Actively Recruiting
Study of a Tankyrase Inhibitor RK-582 for Patients With Unresectable Metastatic Colorectal Cancer
Led by Eiji Shinozaki · Updated on 2025-07-29
48
Participants Needed
1
Research Sites
102 weeks
Total Duration
On this page
Sponsors
E
Eiji Shinozaki
Lead Sponsor
J
Japan Agency for Medical Research and Development
Collaborating Sponsor
AI-Summary
What this Trial Is About
Tankyrase, the fifth and sixth members of the poly(ADP-ribose) polymerase (PARP) family (PARP-5a/b), is responsible for poly(ADP-ribosyl)ation (PARylation), and was originally identified as a factor that promotes the function of telomerase, an enzyme that elongates telomeres. Subsequently, it was reported that tankyrase enhances Wnt/beta-catenin signaling by PARylation and subsequent degradation of AXIN, a negative regulator of Wnt/beta-catenin signaling, suggesting that tankyrase inhibitors may be a new treatment for colorectal cancer. RK-582 was discovered through lead optimization from a tankyrase inhibitor that suppresses the growth of human colorectal cancer cells. It was confirmed that RK-582 selectively inhibited tankyrase among the PARP family enzymes, suppressed the growth of Wnt/beta-catenin signal-dependent human colorectal cancer cells at both the levels of cultured cells and xenograft tumors in immunodeficient mice, and accumulated AXIN to decrease beta-catenin and downregulate the target gene expression as pharmacodynamic biomarkers. Based on these findings, RK-582 is thought to have potential as a new treatment for colorectal cancer patients. At present, however, the efficacy and safety of RK-582 in humans have not been confirmed. Thus, this clinical trial is conducted with the aim of investigating the tolerability and safety of RK-582 for patients with unresectable advanced or recurrent colorectal cancer as a first-in-human trial, in which RK-582 is administered to humans for the first time.
CONDITIONS
Official Title
Study of a Tankyrase Inhibitor RK-582 for Patients With Unresectable Metastatic Colorectal Cancer
Who Can Participate
Eligibility Criteria
You may qualify if you...
- Patients with histologically or cytologically diagnosed colorectal cancer
- Patients who are refractory or intolerant to standard treatment for unresectable advanced or recurrent colorectal cancer
- Patients with measurable disease according to RECIST guideline ver 1.1
- Patients who are able to take capsules orally
You will not qualify if you...
- Patients with clinically relevant gastrointestinal, hepatic, musculoskeletal, respiratory, cerebral/cardiovascular, hematologic, oncologic, endocrine, immunologic, psychiatric, neurologic, or genitourinary diseases, or patients with conditions that threaten safety or affect study outcomes
- Patients with medical history of interstitial lung disease
- Patients with chronic nausea, vomiting or diarrhea that may interfere with oral administration of the investigational drug
- Patients with pulmonary embolism or central deep vein thrombosis
- Patients receiving treatment with strong CYP3A4 inhibitors or inducers
- Patients diagnosed and treated for osteoporosis or with bone mineral density less than T-score -2.5 at screening
- Patients with obvious bone metastases in long bones, vertebrae, or other weight-bearing parts of the legs
AI-Screening
AI-Powered Screening
Complete this quick 3-step screening to check your eligibility
Trial Site Locations
Total: 1 location
1
Cancer Institute Hospital of JFCR
Koto-ku, Tokyo, Japan, 135-8550
Actively Recruiting
Research Team
E
Eiji Shinozaki
CONTACT
How is the study designed?
Study Type
INTERVENTIONAL
Masking
NONE
Allocation
NA
Model
SINGLE_GROUP
Primary Purpose
TREATMENT
Number of Arms
1
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