Sorafenib for the treatment of breast cancer

Bronte, Giuseppe; Andreis, Daniele; Bravaccini, Sara; Maltoni, Roberta; Cecconetto, Lorenzo; Schirone, Alessio; Farolfi, Alberto; Fedeli, Anna; Serra, Patrizia; Donati, Caterina; Amadori, Dino; Rocca, Andrea

doi:10.1080/14656566.2017.1309024

Cited by 35 publications

(18 citation statements)

References 64 publications

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“…Multi-kinase inhibitors with activity against RET such as sorafenib, vandetanib, and others have been tested in clinical trials in unselected breast cancers with modest to no significant activity 60 , 61 . However, both the presence of the target, e.g.…”

Section: Discussionmentioning

confidence: 99%

RET rearrangements are actionable alterations in breast cancer

Chung²,

et al. 2018

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Fusions involving the oncogenic gene RET have been observed in thyroid and lung cancers. Here we report RET gene alterations, including amplification, missense mutations, known fusions, novel fusions, and rearrangements in breast cancer. Their frequency, oncogenic potential, and actionability in breast cancer are described. Two out of eight RET fusions (NCOA4-RET and a novel RASGEF1A-RET fusion) and RET amplification were functionally characterized and shown to activate RET kinase and drive signaling through MAPK and PI3K pathways. These fusions and RET amplification can induce transformation of non-tumorigenic cells, support xenograft tumor formation, and render sensitivity to RET inhibition. An index case of metastatic breast cancer progressing on HER2-targeted therapy was found to have the NCOA4-RET fusion. Subsequent treatment with the RET inhibitor cabozantinib led to a rapid clinical and radiographic response. RET alterations, identified by genomic profiling, are promising therapeutic targets and are present in a subset of breast cancers.

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Section: Discussionmentioning

confidence: 99%

RET rearrangements are actionable alterations in breast cancer

Chung²,

et al. 2018

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“…It has been used to study the pathogenic process of RA and to evaluate the effects of anti‐RA drugs (Kannan et al, ). Until now, sorafenib was mostly studied for its anticancer activities (Kim et al, ; Broecker‐Preuss et al, ; Zahavi et al, ; Branco et al, ; Bronte et al, ). In this study, we first unrevealed the anti‐arthritic effect of sorafenib (10, 20, and 40 mg/kg) in AA rats.…”

Section: Discussionmentioning

confidence: 99%

“…Early reports revealed the effects of sorafenib on immunity through the modulation of effector CD4+ and T cell function in tumor patients (Cabrera et al, ; Romero et al, ). Studies on sorafenib are primarily focused on antitumor activity and mechanisms (Kim et al, ; Broecker‐Preuss et al, ; Zahavi et al, ; Branco et al, ; Bronte et al, ). We investigated, for the first time, whether sorafenib exerts anti‐arthritic effect on RA in vivo .…”

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confidence: 99%

Antiarthritic Effects of Sorafenib in Rats with Adjuvant‐Induced Arthritis

Wang

Liu

Gong

et al. 2018

The Anatomical Record

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Rheumatoid arthritis (RA) is a chronic inflammatory disease affecting the synovial membrane of joints. In this study, we aimed to investigate whether sorafenib exerts antiarthritic effects on RA in vivo. Adjuvant arthritis (AA) was induced (day 0) in male Sprague-Dawley rats by intradermal injection of 0.1 mL of complete Freund's complete adjuvant into the left hind paw. Sorafenib (10, 20, or 40 mg/kg/day) was administered intragastrically from day 10 to 24. Body weight, paw volume, synovial inflammation, and tumor necrosis factor alpha (TNF-α), interleukin-1β (IL-1β), IL-10, and IL-17 serum levels were detected. In addition, microvascular density (MVD) and the expression of vascular endothelial growth factor receptor 2 (VEGFR-2) and fibroblast growth factor receptor 1 (FGFR-1) in synovial tissues were analyzed. Our data revealed that sorafenib administration led to significant body weight gain in AA rats but suppressed paw swelling, synovial hyperplasia, and inflammatory infiltration. Furthermore, it decreased TNF-α, IL-1β, and IL-17 serum levels and upregulated IL-10. MVD and VEGFR-2 and FGFR-1 expression in synovial tissues were significantly reduced. Thus, this study shows that sorafenib exerts anti-arthritic effects in AA rats and therefore has potential in RA treatment. Anat Rec, 301:1519-1526, 2018. © 2018 Wiley Periodicals, Inc.

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“…Paclitaxel, docetaxel, and doxorubicin are important anticancer drugs for the treatment of breast cancer, advanced renal cell carcinoma and other cancers. [1][2][3][4] However, chemotherapy often leads to the occurrence of multidrug resistance (MDR) in various tumor cells. 5 Impacts of anticancer drugs on MDR cancers might be greatly decreased due to the high expression of multidrug resistance-associated protein 2 (MRP2) transporting agents from tumor cells.…”

Section: Introductionmentioning

confidence: 99%

<p>In vitro Transport Ability of <em>ABCC2</em> (G1249A) Polymorphic Variant Towards Anticancer Drugs</p>

Guo

Yuan

Gao

2020

OTT

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Objective: Multidrug resistance-associated protein 2 (MRP2), encoded by ABCC2 gene, is involved in the efflux of certain anticancer drugs. Here we observed whether the ABCC2 (G1249A) polymorphism impacts the transport abilities of MRP2-dependent paclitaxel, docetaxel, and doxorubicin in recombinant LLC-PK1 cell lines. Methods: LLC-PK1 cell lines transfected with ABCC2 1249G wild-type and ABCC2 1249A variant alleles were used to evaluate the sensitivity, intracellular accumulation, and transmembrane transport of paclitaxel, docetaxel, and doxorubicin. Results: The recombinant ABCC2 1249A variant cell line showed higher IC 50 values for paclitaxel and doxorubicin than ABCC2 1249G wild-type cell system (p<0.01). Intracellular accumulations of paclitaxel and doxorubicin in cells transfected with ABCC2 1249A variant allele were significantly decreased compared to cells transfected with ABCC2 1249G wild-type allele (p<0.01). The efflux ratios of paclitaxel and doxorubicin across ABCC2 1249A cell line were significantly increased compared with ABCC2 1249G cell system (p<0.01). However, ABCC2 (G1249A) polymorphism had no effect on the transport activity of MRP2-mediated docetaxel. Conclusion: Our results indicate that ABCC2 (G1249A) polymorphism affects the transport activities of MRP2-dependent paclitaxel and doxorubicin, resulting in greater efflux of these anticancer drugs.

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Sorafenib for the treatment of breast cancer

Cited by 35 publications

References 64 publications

RET rearrangements are actionable alterations in breast cancer

RET rearrangements are actionable alterations in breast cancer

Antiarthritic Effects of Sorafenib in Rats with Adjuvant‐Induced Arthritis

<p>In vitro Transport Ability of <em>ABCC2</em> (G1249A) Polymorphic Variant Towards Anticancer Drugs</p>

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