Overview

NCI Definition [1]:
An orally bioavailable, small molecule inhibitor of certain class I phosphoinositide 3-kinase (PI3K) isoforms and mammalian target of rapamycin kinase (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR inhibitor LY3023414 inhibits both certain PI3K isoforms and mTOR in an ATP-competitive manner which may inhibit both the PI3K/mTOR signaling pathway in and proliferation of tumor cells overexpressing PI3K and/or mTOR. The PI3K/mTOR pathway is upregulated in a variety of tumor cells and plays a key role in promoting cancer cell proliferation, and survival, motility and resistance to chemotherapy and radiotherapy. mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion; therefore, this agent may be more potent than an agent that inhibits either PI3K or mTOR alone. In addition, LY3023414 may inhibit DNA-dependent protein kinase (DNA-PK), thereby inhibiting the ability of tumor cells to repair damaged DNA. DNA-PK is activated upon DNA damage and plays a key role in repairing double-stranded DNA breaks.

Samotolisib has been investigated in 8 clinical trials, of which 5 are open and 3 are closed. Of the trials investigating samotolisib, 5 are phase 1 (2 open) and 3 are phase 2 (3 open).

HER2 Deficient Expression, HER2 Negative, and PIK3CA Mutation are the most frequent biomarker inclusion criteria for samotolisib clinical trials.

Breast carcinoma, malignant solid tumor, and non-hodgkin lymphoma are the most common diseases being investigated in samotolisib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Samotolisib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Samotolisib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating samotolisib 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]:
ly 3023414, ly3023414, pi3k/mtor inhibitor ly3023414, ly-3023414
Drug Categories [2]:
MTOR inhibitors, PI3K inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG, PRKDC
NCIT ID [1]:
C121817

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.