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Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW, Desaiah D, Lahn MM, Benhadji KA, Lallena MJ, Holmgaard RB, Xu X, Zhang F, Manro JR, Iversen PW, Iyer CV, Brekken RA, Kalos MD, Driscoll KE. Yingling JM, et al. Among authors: holmgaard rb. Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23. Oncotarget. 2017. PMID: 29467918 Free PMC article.
Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade.
Holmgaard RB, Schaer DA, Li Y, Castaneda SP, Murphy MY, Xu X, Inigo I, Dobkin J, Manro JR, Iversen PW, Surguladze D, Hall GE, Novosiadly RD, Benhadji KA, Plowman GD, Kalos M, Driscoll KE. Holmgaard RB, et al. J Immunother Cancer. 2018 Jun 4;6(1):47. doi: 10.1186/s40425-018-0356-4. J Immunother Cancer. 2018. PMID: 29866156 Free PMC article.
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