NCT06853496RecruitingPhase 1
Study of a Tankyrase Inhibitor RK-582 for Patients With Unresectable Metastatic Colorectal Cancer
Investigator-initiated Phase I Study of a Tankyrase Inhibitor RK-582 for Patients With Unresectable Metastatic Colorectal Cancer
Source: ClinicalTrials.gov · Last updated 29 Jul 2025 · Not updated for over 12 months - ask the site whether it is still open
Brief summary (registry, in English)
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.
- Status (registry)
- Recruiting
- Phase (registry)
- Phase 1
- Study type
- Interventional
- Enrollment
- 48 (estimated)
- First submitted
- 25 Feb 2025
- Start date
- 13 Mar 2025
- Primary completion date
- Mar 2027
- Lead sponsor
- Eiji Shinozaki
- Diseases
- Colorectal cancer
- NCT number
- NCT06853496
What you commit to
- Study type: Interventional · Phase 1
- Planned participants: 48
- From 13 Mar 2025 to the primary completion date, Mar 2027
- 1 site in 1 country
- Visits and tests: ask the trial team, the registry does not list them
Built from the registry fields of ClinicalTrials.gov. It describes the study, not your situation.
Who cannot take part
Copied verbatim from ClinicalTrials.gov and grouped by topic. Only the trial team decides who can take part.
Prior treatment
- Patients with chronic nausea, vomiting or diarrhea that may interfere with oral administration of the investigational drug
- Patients receiving treatment with strong CYP3A4 inhibitors or inducers.
Other illness
- Patients with clinically relevant gastrointestinal, hepatic, musculoskeletal, respiratory, cerebral/cardiovascular, hematologic, oncologic, endocrine, immunologic, psychiatric, neurologic, or genitourinary diseases, or patients with conditions that are judged to threaten the safety of the participant or to affect the outcome of this clinical trial by the investigators
- Patients with medical history of interstitial lung disease
- Patients with pulmonary embolism or central deep vein thrombosis.
Other
- Patients diagnosed and treated for osteoporosis or patients with a bone mineral density of less than T-score -2.5 at the time of screening
- Patients with obvious bone metastases in the long bones, vertebrae, or other parts of the leg where gravity is applied
Who the study is looking for
- 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
Age in the registry: 18 years to - · Sex: All · Does not accept healthy volunteers
Sites (1)
Sites in registry order. Pick your city on the disease page to sort them by distance.
| Site | City | Country | Site status |
|---|---|---|---|
| Cancer Institute Hospital of JFCR Coordinator of this site? Confirm its status | Koto-Ku | Japan | Recruiting |
This page is information, not medical advice. Discuss any trial with your doctor.