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Cited by 554

The DOI matches its Crossref record; 154 of the 154 references it cites were found in a registry or an index.

Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

Open access
Lahn, Michael, Herbertz, Stephan, Sawyer, J. Scott, Stauber, Anja J, Gueorguieva, Ivelina, Driscoll, Kyla E, Estrem, Shawn T, Cleverly, Ann L, Desaiah, Durisala, Guba, Susan C, Benhadji, Karim A, Slapak, Christopher A·2015·Drug Design, Development and Therapy
DOI 10.2147/dddt.s86621
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Abstract

Transforming growth factor-beta (TGF-β) signaling regulates a wide range of biological processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks of cancer, including tumor proliferation, invasion and metastasis, inflammation, angiogenesis, and escape of immune surveillance. There are several pharmacological approaches to block TGF-β signaling, such as monoclonal antibodies, vaccines, antisense oligonucleotides, and small molecule inhibitors. Galunisertib (LY2157299 monohydrate) is an oral small molecule inhibitor of the TGF-β receptor I kinase that specifically downregulates the phosphorylation of SMAD2, abrogating activation of the canonical pathway. Furthermore, galunisertib has antitumor activity in tumor-bearing animal models such as breast, colon, lung cancers, and hepatocellular carcinoma. Continuous long-term exposure to galunisertib caused cardiac toxicities in animals requiring adoption of a pharmacokinetic/pharmacodynamic-based dosing strategy to allow further development. The use of such a pharmacokinetic/pharmacodynamic model defined a therapeutic window with an appropriate safety profile that enabled the clinical investigation of galunisertib. These efforts resulted in an intermittent dosing regimen (14 days on/14 days off, on a 28-day cycle) of galunisertib for all ongoing trials. Galunisertib is being investigated either as monotherapy or in combination with standard antitumor regimens (including nivolumab) in patients with cancer with high unmet medical needs such as glioblastoma, pancreatic cancer, and hepatocellular carcinoma. The present review summarizes the past and current experiences with different pharmacological treatments that enabled galunisertib to be investigated in patients.

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Metadata

Authors
Lahn, M., Herbertz, S., Sawyer, J. S., Stauber, A. J., Gueorguieva, I., Driscoll, K. E., Estrem, S. T., Cleverly, A. L., Desaiah, D., Guba, S. C., Benhadji, K. A., & Slapak, C. A.
Venue
Drug Design, Development and Therapy
Publisher
Informa UK Limited
Published
2015-08
Volume
9
Pages
4479
ISSN
1177-8881 (ISSN-L)
DOI
10.2147/dddt.s86621
OpenAlex
W1700691315
Cited by
554
References
154
FWCI
18.65
Type
journal article
Language
en
Open access
gold

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CoChat. (2026). Citation check: Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. https://app.cochat.ai/papers/10.2147/dddt.s86621
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Lahn, M., Herbertz, S., Sawyer, J. S., Stauber, A. J., Gueorguieva, I., Driscoll, K. E., Estrem, S. T., Cleverly, A. L., Desaiah, D., Guba, S. C., Benhadji, K. A., & Slapak, C. A. (2015). Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug Design, Development and Therapy. https://doi.org/10.2147/dddt.s86621

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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.

Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.