Phase I/II Study of TSU-68 for Advanced Hepatocellular Carcinoma

This study has been completed.
Information provided by (Responsible Party):
Taiho Pharmaceutical Co., Ltd. Identifier:
First received: October 30, 2008
Last updated: March 22, 2012
Last verified: March 2012
The purpose of this study is to evaluate the safety and efficacy of Orantinib, an oral tyrosine kinase inhibitor of vascular endothelial growth factor receptor-2, platelet-derived growth factor receptor, and fibroblast growth factor receptor, in patients with advanced hepatocellular carcinoma (HCC).

Condition Intervention Phase
Hepatocellular Carcinoma
Drug: Orantinib (TSU-68)
Phase 1
Phase 2

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Safety/Efficacy Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: Phase I/II Study of TSU-68 for Advanced Hepatocellular Carcinoma

Resource links provided by NLM:

Further study details as provided by Taiho Pharmaceutical Co., Ltd.:

Primary Outcome Measures:
  • Step 1(Phase I) Safety [ Time Frame: During chemotherapy ] [ Designated as safety issue: Yes ]
  • Step 2(Phase II) Response rate(RR) [ Time Frame: Until progression ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Step 1(Phase I) Response rate(RR) [ Time Frame: Until progression ] [ Designated as safety issue: No ]
  • Step 2(Phase II) Safety [ Time Frame: During chemotherapy ] [ Designated as safety issue: Yes ]

Enrollment: 35
Study Start Date: September 2003
Study Completion Date: March 2012
Primary Completion Date: October 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: 1
Drug: Orantinib (TSU-68)
200 or 400 mg bid day 1~day 28 cycle until progression or unacceptable toxicity develops

Detailed Description:
As HCC is a highly vascular tumor, a number of antiangiogenic agents have been tested for the treatment of HCC. Orantinib is an orally administered, small-molecule, multiple receptor tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR). Phase I studies that have been conducted in Japan for patients with solid tumors recommended a dosage of 400 mg bid. As a potent antiangiogenic agent, Orantinib is also expected to be effective against HCC. However, because most HCC patients have accompanying liver cirrhosis or hepatitis, its safety must be reevaluated in the presence of liver function impairment.

Ages Eligible for Study:   20 Years to 74 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   No

Inclusion Criteria:

  • Age 20-74
  • PS 0-2
  • Patients who did not respond to surgery, RFA, TAE, chemotherapy, or radiotherapy
  • Chid-Pugh A or B
  • At least one measurable lesion by RECIST criteria

Exclusion Criteria:

  • Large amount of pleural effusion or ascites
  • Esophageal varices
  • Simultaneously active double cancer
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its identifier: NCT00784290

Chiba University Hospital
Inohana Chuo-ku Chiba, Chiba, Japan, 260-8670
Sponsors and Collaborators
Taiho Pharmaceutical Co., Ltd.
Study Chair: Masao Omata, M.D. Yamanashi Prefectural Central Hospital
  More Information

Publications automatically indexed to this study by Identifier (NCT Number):
Responsible Party: Taiho Pharmaceutical Co., Ltd. Identifier: NCT00784290     History of Changes
Other Study ID Numbers: Taiho132070 
Study First Received: October 30, 2008
Last Updated: March 22, 2012
Health Authority: Japan: Ministry of Health, Labor and Welfare

Additional relevant MeSH terms:
Carcinoma, Hepatocellular
Digestive System Diseases
Digestive System Neoplasms
Liver Diseases
Liver Neoplasms
Neoplasms by Histologic Type
Neoplasms by Site
Neoplasms, Glandular and Epithelial
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Protein Kinase Inhibitors processed this record on May 26, 2016