LY-2157299

01/01/2021 - "We further simulated the molecular docking of Galunisertib, a small molecule inhibitor targeting TGFβ signaling in cancer, which is currently undergoing FDA-approved clinical trials. "
06/19/2020 - "Our findings can provide the basis for further preclinical and clinical studies of the combination of Galunisertib and CAR T cells in the treatment of solid tumors."
09/05/2019 - "Galunisertib is an anti-cancer drug currently evaluated in phase I and II clinical trials. "
01/23/2018 - "Galunisertib has been tested in several clinical studies with evidence of anti-tumor activity observed in subsets of patients. "
01/01/2013 - "This study supports the use of LY2157299 in clinical trials, and presents new insights into TGF-β receptor cycling in cancer cells."

09/14/2022 - "After being applied to a rat model of MI, the galunisertib-loaded MN patch improved long-term cardiac function and reduced cardiac fibrosis by effectively inhibiting TGF-β depending on fibroblast activation. "
01/01/2021 - "Interestingly, AAV-shTGFβ1 accelerated the regeneration of fibrotic functional liver remnant and improved fibrosis, while LY2157299 only enhanced liver regeneration. "
06/15/2022 - "We induced fibrosis in human dermal fibroblasts with exogenous TGF-β and performed cellular proliferation assays after treatment with varying concentrations of galunisertib. "
09/01/2017 - "Fibrosis-related parameters, both transcriptional and translational level, were assessed after treatment with galunisertib. "
08/19/2023 - "Galunisertib also reduced inflammation and, more importantly, reduced the onset of fibrosis after 48 h of incubation. "

11/01/2019 - "Galunisertib exposure metrics for each patient in the GG arm (n = 99) of a phase 2 study of pancreatic cancer were calculated. "
11/01/2019 - "This analysis suggests that 300 mg/day galunisertib administered as 150 mg twice daily for 14 days on/14 days off treatment is an appropriate dosing regimen for patients with pancreatic cancer."
11/01/2018 - "The effect of galunisertib vs. placebo in patients with unresectable pancreatic cancer was determined. "
11/01/2018 - "Galunisertib-gemcitabine combination improved overall survival vs. gemcitabine in patients with unresectable pancreatic cancer, with minimal added toxicity. "
11/01/2018 - "Galunisertib plus gemcitabine vs. gemcitabine for first-line treatment of patients with unresectable pancreatic cancer."

01/01/2022 - "Notably, TGF-β signaling inhibitor LY 2157299 could effectively impede liver and peritoneal metastasis but not concurrently aggravate sepsis in those AIC-bearing nude mice. "
01/01/2019 - "Mechanistically, we found that KDM6B exerts its function by modulating the transforming growth factor-β1 (TGF-β1) expression, and TGF-β1 signal pathway inhibitor LY2157299 significantly inhibited KDM6B-induced proliferation, migration, metastasis, and EMT in ovarian cancer cells. "
06/01/2021 - "In mice, gemcitabine plus galunisertib treatment decreased metastases (p = 0.018), whereas galunisertib increased PD-L1 expression (p < 0.0001). "
01/01/2018 - "In a mouse liver metastases model of colon cancer, we observed significantly improved eradication of liver metastases in mice treated with adoptive NK cells combined with LY2157299 compared with mice receiving NK cells or TGF beta inhibition alone. "
01/01/2019 - "Importantly, combinatorial LY2157299 treatment sensitized PC cells to enzalutamide, leading to synergistic effects in inhibiting cell invasion in vitro and xenograft CRPC tumor growth and metastasis in vivo. "

07/01/2020 - "The results of the present study suggest that galunisertib may be an effective treatment for liver cirrhosis."
07/01/2020 - "Galunisertib treatment dose‑dependently prevented liver fibrosis, as demonstrated by the direct inhibition of α‑smooth muscle actin‑positive activated hepatic stellate cells (HSCs) after 8 weeks of CCl4 treatment. "
01/01/2018 - "In conclusion, TGF-β inhibition by galunisertib interferes, to some extent, with chronic liver progression, not by reducing the stage of liver fibrosis as measured by different scoring systems, but rather by modulating the biochemical composition of the deposited ECM, likely affecting the fate of non-parenchymal cells."
09/01/2017 - "Galunisertib is a drug that deserves to be further investigated for the treatment of liver fibrosis. "
09/01/2017 - "Here, we evaluated the potency of galunisertib in a human ex vivo model of liver fibrosis. "