Drug intelligence / Profile preview

ABT-869 + oxaliplatin + folinic acid + fluorouracil

Development stage
Unknown
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral (ABT-869), Intravenous (oxaliplatin, Folinic Acid, Fluorouracil)
01

Overview

This combination consists of **ABT-869 (linifanib)**, **oxaliplatin**, **folinic acid (leucovorin)**, and **fluorouracil (5-FU)**. - **ABT-869 (linifanib)** is an orally active, small molecule, multi-targeted tyrosine kinase inhibitor with potent antagonism of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) family kinases. Its primary mechanism of action is anti-angiogenesis (inhibiting tumor blood vessel formation), as well as direct antiproliferative effects on tumor cells, especially in cancers reliant on these pathways[1][5][6]. - **Oxaliplatin** is a platinum-based antineoplastic agent which forms DNA adducts, leading to cell-cycle arrest and apoptosis, primarily used in gastrointestinal cancers[4][6]. - **Folinic acid (leucovorin)** is not cytotoxic itself but potentiates the effects of fluorouracil by stabilizing binding of fluorouracil’s metabolite to thymidylate synthase, enhancing antitumor efficacy[4]. - **Fluorouracil (5-FU)** is a pyrimidine analog antimetabolite inhibiting thymidylate synthase (TS) and interfering with DNA and RNA synthesis[4][6]. This four-component regimen is not an approved product but may be used in research and investigational settings, typically in gastrointestinal (especially colorectal) cancers. Combining ABT-869 with standard chemotherapy regimens such as FOLFOX (oxaliplatin, folinic acid, fluorouracil) has been hypothesized to provide synergistic anticancer effects by targeting both angiogenesis and tumor cell proliferation[1][6].

Other names
ABT-869 + oxaliplatin + leucovorin + 5-fluorouracillinifanib + oxaliplatin + leucovorin + 5-FUABT-869 + FOLFOX
02

Targets

TS (Thymidylate synthase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TEK (Tie2)PDGFRB (Platelet-derived growth factor receptor beta)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)

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