Overview

NCI Definition [1]:
An orally available inhibitor of maternal embryonic leucine zipper kinase (MELK) with potential antineoplastic activity. Upon administration, OTS167 binds to MELK, which prevents both MELK phosphorylation and activation; thus inhibiting the phosphorylation of downstream MELK substrates. This may lead to an inhibition of both cell proliferation and survival in MELK-expressing tumor cells. MELK, a serine/threonine kinase, is involved in cancer cell survival, invasiveness and cancer-stem cell formation and maintenance; it is highly upregulated in various types of cancer cells and absent in normal, healthy cells.

Ots167 has been investigated in 2 clinical trials, of which 2 are open and 0 are closed. Of the trials investigating ots167, 1 is phase 1 (1 open) and 1 is phase 1/phase 2 (1 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for ots167 clinical trials.

Acute biphenotypic leukemia, acute lymphoblastic leukemia, and acute myeloid leukemia are the most common diseases being investigated in ots167 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Ots167
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating ots167 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]:
melk inhibitor ots167
Drug Categories [2]:
Serine/threonine kinase inhibitors
Drug Target(s) [2]:
MELK
NCIT ID [1]:
C111569

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.