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cisplatin + gemcitabine + nintedanib
- Development stage
- Phase 1
- Lead developer
- Boehringer Ingelheim
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination regimen consisting of three drugs—cisplatin, gemcitabine, and nintedanib—used in oncology clinical research. - **Cisplatin** is a platinum-based chemotherapy agent that forms DNA crosslinks, leading to apoptosis in rapidly dividing cells. - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporation into DNA and inhibition of ribonucleotide reductase. - **Nintedanib** is an oral small molecule tyrosine kinase inhibitor targeting vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptors (FGFR), and platelet-derived growth factor receptors (PDGFR). Nintedanib blocks angiogenesis and tumor cell proliferation by inhibiting these pathways[2][3][4][6]. This combination has been explored in clinical trials for various solid tumors, including non-small cell lung cancer (NSCLC) and malignant pleural mesothelioma[7]. While nintedanib is approved for use with docetaxel in NSCLC adenocarcinoma after first-line chemotherapy failure[2][3][4], its use with cisplatin plus gemcitabine remains investigational.
- Other names
- nintedanib + gemcitabine + cisplatin
02
Targets
DNADNA polymerase familyFGFR (FGFR family)PDGFRA (Platelet-derived growth factor receptor alpha)RNR (Ribonucleotide reductase)VEGFR (VEGFR family)
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