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Drug intelligence / Profile preview
romidepsin + gemcitabine
- Development stage
- Phase 2
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Romidepsin + gemcitabine is an investigational combination therapy consisting of two small molecule drugs with distinct mechanisms of action. Romidepsin is a histone deacetylase (HDAC) inhibitor that induces cell cycle arrest and apoptosis by altering gene expression through epigenetic modulation. It is FDA-approved for the treatment of T-cell lymphoma. Gemcitabine is a nucleoside analog and antimetabolite that inhibits DNA synthesis, leading to cell death in rapidly dividing cells. The combination has been studied in various advanced solid tumors and hematologic malignancies—including pancreatic cancer, urothelial carcinoma, and lymphomas—where it aims to enhance anti-tumor efficacy by targeting both epigenetic regulation (romidepsin) and DNA replication (gemcitabine). Preclinical studies suggest synergistic effects via increased apoptosis mediated by reactive oxygen species generation and caspase activation[2][6].
- Other names
- depsipeptide + gemcitabine
02
Targets
POLA1 (DNA polymerase alpha)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)RRM1
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