biostudies-literatureLieu CHDivision of Cancer Prevention, National Cancer Institute (DCP, NCI)Division of Cancer Prevention, National Cancer Institute1771-1778https://www.ebi.ac.uk/biostudies/studies/S-EPMC12498271biostudies-literatureUnknown5(10)<h4>Purpose</h4>The pathogenesis of colorectal cancer is largely driven by mutations of the tumor suppressor gene APC (adenomatous polyposis coli) that lead to aberrant activation of the β-catenin-dependent (canonical) Wnt signaling pathway. We evaluated basroparib, a tankyrase-selective inhibitor targeting the Wnt/β-catenin signaling pathway, in a first-in-human phase I clinical study for safety, tolerability, pharmacokinetics, and efficacy in patients with advance-stage solid tumors.<h4>Patients and methods</h4>Patients enrolled to this open-label, multicenter study (NCT04505839) were treated with basroparib capsules orally once daily in 28-day cycles (21-day on and 7-day off) in dose escalation at seven dose levels (30-360 mg) following the classic "3 + 3" design.<h4>Results</h4>Twenty-Cancer research communicationsA First-In-Human Dose-Escalation Phase I Study of Basroparib, a Tankyrase Inhibitor, in Patients with Advanced-Stage Solid Tumors.PMC124982712P30CA046934-34Kim UILieu CHKim SHLenz HJKim KSung MJBenson ABMeng XfalseA First-In-Human Dose-Escalation Phase I Study of Basroparib, a Tankyrase Inhibitor, in Patients with Advanced-Stage Solid Tumors.<h4>Purpose</h4>The pathogenesis of colorectal cancer is largely driven by mutations of the tumor suppressor gene APC (adenomatous polyposis coli) that lead to aberrant activation of the β-catenin-dependent (canonical) Wnt signaling pathway. We evaluated basroparib, a tankyrase-selective inhibitor targeting the Wnt/β-catenin signaling pathway, in a first-in-human phase I clinical study for safety, tolerability, pharmacokinetics, and efficacy in patients with advance-stage solid tumors.<h4>Patients and methods</h4>Patients enrolled to this open-label, multicenter study (NCT04505839) were treated with basroparib capsules orally once daily in 28-day cycles (21-day on and 7-day off) in dose escalation at seven dose levels (30-360 mg) following the classic "3 + 3" design.<h4>Results</h4>Twenty-2025-01-01T00:00:00Z2025 Oct2026-06-04T05:44:01.722Z2026-05-05T03:13:09.515ZS-EPMC124982714096496610.1158/2767-9764.CRC-25-0502