• Alias: LY2157299
    • An orally available, small-molecule antagonist of the tyrosine kinase TGF-β receptor type 1 (TGFβR1) that specifically targets and binds to the kinase domain of TGFβR1, thereby preventing the activation of TGF-β-mediated signaling pathways. This may inhibit the proliferation of TGF-β-overexpressing tumor cells.
    • Phase 2 in combination with enzalutamide in metastatic, castrate-resistant prostate cancer; phase 1b/2 in combination with nivolumab in recurrent and refractory HCC and NSCLC; phase 1b/2 in combination with paclitaxel in triple-negative breast cancer; phase 1b in combination with durvalumab in metastatic pancreatic cancer.
    • Recommended phase 2 dose:
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