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lxh254

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Associated Genetic Biomarkers

Overview

NCI Definition [1]:
An orally available inhibitor of all members of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon administration, pan-RAF inhibitor LXH254 binds to Raf proteins and inhibits Raf-mediated signal transduction pathways. This inhibits proliferation of Raf-overexpressing tumor cells. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. They play key roles in tumor cell proliferation and survival.

Clinical Trials

View Clinical Trials for lxh254

Lxh254 has been investigated in 5 clinical trials, of which 5 are open and 0 are closed. Of the trials investigating lxh254, 4 are phase 1 (4 open) and 1 is phase 2 (1 open).

NRAS Mutation, BRAF Codon 600 Missense, and BRAF Mutation are the most frequent biomarker inclusion criteria for lxh254 clinical trials.

Cutaneous melanoma, non-small cell lung carcinoma, and colorectal carcinoma are the most common diseases being investigated in lxh254 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Lxh254
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating lxh254 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]:
raf family kinase inhibitor lxh254, pan-raf kinase inhibitor lxh254, pan-raf inhibitor lxh254, lxh 254, lxh-254, raf family kinase inhibitor lxh254, pan-raf inhibitor lxh254
Drug Categories [2]:
BRAF inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
ARAF, BRAF, RAF1
NCIT ID [1]:
C125003

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.