Linifanib

doi:10.2165/11584520-000000000-00000

Cited by 16 publications

(2 citation statements)

References 12 publications

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“…Its inhibition has been found to stop transformation, proliferation, migration, differentiation, and metastasis of cancer cells. To improve the efficacy of Abbott’s Linifanib, 61 Shi et al reported a diaryl-urea with isoxazol[3,4-b]pyridine-3-amino-derivative 62 with inhibition potentials of 4 nM, 3 nM, and 8 nM against fms related receptor tyrosine kinase 3 (FLT3), kinase insert domain receptor (KDR), and platelet-derived growth factor receptor beta (PDGFR-β), respectively [ 69 , 70 ]. In another study, Jinfeng Wang and co-workers discovered two triple inhibition chemotypes, 63 and 64 ( Figure 6 ) from screening of these compounds derived from reaction between biphenyl-aryl urea and salicylaldoxime [ 71 ].…”

Section: Heterocyclic Compoundsmentioning

confidence: 99%

Synthetic and Naturally Occurring Heterocyclic Anticancer Compounds with Multiple Biological Targets

et al. 2021

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Cancer is a complex group of diseases initiated by abnormal cell division with the potential of spreading to other parts of the body. The advancement in the discoveries of omics and bio- and cheminformatics has led to the identification of drugs inhibiting putative targets including vascular endothelial growth factor (VEGF) family receptors, fibroblast growth factors (FGF), platelet derived growth factors (PDGF), epidermal growth factor (EGF), thymidine phosphorylase (TP), and neuropeptide Y4 (NY4), amongst others. Drug resistance, systemic toxicity, and drug ineffectiveness for various cancer chemo-treatments are widespread. Due to this, efficient therapeutic agents targeting two or more of the putative targets in different cancer cells are proposed as cutting edge treatments. Heterocyclic compounds, both synthetic and natural products, have, however, contributed immensely to chemotherapeutics for treatments of various diseases, but little is known about such compounds and their multimodal anticancer properties. A compendium of heterocyclic synthetic and natural product multitarget anticancer compounds, their IC50, and biological targets of inhibition are therefore presented in this review.

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Section: Heterocyclic Compoundsmentioning

confidence: 99%

Synthetic and Naturally Occurring Heterocyclic Anticancer Compounds with Multiple Biological Targets

et al. 2021

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“…To date, tumor regression in response to ABT-869 has been evaluated in multiple xenograft models 9 10 11 12 . Moreover, the clinical benefits of ABT-869 have been assessed in phase I to III trials in patients with non-small cell lung cancer, acute myeloid leukemia, colorectal cancer and hepatocellular carcinoma 13 . These trials have provided evidences for the safety and efficacy of ABT-869 treatment.…”

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confidence: 99%

Linifanib (ABT-869) Potentiates the Efficacy of Chemotherapeutic Agents through the Suppression of Receptor Tyrosine Kinase-Mediated AKT/mTOR Signaling Pathways in Gastric Cancer

Chen

Guo

Chen

et al. 2016

Sci Rep

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Gastric cancer, highly dependent on tumor angiogenesis, causes uncontrolled lethality, in part due to chemoresistance. Here, we demonstrate that linifanib (ABT-869), a novel multi-targeted receptor tyrosine kinase inhibitor, markedly augments cytotoxicity of chemotherapies in human gastric cancer. ABT-869 and chemotherapeutic agents exhibited a strong synergy to inhibit the viability of several gastric cancer cell lines, with combination index values ranging from 0.017 to 0.589. Additionally, the combination of ABT-869 and chemotherapeutic agents led to remarkable suppression of vascular endothelial growth factor (VEGF)-induced angiogenesis in vitro and in vivo. Importantly, in a preclinical gastric cancer xenograft mouse model, drug co-treatments led to increased mouse survival as well as a synergistic reduction in tumor size and the inhibition of tumor angiogenesis. Mechanistic studies further revealed that all of the co-treatments containing ABT-869 resulted in decreased activation of the VEGF receptor, the epidermal growth factor receptor and the insulin growth factor receptor. Inhibition of these receptor tyrosine kinases consequently attenuated the activation of the downstream AKT/mTOR signaling pathway both in cultured gastric cancer cells and in gastric cancer xenografts. Collectively, our findings suggest that the addition of ABT-869 to traditional chemotherapies may be a promising strategy for the treatment of human gastric cancer.

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Solid Form Development for Poorly Soluble Compounds

Mattei

Chen

et al. 2019

Chemical Engineering in the Pharmaceutical Industry

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Linifanib

Cited by 16 publications

References 12 publications

Synthetic and Naturally Occurring Heterocyclic Anticancer Compounds with Multiple Biological Targets

Synthetic and Naturally Occurring Heterocyclic Anticancer Compounds with Multiple Biological Targets

Linifanib (ABT-869) Potentiates the Efficacy of Chemotherapeutic Agents through the Suppression of Receptor Tyrosine Kinase-Mediated AKT/mTOR Signaling Pathways in Gastric Cancer

Solid Form Development for Poorly Soluble Compounds

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