galunisertib + temozolomide

Galunisertib + temozolomide is an investigational drug combination studied primarily in patients with malignant glioma, including glioblastoma. Galunisertib is an oral small molecule inhibitor of transforming growth factor-beta receptor I kinase (TGF-βRI/ALK5), which blocks TGF-β signaling and downregulates SMAD2 phosphorylation, thereby inhibiting tumor proliferation, invasion, metastasis, and immune evasion[1][2][3]. Temozolomide is an oral alkylating agent that induces DNA damage leading to tumor cell death and is a standard chemotherapeutic agent used in gliomas[8]. The combination has been evaluated in clinical trials alongside radiotherapy to assess safety, tolerability, pharmacodynamics, and efficacy. In a Phase 1b/2a trial in newly diagnosed malignant glioma patients receiving radiochemotherapy with temozolomide plus galunisertib versus standard therapy alone, no significant differences were observed in efficacy or safety between arms[1][4].

Brand names

galunisertibtemozolomide

Other names

LY2157299 monohydrateLY-2157299 monohydrateLY 2157299 monohydrateTMZ