Drug intelligence / Profile preview

tivantinib

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Tivantinib is an orally bioavailable small molecule that was developed as a selective inhibitor of the c-Met (MET) receptor tyrosine kinase, which plays a key role in cancer cell growth, survival, and metastasis. By binding to the inactive form of c-Met, tivantinib disrupts downstream signaling pathways such as RAS-MAPK and PI3K-AKT, leading to reduced proliferation and increased apoptosis in tumor cells overexpressing or constitutively activating c-Met[1][2][6][8]. While initially characterized as a highly selective MET inhibitor with antineoplastic activity, subsequent research has suggested that tivantinib may also exert cytotoxic effects independent of MET inhibition—most notably through microtubule binding[3][8]. Tivantinib has been investigated for several cancers including non-small-cell lung carcinoma (NSCLC), hepatocellular carcinoma (HCC), colorectal cancer, gastric cancer, mesothelioma, prostate cancer, renal cell carcinoma and others. Despite promising early results in tumors with high MET expression[8], pivotal phase III trials failed to meet primary endpoints in advanced HCC[3], leading to discontinuation of its development for most indications.

Brand names
tivantinib
Other names
tivantinib
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)ABCG2 (Breast cancer resistance protein)TUBB (Tubulin (alpha and beta subunits))

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