Overview

NCI Definition [1]:
An orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. As mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K, this agent may potentially be more potent than an agent that inhibits either PI3K kinase or mTOR kinase. By inhibiting mTOR to a lesser extent than PI3K, PQR309 does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling. Blocking the negative feedback loop would potentially increase PI3K signaling and decrease therapeutic efficacy.

Bimiralisib has been investigated in 2 clinical trials, of which 0 are open and 2 are closed. Of the trials investigating bimiralisib, 1 is phase 1/phase 2 (0 open) and 1 is phase 2 (0 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for bimiralisib clinical trials.

Breast carcinoma and head and neck squamous cell carcinoma are the most common diseases being investigated in bimiralisib clinical trials [2].

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Bimiralisib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating bimiralisib 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]:
pqr309, pqr-309, pan-pi3k/mtor inhibitor pqr309
Drug Categories [2]:
MTOR inhibitors, PI3K inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG, RICTOR
NCIT ID [1]:
C111898

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.