Drug intelligence / Profile preview

nintedanib + pegylated liposomal doxorubicin + carboplatin

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of three agents: - **Nintedanib** is an oral small molecule tyrosine kinase inhibitor that targets multiple receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptors (FGFR), and platelet-derived growth factor receptors (PDGFR). It inhibits angiogenesis and tumor cell proliferation. Nintedanib is primarily developed for use in idiopathic pulmonary fibrosis and certain cancers. - **Pegylated liposomal doxorubicin** (PLD) is a formulation of the anthracycline antibiotic doxorubicin encapsulated in pegylated liposomes to reduce cardiotoxicity while maintaining antitumor efficacy. Its mechanism involves intercalation into DNA and inhibition of topoisomerase II activity leading to DNA damage and apoptosis. The pegylation prolongs circulation time and alters tissue distribution[4][8]. - **Carboplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks resulting in inhibition of DNA synthesis and function. The combination of PLD with carboplatin has demonstrated efficacy in recurrent ovarian cancer[1][2][6]. The addition of nintedanib introduces antiangiogenic effects to the cytotoxic backbone.

Brand names
DoxilLipodox
Other names
BIBF 1120BIBF1120BIBF-1120
02

Targets

PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)TOP2A (DNA topoisomerase II)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)

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