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carboplatin + enzastaurin + pemetrexed
- Development stage
- Discontinued
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination chemotherapy regimen that includes carboplatin (a platinum-based chemotherapy agent), enzastaurin (an oral serine/threonine kinase inhibitor targeting protein kinase C-beta and the phosphatidylinositol-3-kinase/AKT pathway), and pemetrexed (an antifolate metabolic inhibitor). The combination was studied in clinical trials for the treatment of advanced non-small cell lung cancer (NSCLC). Clinical trials have shown that enzastaurin did not add to the activity of pemetrexed-carboplatin, and this specific three-drug combination does not warrant further study in NSCLC based on trial results.
02
Targets
GSK3 (Glycogen synthase kinase 3 beta)GART (GAR transformylase)PRKCG (Protein kinase C gamma)PRKCA (Protein kinase C alpha)DHFR (Dihydrofolate reductase)ABCB1 (P-glycoprotein)DNAPRKCB (Protein kinase C beta)PRKCE (Protein Kinase C epsilon)ABCG2 (Breast cancer resistance protein)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)TS (Thymidylate synthase)
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