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nemtabrutinib

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Overview

NCI Definition [1]:
An orally available reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon administration, nemtabrutinib non-covalently binds to and inhibits the activity of both the wild-type and the C481S mutated form of BTK, a resistance mutation in the BTK active site in which cysteine is substituted for serine at residue 481. This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B-cells that overexpress BTK. Compared to other BTK inhibitors, nemtabrutinib does not require interaction with the BTK C481 site and inhibits the proliferation of cells harboring the BTK C481S mutation. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed or mutated in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B-lymphocytes.

Clinical Trials

View Clinical Trials for nemtabrutinib

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

BCL2 Fusion, BCL6 Fusion, and CCND1 Expression are the most frequent biomarker inclusion criteria for nemtabrutinib clinical trials.

Chronic lymphocytic leukemia/small lymphocytic lymphoma, mantle cell lymphoma, and marginal zone lymphoma are the most common diseases being investigated in nemtabrutinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Nemtabrutinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating nemtabrutinib 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]:
mk1026, bruton's tyrosine kinase inhibitor arq 531, arq531, arq 531, btk inhibitor arq 531
Drug Target(s) [2]:
BTK
NCIT ID [1]:
C138066

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.