phase 2/phase 3 (1 open), 7 are phase 3 (7 open), and 2 are phase 4 (0 open).

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

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

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Abemaciclib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Abemaciclib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating abemaciclib 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]:
ly2835219, ly-2835219, 2-pyrimidinamine, n-(5-((4-ethyl-1-piperazinyl)methyl)-2-pyridinyl)-5-fluoro-4-(4-fluoro-2-methyl-1-(1-methylethyl)-1h-benzimidazol-6-yl), abemaciclib, 2-pyrimidinamine, n-(5-((4-ethyl-1-piperazinyl)methyl)-2-pyridinyl)-5-fluoro-4-(4-fluoro-2-methyl-1-(1-methylethyl)-1h-benzimidazol-6-yl), 1231929-97-7, cdk4/6 dual inhibitor ly2835219
Drug Categories [2]:
CDK inhibitors, CDK4/6 inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
CDK4, CDK6
NCIT ID [1]:
C97660

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.