Intérêt du pazopanib dans le traitement des cancers du rein et des sarcomes des tissus mous

Brotelle, Thibault; Bay, Jacques‐Olivier

doi:10.1684/bdc.2014.1981

Cited by 7 publications

(4 citation statements)

References 19 publications

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“…The FDA-approved drug pazopanib is effective against VEGFR inhibitors and used for the treatment of advanced renal cell carcinoma . Drug resistance and tumor relapsing have been reported in most patients who have received pazopanib .…”

Section: Dual Vascular Endothelial Growth Factor Receptor (Vegfr) And...mentioning

confidence: 99%

“…The FDA-approved drug pazopanib is effective against VEGFR inhibitors and used for the treatment of advanced renal cell carcinoma. 40 Drug resistance and tumor relapsing have been reported in most patients who have received pazopanib. 41 A report indicates that combination therapy using pazopanib and HDAC enhances antitumor efficacy and minimizes drug resistance.…”

Section: Dual Vascular Endothelial Growth Factor Receptor (Vegfr) And...mentioning

confidence: 99%

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Single Inhibitors versus Dual Inhibitors: Role of HDAC in Cancer

et al. 2023

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Due to the multimodal character of cancer, inhibition of two targets simultaneously by a single molecule is a beneficial and effective approach against cancer. Histone deacetylase (HDAC) was widely investigated as a novel category of anticancer drug targets due to its crucial role in various biological processes like cell-proliferation, metastasis, and apoptosis. Numerous HDAC inhibitors such as vorinostat and panobinostat are clinically approved but have limited usage due to their low efficacy, nonselectivity, drug resistance, and toxicity. Therefore, HDACs with a dual targeting ability have attracted great attention. The strategy of combining a HDAC inhibitor with other antitumor agents has been proved advantageous for combating the nonselectivity and drug resistivity problems associated with single-target drugs. Henceforth, we have highlighted dual-targeting inhibitors to target HDAC along with topoisomerase, receptor tyrosine kinase inhibitors, and the zeste homolog 2 enzyme. Our Review mainly focuses on the impact of the substituent effect along with the linker variation of well-known HDAC-inhibitor-conjugated anticancer drugs.

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Section: Dual Vascular Endothelial Growth Factor Receptor (Vegfr) And...mentioning

confidence: 99%

Section: Dual Vascular Endothelial Growth Factor Receptor (Vegfr) And...mentioning

confidence: 99%

Single Inhibitors versus Dual Inhibitors: Role of HDAC in Cancer

et al. 2023

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“…The vascular endothelial growth factor (VEGF)/vascular endothelial growth factor receptor (VEGFR) signaling pathway is one of the most important targets for antiangiogenesis and counts over 10 small molecule inhibitors and monoclonal antibodies adopted for the treatment of solid tumors . Pazopanib 63 (Figure ) is a multiple VEGFR inhibitor approved by the FDA for the treatment of advanced soft tissue sarcoma and advanced renal cell carcinoma .…”

Section: The Mtdl Approachmentioning

confidence: 99%

“…and monoclonal antibodies adopted for the treatment of solid tumors. [278][279][280] Pazopanib 63 ( Figure 6) is a multiple VEGFR inhibitor approved by the FDA for the treatment of advanced soft tissue sarcoma and advanced renal cell carcinoma. 281 Unfortunately, the clinical application of pazopanib 63 is limited by the insurgence of resistance and tumor relapse.…”

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confidence: 99%

Epigenetic polypharmacology: A new frontier for epi‐drug discovery

Tomaselli

Lucidi

Rotili

et al. 2019

Medicinal Research Reviews

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Recently, despite the great success achieved by the so‐called “magic bullets” in the treatment of different diseases through a marked and specific interaction with the target of interest, the pharmacological research is moving toward the development of “molecular network active compounds,” embracing the related polypharmacology approach. This strategy was born to overcome the main limitations of the single target therapy leading to a superior therapeutic effect, a decrease of adverse reactions, and a reduction of potential mechanism(s) of drug resistance caused by robustness and redundancy of biological pathways. It has become clear that multifactorial diseases such as cancer, neurological, and inflammatory disorders, may require more complex therapeutic approaches hitting a certain biological system as a whole. Concerning epigenetics, the goal of the multi‐epi‐target approach consists in the development of small molecules able to simultaneously and (often) reversibly bind different specific epi‐targets. To date, two dual histone deacetylase/kinase inhibitors (CUDC‐101 and CUDC‐907) are in an advanced stage of clinical trials. In the last years, the growing interest in polypharmacology encouraged the publication of high‐quality reviews on combination therapy and hybrid molecules. Hence, to update the state‐of‐the‐art of these therapeutic approaches avoiding redundancy, herein we focused only on multiple medication therapies and multitargeting compounds exploiting epigenetic plus nonepigenetic drugs reported in the literature in 2018. In addition, all the multi‐epi‐target inhibitors known in literature so far, hitting two or more epigenetic targets, have been included.

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