Case Series of Cancer Patients Treated With Galunisertib, a Transforming Growth Factor-Beta Receptor I Kinase Inhibitor in a First-in-Human Dose Study

Analia Azaro, Jordi Rodon, Michael Carducci, Juan M. Sepulveda-Sanchez, Ivelina Gueorguieva, Ann L. Cleverly, Durisala Desaiah, Sokalingum P. Namaseevayam, Matthias Holdhoff, Michael M. Lahn


Galunisertib (LY2157299 monohydrate) is a first-in-class small molecule inhibitor (SMI) of the transforming growth factor-beta (TGF-beta) signaling pathway. Some adverse events were associated with galunisertib during the first-in-human dose (FHD) study. Among these adverse events (n = 11) were four cases of infection, two cases of thromboembolic events and two cases of thrombocytopenia. In one of the patients with thromboembolic events, an autopsy was also performed to examine possible changes of the aorta. No significant histopathologic changes were observed. Single cases of grade 2 diarrhea (only associated with drug intake), stroke (after resection for relapsed glioma), and pre-existing co-primary tumor (possible colorectal cancer) were observed. Because TGF-beta plays an important role in tissue homeostasis and in immune response regulation, the present case series may serve as a future reference for adverse events observed in subsequent clinical trials with galunisertib.

J Med Cases. 2014;5(11):603-609


TGF-beta Inhibitor; Galunisertib; First-in-human study; Glioma; Adverse events; Case reports

Full Text: HTML PDF

Browse  Journals  


Journal of Clinical Medicine Research

Journal of Endocrinology and Metabolism

Journal of Clinical Gynecology and Obstetrics


World Journal of Oncology

Gastroenterology Research

Journal of Hematology


Journal of Medical Cases

Journal of Current Surgery

Clinical Infection and Immunity


Cardiology Research

World Journal of Nephrology and Urology

Cellular and Molecular Medicine Research


Journal of Neurology Research

International Journal of Clinical Pediatrics



Journal of Medical Cases, monthly, ISSN 1923-4155 (print), 1923-4163 (online), published by Elmer Press Inc.                     
The content of this site is intended for health care professionals.
This is an open-access journal distributed under the terms of the Creative Commons Attribution-NonCommercial 4.0 International License, which permits unrestricted
non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
Creative Commons Attribution license (Attribution-NonCommercial 4.0 International CC-BY-NC 4.0)

This journal follows the International Committee of Medical Journal Editors (ICMJE) recommendations for manuscripts submitted to biomedical journals,
the Committee on Publication Ethics (COPE) guidelines, and the Principles of Transparency and Best Practice in Scholarly Publishing.

website:   editorial contact:
Address: 9225 Leslie Street, Suite 201, Richmond Hill, Ontario, L4B 3H6, Canada

© Elmer Press Inc. All Rights Reserved.

Disclaimer: The views and opinions expressed in the published articles are those of the authors and do not necessarily reflect the views or opinions of the editors and Elmer Press Inc. This website is provided for medical research and informational purposes only and does not constitute any medical advice or professional services. The information provided in this journal should not be used for diagnosis and treatment, those seeking medical advice should always consult with a licensed physician.