Clinical Trials

Numerous Phase 1 through Phase 3 clinical trials, supported by industry partners and academic institutions, have investigated the therapeutic potential and pharmacokinetic profile of tivantinib (ARQ 197). These completed or terminated protocols evaluated tivantinib as a single agent or in combination regimens across diverse oncology indications—including MET-high hepatocellular carcinoma, non-small cell lung cancer, colorectal cancer, triple-negative breast cancer, and advanced solid tumors—as well as in cohorts with hepatic impairment.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01178411 COMPLETED
Advanced Solid Tumors
ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)
 2010-08-31 PHASE1; PHASE2
NCT01654965 COMPLETED
Adult Solid Neoplasm
National Cancer Institute (NCI)
 2012-07-24 PHASE1
NCT01696955 COMPLETED
Head and Neck Squamous Cell Carcinoma; Recurrent Head and Neck Carcinoma
National Cancer Institute (NCI)
 2012-08-20 PHASE2
NCT01688973 COMPLETED
Recurrent Renal Cell Carcinoma; Stage III Renal Cell Cancer; Stage IV Renal Cell Cancer; Type 1 Papillary Renal Cell Carcinoma; Type 2 Papillary Renal Cell Carcinoma
National Cancer Institute (NCI)
 2012-08-20 PHASE2
NCT01755767 COMPLETED
Hepatocellular Carcinoma
Daiichi Sankyo
 2012-12-27 PHASE3
NCT02608411 TERMINATED
Carcinoma, Small Cell
Istituto Oncologico Veneto IRCCS
 2016-02-19 PHASE2
NCT01395758 COMPLETED
Metastatic Non-Small Cell Lung Cancer
ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)
 2011-07 PHASE2
NCT01749384 COMPLETED
Solid Neoplasm
National Cancer Institute (NCI)
 2012-12-06 PHASE1
NCT01892527 COMPLETED
Colorectal Cancer Metastatic; C-met Overexpression
Armando Santoro, MD
 2013-03 PHASE2
NCT02049060 COMPLETED
Malignant Pleural Mesothelioma; Nonsquamous Nonsmall Cell Neoplasm of Lung
Armando Santoro, MD
 2013-01 PHASE1; PHASE2
NCT02150733 COMPLETED
Hepatic Impairment; Solid Tumor; Cancer
Daiichi Sankyo
 2014-04 PHASE1
NCT01625156 COMPLETED
Adult Solid Neoplasm
National Cancer Institute (NCI)
 2012-05 PHASE1
NCT01519414 COMPLETED
Hormone-Resistant Prostate Cancer; Prostate Adenocarcinoma; Recurrent Prostate Carcinoma; Stage IV Prostate Cancer
National Cancer Institute (NCI)
 2012-01-11 PHASE2
NCT01611857 COMPLETED
Malignant Solid Tumour; Gastroesophageal Cancer
SCRI Development Innovations, LLC
 2012-07 PHASE1; PHASE2
NCT01725191 COMPLETED
Childhood Solid Neoplasm
National Cancer Institute (NCI)
 2012-10 PHASE1
NCT01861301 TERMINATED
Epithelioid Mesothelioma; Recurrent Malignant Mesothelioma; Sarcomatoid Mesothelioma; Stage II Pleural Mesothelioma; Stage III Pleural Mesothelioma; Stage IV Pleural Mesothelioma
National Cancer Institute (NCI)
 2013-01 PHASE2
NCT01468922 COMPLETED
Solid Tumor
National Cancer Institute (NCI)
 2012-01-23 PHASE1
NCT02150733 Completed
Hepatic Impairment|Solid Tumor|Cancer
Daiichi Sankyo|Medpace Inc.
 2014-04 Phase 1
NCT01447914 COMPLETED
Refractory Multiple Myeloma
National Cancer Institute (NCI)
 2011-11 PHASE2
NCT01517399 COMPLETED
Solid Tumors
Daiichi Sankyo
 2011-12 PHASE1
NCT01575522 COMPLETED
Estrogen Receptor Negative; HER2/Neu Negative; Progesterone Receptor Negative; Recurrent Breast Carcinoma; Stage IV Breast Cancer; Triple-Negative Breast Carcinoma
National Cancer Institute (NCI)
 2012-03 PHASE2
NCT01892527 Completed
Colorectal Cancer Metastatic|C-met Overexpression
Armando Santoro MD|Istituto Clinico Humanitas
 2013-03 Phase 2
NCT01699061 COMPLETED
Solid Tumors
Daiichi Sankyo
 2012-07 PHASE1
NCT02049060 Completed
Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung
Armando Santoro MD|Istituto Clinico Humanitas
 2013-01 Phase 1|Phase 2
NCT01244191 TERMINATED
Non Squamous, Non-small-cell Lung Cancer
Daiichi Sankyo
 2011-01-11 PHASE3
NCT01755767 Completed
Hepatocellular Carcinoma
Daiichi Sankyo|ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)
 2012-12-27 Phase 3
NCT01075048 COMPLETED
Metastatic Colorectal Cancer
Daiichi Sankyo
 2010-01-26 PHASE1; PHASE2
NCT01055067 TERMINATED
Non-CNS Germ Cell Tumors (Seminomas and Nonseminomas)
Daiichi Sankyo
 2010-02-02 PHASE2
NCT01149720 COMPLETED
Solid Tumors
Daiichi Sankyo
 2010-07 PHASE1

(data from https://clinicaltrials.gov, updated on 2021-03-10)

Check the Tivantinib product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Tivantinib selectively binds to the human c-Met receptor tyrosine kinase through a non-ATP-competitive mechanism, suppressing constitutive c-Met autophosphorylation and downstream MAPK pathway activation. This biochemical inhibition triggers G2/M cell cycle arrest and apoptosis while blocking cancer cell proliferation, invasion, and migration, providing the biological rationale for targeting c-Met-overexpressing solid tumors such as hepatocellular carcinoma and non-small cell lung cancer in clinical trials.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.