A First-In-Human Dose-Escalation Phase I Study of Basroparib, a Tankyrase Inhibitor, in Patients with Advanced-Stage Solid Tumors.

ABSTRACT:

Purpose

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.

Patients and methods

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.

Results

Twenty-

SUBMITTER: Lieu CH 

PROVIDER: S-EPMC12498271 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature