Drug intelligence / Profile preview

irinotecan + rapamycin

Development stage
Phase 1
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Irinotecan + rapamycin is a combination therapy that targets multiple pathways in cancer cells. This combination specifically targets the mTOR/HIF-1α axis, with rapamycin inhibiting the mammalian target of rapamycin (mTOR) and irinotecan inhibiting topoisomerase I and preventing the accumulation of HIF-1α. Studies have shown that this combination demonstrates synergistic effects in various cancer models, particularly in colon cancer and pancreatic cancer. The combination has shown potent inhibition of tumor growth in xenografted models, with dramatic reduction in tumor volume compared to single-agent therapy. In hypoxic conditions, the combination induces massive cancer cell death, suggesting its effectiveness is mediated through HIF-1α inhibition rather than through genotoxic lesions.

02

Targets

TOP1 (DNA Topoisomerase I)Mechanistic target of rapamycin complex 1HIF1A (Hypoxia-inducible factor 1-alpha)

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