A First-In-Human Dose-Escalation Phase I Study of Basroparib, a Tankyrase Inhibitor, in Patients with Advanced-Stage Solid Tumors
Tankyrase in the active β-catenin-dependent (canonical) Wnt signaling pathway has been a desirable but difficult target because of safety concerns. We developed a tankyrase-selective inhibitor, basroparib, and successfully introduced it in a first-in-human study. This study demonstrated a favorable safety profile and modest antitumor activity for basroparib and suggests that basroparib may play a role when combined with other rational targeted therapies.
Authors
- Christopher H. Lieu (ORCID: https://orcid.org/0000-0002-4852-4642)
- Al B. Benson (ORCID: https://orcid.org/0000-0001-5485-7227)
- Moo Je Sung
- Heinz‐Josef Lenz (ORCID: https://orcid.org/0000-0003-2178-9568)
- Uk-Il Kim
- Song Hyun Kim
- Kyungjin Kim (ORCID: https://orcid.org/0000-0002-7128-7374)
- Xue Meng
Institutions
- University of Southern California (US)
- Korea Pharma (South Korea) (KR)
- USC Norris Comprehensive Cancer Center (US)
- University of Colorado Cancer Center (US)
- Northwestern Medicine (US)
- Robert H. Lurie Comprehensive Cancer Center of Northwestern University
- University of Colorado Denver (US)
Publication Details
- Journal
- Cancer Research Communications
- Published
- 2025-09-18
- DOI
- https://doi.org/10.1158/2767-9764.crc-25-0502
- Primary Topic
- Wnt/β-catenin signaling in development and cancer
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Division of Cancer Prevention, National Cancer Institute
- BeiGene
- National Institutes of Health
- Genentech
- National Cancer Institute