Overview

Generic Name(s):
palbociclib
Trade Name(s):
Ibrance
NCI Definition [1]:
An orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of cell cycle progression.

Biomarker-Directed Therapies

Palbociclib has been investigated in 149 clinical trials, of which 131 are open and 18 are closed. Of the trials investigating palbociclib, 3 are early phase 1 (3 open), 37 are phase 1 (34 open), 20 are phase 1/phase 2 (19 open), 66 are phase 2 (56 open), 2 are phase 2/phase 3 (1 open), 16 are phase 3 (14 open), 2 are phase 4 (1 open), and 3 are no phase specified (3 open).

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

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

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Palbociclib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Palbociclib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating palbociclib 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]:
pd 0332991, pd-0332991, Ibrance, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8h)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-8h-pyrido(2,3-d)pyrimidin-7-one, 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7(8h)-one, pd-332991, palbociclib (substance), palbociclib, 571190-30-2, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-8h-pyrido(2,3-d)pyrimidin-7-one, pd0332991, palbociclib
Drug Categories [2]:
CDK inhibitors, CDK4/6 inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
CDK4, CDK6
NCIT ID [1]:
C49176
SNOMED ID [1]:
R-FF849

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.