Study of a Tankyrase Inhibitor RK-582 for Patients With Unresectable Metastatic Colorectal
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 tankyras
| Condition(s) | Unresectable Colorectal Neoplasm Metastasis |
|---|---|
| Status | Recruiting |
| Phase | Phase 1 |
| Study type | Interventional |
| Summary | 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/ |
| Who can participate | Inclusion Criteria: * 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 Exclusion Criteria: * 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 * Pati |
| Ages | 18 Years |
| Sex | All |
| Lead sponsor | Eiji Shinozaki |
| Locations | Koto-ku, Tokyo, Japan |
| Start date | 2025-03-13 |
| NCT ID | NCT06853496 |
| Official listing | https://clinicaltrials.gov/study/NCT06853496 |