Geftinib

Gupta, Ajay; Raina, Vinod

doi:10.4103/0973-1482.73330

Cited by 9 publications

(4 citation statements)

References 41 publications

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“…Thus, the most targeted area of developing antineoplastic drugs is through the inhibition of EGFR and VEGFR signaling. This therapeutic strategy in oncology has been successful using biologics, cetuximab [26] and ramucirumab [27], as well as small molecules such as gefitinib [28], vandetanib [8], sorafenib, sunitinib [1]. As an example, the direct inhibition of VEGFR-2 tyrosine kinase activity with a small molecule (sorafenib and sunitinib) has been recently approved by the FDA for the treatment of renal cell cancer.…”

Section: Discussionmentioning

confidence: 99%

Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells

Bocci¹,

Fioravanti²,

Motta³

et al. 2011

Biochemical Pharmacology

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Aims. To demonstrate the antiproliferative and pro-apoptotic activity of the novel pyrazolopyrimidine derivative multiple tyrosine kinase inhibitor CLM3, alone and in combination with SN-38 (the active metabolite of irinotecan), on endothelial and tumour cells and to show its mechanism of action.Methods. Proliferation and apoptotic assays were performed on microvascular endothelial (HMVECd) and lung (A549) and thyroid cancer (8305C, TT) cell lines exposed to CLM3 and to the simultaneous combination with SN38 for 72h. Cell-based phospho-VEGFR-2, phospho-EGFR and phospho-RET inhibition assays were performed and ERK1/2 and Akt phosphorylation were quantified by ELISA kits. Conclusions.The pyrazolopyrimidine derivative CLM3 demonstrated a highly significant and promising antiproliferative and proapoptotic activity, alone and in combination with SN-38, for activated endothelial and cancer cell cells. These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signalling pathways.

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Section: Discussionmentioning

confidence: 99%

Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells

Bocci¹,

Fioravanti²,

Motta³

et al. 2011

Biochemical Pharmacology

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“…Approximately one third of patients with gefitinib-induced ILD died. The median time to onset of gefitinib-associated ILD was 24 days in Japan and 42 days in America (7). To prevent exacerbation of ILD, early diagnosis and the withdrawal of gefitinib are required, and early administration of high-dose glucocorticoids generally presents curative effects.…”

Section: Discussionmentioning

confidence: 99%

Gefitinib in combination with prednisolone to avoid interstitial lung disease during non-small cell lung cancer treatment: A case report

Xue

Liu

et al. 2013

Oncology Letters

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Gefitinib-induced interstitial lung disease (ILD) is a rare but lethal drug adverse event, which usually leads to the withdrawal of gefitinib and causes complications with anticancer treatment. In this study, gefitinib administration combined with prednisolone in a female with stage IIIb non-small cell lung cancer (NSCLC) produced a good outcome without inducing ILD. The results suggested that combined administration of gefitinib with glucocorticoids may be an efficient method to treat NSCLC while avoiding complications with ILD.

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“…Gefitinib (Iressa™; AstraZenca, London, UK) is the first selective inhibitor of the EGFR tyrosine kinase domain 84. Gefitinib used as monotherapy is an effective treatment for patients with locally advanced or metastatic nonsmall cell lung cancer (NSCLC) with EGFR mutations 85.…”

Section: Target Identification From Drug Action (Chemical Proteomics)mentioning

confidence: 99%

Advances in the proteomic discovery of novel therapeutic targets in cancer

Guo¹,

Zhang²,

Wang³

2013

DDDT

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Proteomic approaches are continuing to make headways in cancer research by helping to elucidate complex signaling networks that underlie tumorigenesis and disease progression. This review describes recent advances made in the proteomic discovery of drug targets for therapeutic development. A variety of technical and methodological advances are overviewed with a critical assessment of challenges and potentials. A number of potential drug targets, such as baculoviral inhibitor of apoptosis protein repeat-containing protein 6, macrophage inhibitory cytokine 1, phosphoglycerate mutase 1, prohibitin 1, fascin, and pyruvate kinase isozyme 2 were identified in the proteomic analysis of drug-resistant cancer cells, drug action, and differential disease state tissues. Future directions for proteomics-based target identification and validation to be more translation efficient are also discussed.

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Geftinib

Cited by 9 publications

References 41 publications

Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells

Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells

Gefitinib in combination with prednisolone to avoid interstitial lung disease during non-small cell lung cancer treatment: A case report

Advances in the proteomic discovery of novel therapeutic targets in cancer

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