Drug intelligence / Profile preview

tivantinib + anti-cancer therapy

Development stage
Discontinued
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Tivantinib (ARQ 197) is an oral, selective, small-molecule, non-ATP competitive inhibitor of the c-MET receptor tyrosine kinase, developed by ArQule (a subsidiary of Merck & Co.). The c-MET pathway is frequently dysregulated in human cancers, contributing to tumor cell proliferation, survival, invasion, and angiogenesis. This specific combination therapy regimen involves tivantinib used in conjunction with other anti-cancer agents such as erlotinib, sorafenib, pemetrexed, docetaxel, gemcitabine, irinotecan, or cetuximab. It was primarily investigated for the treatment of advanced refractory solid tumors, including hepatocellular carcinoma (HCC) and non-small cell lung cancer (NSCLC). Despite promising early-phase results, tivantinib failed to meet primary endpoints in several Phase 3 trials, leading to the discontinuation of its development for major indications.

Other names
ARQ-197ARQ197ARQ 197tivantinib combination therapy
02

Targets

TUBB (Tubulin (alpha and beta subunits))GSK3 (Glycogen synthase kinase 3 beta)MET (Mesenchymal-epithelial transition factor receptor)

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