Osimertinib: First Global Approval

Drugs, Год журнала: 2016, Номер 76(2), С. 263 - 273

Опубликована: Янв. 4, 2016

Язык: Английский

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The association between PD-L1 and EGFR status and the prognostic value of PD-L1 in advanced non-small cell lung cancer patients treated with EGFR-TKIs

Oncotarget, Год журнала: 2015, Номер 6(16), С. 14209 - 14219

Опубликована: Март 29, 2015

// Yanna Tang 1,2,3 ,* , Wenfeng Fang Yaxiong Zhang Shaodong Hong Shiyang Kang Yue Yan Nan Chen Jianhua Zhan Xiaobo He Tao Qin Ge Li 4 Wenyi 5 Peijian Peng and 1 Department of Medical Oncology, Sun Yat-sen University Cancer Center, Guangzhou, China 2 State Key Laboratory Oncology in South China, 3 Collaborative Innovation Center for Medicine, Stem Cells Tissue Engineering, University, The Fifth Affiliated Hospital Yat-Sen Zhu Hai, * These authors have contributed equally to this work Correspondence to: Zhang, email: Peng, Keywords : NSCLC, PD-L1, EGFR status, TKI, prognosis Received January 08, 2015 Accepted March 01, Published 29, Abstract Backgrounds: Recent clinical trials shown that immune-checkpoint blockade yields remarkable response a subset non–small cell lung cancer (NSCLC) patients. However, few studies directly focus on the association between epidermal growth factor receptor (EGFR) mutational status programmed death-ligand (PD-L1) expression. We examined whether PD-L1 is related clinicopathologic factors patients with advanced NSCLC treated EGFR-tyrosine kinase inhibitors (EGFR-TKIs). Methods: One-hundred seventy were explored. Paraffin-embedded tumour sections stained antibody. mutation was by fluorescent quantitative polymerase chain reaction (PCR). correlations expression survival parameters analyzed. Results: overall frequency over-expression 65.9% (112/170). In adenocarcinoma, tended be associated mutant (PD-L1 overexpression wild-type EGFR, 64/89 (71.9%) vs. 32/56 (57.1%), respectively; p=0.067). Subgroup analyses showed high significantly shorter (OS) (p=0.029) but not (p=0.932) EGFR-TKIs. Even more, patients, higher might only signal better outcome TKIs. Conclusions: High likely presence adenocarcinoma. For over can considered as poor prognostic indicator OS.

Язык: Английский

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Signaling Pathways in Cancer: Therapeutic Targets, Combinatorial Treatments, and New Developments

Cells, Год журнала: 2021, Номер 10(3), С. 659 - 659

Опубликована: Март 16, 2021

Molecular alterations in cancer genes and associated signaling pathways are used to inform new treatments for precision medicine cancer. Small molecule inhibitors monoclonal antibodies directed at relevant cancer-related proteins have been instrumental delivering successful of some blood malignancies (e.g., imatinib with chronic myelogenous leukemia (CML)) solid tumors tamoxifen ER positive breast trastuzumab HER2-positive cancer). However, inherent limitations such as drug toxicity, well acquisition de novo or acquired mechanisms resistance, still cause treatment failure. Here we provide an up-to-date review the successes current targeted therapies highlight how recent technological advances provided a level understanding molecular complexity underpinning resistance therapies. We also raise three basic questions concerning discovery based on markers selected pathways, further discuss combination may become preferable approach over monotherapy treatments. Finally, consider novel therapeutic developments that complement delivery significantly improve clinical response outcomes patients.

Язык: Английский

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Renal Drug Transporters and Drug Interactions

Clinical Pharmacokinetics, Год журнала: 2017, Номер 56(8), С. 825 - 892

Опубликована: Фев. 16, 2017

Язык: Английский

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Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis

Journal of Medicinal Chemistry, Год журнала: 2021, Номер 65(2), С. 1047 - 1131

Опубликована: Окт. 8, 2021

The central role of dysregulated kinase activity in the etiology progressive disorders, including cancer, has fostered incremental efforts on drug discovery programs over past 40 years. As a result, inhibitors are today one most important classes drugs. FDA approved 73 small molecule inhibitor drugs until September 2021, and additional were by other regulatory agencies during that time. To complement published literature clinical inhibitors, we have prepared review recaps this large data set into an accessible format for medicinal chemistry community. Along with therapeutic pharmacological properties each across world 2020, provide synthesis routes originally used phase, many which only available patent applications. In last section, also update 2021.

Язык: Английский

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Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma

Nature Medicine, Год журнала: 2016, Номер 22(3), С. 270 - 277

Опубликована: Фев. 8, 2016

Язык: Английский

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Long non-coding RNA UCA1 induces non-T790M acquired resistance to EGFR-TKIs by activating the AKT/mTOR pathway in EGFR-mutant non-small cell lung cancer

Oncotarget, Год журнала: 2015, Номер 6(27), С. 23582 - 23593

Опубликована: Июнь 8, 2015

// Ningning Cheng 1,* , Weijing Cai Shengxiang Ren 1 Xuefei Li 2 Qi Wang Hui Pan Mingchuan Zhao Jiayu Yishi Zhang Chao Xiaoxia Chen Ke Fei 3 Caicun Zhou and Fred R. Hirsch 4 Department of Medical Oncology, Shanghai Pulmonary Hospital, Tongji University, University School Cancer Institute, Shanghai, P. China Lung Immunology, Thoracic Surgery, Pathology, Colorado Center, Aurora, Colorado, USA * These authors have contributed equally to this work Correspondence to: Zhou, email: Keywords : UCA1, EGFR-TKIs, acquired resistance, non-small cell lung cancer Received February 09, 2015 Accepted June 01, Published 08, Abstract The aim study was explore the role long non-coding RNA UCA1 (urothelial cancer-associated 1) in resistance epidermal growth factor receptor tyrosine kinase inhibitors ( EGFR -TKIs) -mutant (NSCLC). In our study, expression significantly increased cells patients with -TKIs. Over-expression associated a shorter progression-free survival (PFS) [13.0 vs . 8.5 months, P < 0.01] tumors respond significant relationship not observed T790M mutation (10.5 12.0 = 0.778), but non-T790M (19.0 vs. 9.0 0.023). knockdown restored gefitinib sensitivity resistant inhibited activation AKT/mTOR pathway epithelial-mesenchymal transition (EMT). mTOR inhibitor effective -expressing PC9/R. Inhibiting could change although there no difference. conclusion, influence over-expression on PFS for -TKIs from subgroup mutation. may induce by activating EMT.

Язык: Английский

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Olmutinib: First Global Approval

Drugs, Год журнала: 2016, Номер 76(11), С. 1153 - 1157

Опубликована: Июнь 28, 2016

Язык: Английский

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Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance

European Journal of Medicinal Chemistry, Год журнала: 2017, Номер 142, С. 32 - 47

Опубликована: Май 12, 2017

Язык: Английский

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Repurposing of Kinase Inhibitors for Treatment of COVID-19

Pharmaceutical Research, Год журнала: 2020, Номер 37(9)

Опубликована: Авг. 10, 2020

Язык: Английский

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