Overview

Generic Name(s):
buparlisib
NCI Definition [1]:
An orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. Buparlisib specifically inhibits class I PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Buparlisib has been investigated in 9 clinical trials, of which 2 are open and 7 are closed. Of the trials investigating buparlisib, 4 are phase 1 (1 open), 2 are phase 2 (0 open), and 3 are phase 3 (1 open).

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

Breast carcinoma, head and neck squamous cell carcinoma, and malignant solid tumor are the most common diseases being investigated in buparlisib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Buparlisib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Buparlisib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating buparlisib 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]:
bkm120, pi3k_inhibitor_bkm120, pi3k inhibitor bkm120, pi3k inhibitor bkm120, an2025
Drug Categories [2]:
PI3K inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
PIK3CA, PIK3CB, PIK3CD, PIK3CG
NCIT ID [1]:
C90565

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.