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galunisertib + lomustine
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Galunisertib + lomustine is a combination therapy consisting of galunisertib, a small molecule inhibitor of the transforming growth factor-beta receptor type I (TGF-βRI/ALK5), and lomustine, an alkylating nitrosourea chemotherapeutic agent. Galunisertib acts by selectively inhibiting TGF-βRI kinase activity, thereby blocking TGF-β signaling pathways involved in tumor progression and immune evasion. Lomustine exerts its antitumor effects through DNA alkylation and cross-linking, leading to cell cycle arrest and apoptosis in rapidly dividing cells. This combination has been investigated primarily for the treatment of recurrent glioblastoma but did not demonstrate improved overall survival compared to standard therapies in clinical trials[1][2][3][5].
- Other names
- galunisertib + lomustineLY2157299 monohydrate + lomustine
02
Targets
ACVR1B (Activin A receptor type IB)DNATGFBR1
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