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Clinical Trials in Japan / NCT06853496
Recruiting Phase 1

Study of a Tankyrase Inhibitor RK-582 for Patients With Unresectable Metastatic Colorectal Cancer

NCT06853496 · tracked via the Priya Life Science Japan tracker
Sponsor
Eiji Shinozaki
Phase
Phase 1
Started
2025-03-13
Last updated
2025-07-29

Condition(s) studied

Unresectable Colorectal Neoplasm Metastasis

Investigational drug(s) / intervention(s)

RK-582

RK-582: Dosing Frequency: Do single dose of RK-582 at the dose level specified for the cohort. Seven days after the first dose, Start repeated daily dose and continue until discontinuation criteria were met. Dose level per dose: Dose Level 1: 5 mg BID Dose level 2: 10 mg QD Dose level 3: 20 mg QD Dose level 4: 40 mg QD Dose Level 5: 60 mg QD Dose Level 6: 80 mg QD Dose Level 7: 100 mg QD Dose Level 8: 200 mg QD

Study 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/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.

Eligibility

Sex
ALL
Min age
18 Years
Max age
—
Healthy volunteers
No
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 * 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 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

Primary outcome measure(s)

  • Percentage of dose-limiting toxicity — 35 days after the first dose of RK-582
  • Number of participants with adverse events as assessed by CTCAE v5.0 — Approximately 1 year after the first dose of RK-582

Trial sites (1)

FacilityCityRegionStatus
Cancer Institute Hospital of JFCR Koto-ku Tokyo Recruiting
Official registry record

This page summarises publicly available registry data for informational purposes — not medical advice. Eligibility is determined by each study team; patients should discuss participation with their clinician.

View NCT06853496 on ClinicalTrials.gov ↗ ← All trials in Japan