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Anaplastic thyroid carcinoma.

Thyroid cancers represent about 1% of all human cancers. Differentiate thyroid carcinomas (DTCs), papillary and follicular cancers, are the most frequent forms, instead Anaplastic Thyroid Carcinoma (ATC) is estimated to comprise 1-2% of thyroid malignancies and it accounts for 14-39% of thyroid cancer deaths. The annual incidence of ATC is about one to two cases/million, with the overall incidence being higher in Europe (and area of endemic goiter) than in USA. ATC has a more complex genotype than DTCs, with chromosomal aberrations present in 85-100% of cases. A small number of gene mutations

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… Moreover Pennell et al studied the efficacy of gefitinib in a large group of thyroid cancer, including anaplastic thyroid cancer. … Although gefitinib therapy did not result in any complete responses, the 32% of all patients underwent therapy with gefitinib have had reductions in tumor volume and prolonged stable disease, for the authors this may indicate biologic activity (Pennel et al., 2008 ). …

Molecular chess? Hallmarks of anti-cancer drug resistance.

BackgroundThe development of resistance is a problem shared by both classical chemotherapy and targeted therapy. Patients may respond well at first, but relapse is inevitable for many cancer patients, despite many improvements in drugs and their use over the last 40 years.ReviewResistance to anti-cancer drugs can be acquired by several mechanisms within neoplastic cells, defined as (1) alteration of drug targets, (2) expression of drug pumps, (3) expression of detoxification mechanisms, (4) reduced susceptibility to apoptosis, (5) increased ability to repair DNA damage, and (6) altered prolife

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… Pharmaceutical chemists now design drugs with this mind, so that pump mechanisms are less problematic than they were, though even some TKIs, including gefitinib and erlotinib [ 37 , 38 ], are pumped. … Costa DB Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib Clin Cancer Res 2008 14 21 7060 7 10.1158/1078-0432.CCR-08-1455 18981003 PMC2596582 28. …

Clinical benefit and risk of elemene in cancer patients undergoing chemotherapy: a systematic review and meta-analysis.

Introduction: Elemene injection and oral emulsion, known as elemene, have been utilized have been used in adjuvant therapy for cancer patients in China for more than 20 years. In order to evaluate the efficacy and potential risks of the treatments in cancer patients undergoing chemotherapy, a system review and meta-analysis were conducted. Additionally, the factors that may influence the outcomes were also explored. Methods: A comprehensive search was conducted across various databases including PubMed, Cochrane Library, Web of Science, EMBASE, CKNI, Wan Fang, and VIP databases. Meta-regressio

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… The mechanism of m6A methyltransferase METTL3-mediated autophagy in reversing gefitinib resistance in NSCLC cells by β-elemene. … P21 (waf1/cip1) is required for non-small cell lung cancer sensitive to Gefitinib treatment. Biomed. Pharmacother. 65, 151–156. 10.1016/j.biopha.2011.02.009 Zheng C., Cai X., Wu S., Liu Z., Shi Y., Zhou W. (2014). …

Narrative Review of Drug-Associated Nail Toxicities in Oncologic Patients.

IntroductionNail toxicity represents one of the most common cutaneous adverse effects of both classic chemotherapeutic agents and new oncologic drugs, including targeted treatments and immunotherapy.ObjectivesWe aimed to provide a comprehensive literature review of nail toxicities derived from conventional chemotherapeutic agents, targeted therapies (EGFR inhibitors, multikinase inhibitors, BRAF and MEK inhibitors) and immune checkpoint inhibitors (ICIs), including clinical presentation, implicated drugs and approaches for prevention and management.MethodsRetrieved literature from PubMed regis

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… EGFR-Inhibitors Epidermal growth factor receptor inhibitors (gefitinib, erlotinib, cetuximab, panitumumab) block the signal transduction pathway, needed for cell proliferation, migration and angiogenesis of tumor cells [ 37 – 40 ]. … Gefitinib and erlotinib are orally administered EGFR tyrosine kinase inhibitors, whilst cetuximab and panitumumab are humanized monoclonal antibodies that are given intravenously. …

Osteoblastic bone reaction in non-small cell lung cancer harboring epidermal growth factor receptor mutation treated with osimertinib.

BackgroundOsteoblastic bone reaction (OBR) refers to an increase in bone density at the site of bone metastasis or the appearance of new sclerotic bone lesions after anticancer treatment. OBR can be misunderstood as disease progression. In this study, we aimed to investigate the prevalence and details of OBR and its association with clinical outcomes in patients with epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC) treated with osimertinib.MethodsThis was a single-center, retrospective cohort study. We reviewed patients who were diagnosed with EGFR-mutant NSCLC

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… Yamashita Y Aoki T Hanagiri T Yoshii C Mukae H Uramoto H Osteosclerotic lesions in patients treated with gefitinib for lung adenocarcinomas: a sign of favorable therapeutic response Skelet Radiol 2012 41 409 414 10.1007/s00256-011-1253-9 21866322 4. … Chao HS Chang CP Chiu CH Chu LS Chen YM Tsai CM Bone scan flare phenomenon in non–small-cell lung cancer patients treated with gefitinib Clin Nucl Med 2009 34 346 349 10.1097/RLU.0b013e3181a344df 19487842 19. …

Combined Administration of Bisphosphonates, Chemotherapeutic Agents, and/or Targeted Drugs Increases the Risk for Stage 3 Medication-Related Osteonecrosis of the Jaw: A 4-Year Retrospective Study.

OBJECTIVES: Patients with stage 3 medication-related osteonecrosis of the jaw (MRONJ) suffer from severe complications. Chemotherapeutic agents and targeted drugs are considered to be associated with the development of MRONJ. However, little is known regarding the association of those agents with stage 3 MRONJ. The purpose of this study is to analyze the comprehensive medication history of patients with advanced-stage MRONJ (stage 2 and stage 3) and evaluate the possible risk factors for stage 3 MRONJ. Patients and Methods. Sixty patients with advanced-stage MRONJ were involved in this retrosp

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… The use of targeted drugs among advanced-stage MRONJ was distributed, and gefitinib was relatively used more frequently than other drugs (8 of 23 patients; 34.5%). … In the present study, we demonstrated that targeted therapy was a risk factor for stage 3 MRONJ and gefitinib was the most used targeted drug among MRONJ patients. …

New prognostic factors and scoring system for patients with skeletal metastasis.

The aim of this study was to update a previous scoring system for patients with skeletal metastases, that was proposed by Katagiri et al. in 2005, by introducing a new factor (laboratory data) and analyzing a new patient cohort. Between January 2005 and January 2008, we treated 808 patients with symptomatic skeletal metastases. They were prospectively registered regardless of their treatments, and the last follow-up evaluation was performed in 2012. There were 441 male and 367 female patients with a median age of 64 years. Of these patients, 749 were treated nonsurgically while the remaining 5

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… Table 1 Type of primary tumor, patient median survival, and classification S, slow growth group; M, moderate growth group; R, rapid growth group; NSC, non-small cell. 1 Molecularly targeted agents: gefitinib and/or erlotinib. … To determine the survival period, we divided lung cancer patients into two subgroups, namely, lung cancer patients who were indicated for treatment with molecularly targeted agents (gefitinib and/or erlotinib), and other lung cancer patients. …

The influence of targeted therapies in the inner ear.

Scientific research has significantly propelled advancements in healthcare. One notable application is precision medicine, which seeks to analyze and comprehend disease pathology to offer personalized medical treatments to patients. Targeted oncology, a branch of precision medicine, focuses on identifying and targeting specific molecules that regulate cancer cells, thereby minimizing harm to healthy cells. Different types of targeted therapy against cancer include monoclonal antibodies and small molecules. This manuscript intends to provide an overview of the influence of these targeted oncolo

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… Tyrosine kinase inhibitors (TKI): imatinib, gefitinib, erlotinib, sunitinib Imatinib was the first small molecule TKI approved for use. … Sensorineural hearing loss induced by gefitinib: a CARE-compliant case report and literature reviews. Medicine 102 (45), e36010. 10.1097/MD.0000000000036010 …

Combinational Antitumor Strategies Based on the Active Ingredients of Toad Skin and Toad Venom.

A multidrug combination strategy is an important mean to improve the treatment of cancer and is the mainstream scheme of clinical cancer treatment. The active ingredients of traditional Chinese medicine, represented by toad skin and toad venom, have the advantages of high efficiency, low toxicity, wide action and multiple targets and have become ideal targets in combined treatment strategies for tumors in recent years. Toad skin and toad venom are traditional Chinese animal medicines derived from Bufo bufo gargarizans Cantor or Bufo melanostictus Schneider that have shown excellent therapeutic

Novel Indications for Bruton's Tyrosine Kinase Inhibitors, beyond Hematological Malignancies.

Bruton's tyrosine kinase (BTK) is a critical terminal enzyme in the B-cell antigen receptor (BCR) pathway. BTK activation has been implicated in the pathogenesis of certain B-cell malignancies. Targeting this pathway has emerged as a novel target in B-cell malignancies, of which ibrutinib is the first-in-class agent. A few other BTK inhibitors (BTKi) are also under development (e.g., acalabrutinib). While the predominant action of BTKi is the blockade of B-cell receptor pathway within malignant B-cells, increasing the knowledge of off-target effects as well as a potential role for B-cells in p

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… A more recent study confirmed that ibrutinib inhibits mutant EGFR kinases through formation of a covalent bond with Cys797 similar to other irreversible EGFR TKIs such as gefitinib and erlotinib [ 27 ]. … Tumor progression was slowed by ibrutinib in xenograft mouse models, however not to same extent as seen with gefitinib [ 25 ]. Ibrutinib also slowed tumor progression in a T790M mutation mouse model. …

A Holistic Review of Oncological Drug Targets and Trajectories of Resistance in Cancer Therapy.

The prolonged and intricate history of oncological treatments has transitioned significantly since the introduction of chemotherapy. Substantial therapeutic benefits in cancer therapy have been achieved by the integration of conventional treatments with molecular biosciences and omics technologies. Human epidermal growth factor receptor, hormone receptors, and angiogenesis factors are among the established therapies in tumor reduction and managing side effects. Novel targeted therapies like KRAS G12C, Claudin-18 isoform 2 (CLDN18.2), Trophoblast cell-surface antigen 2 (TROP2), and epigenetic r

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… Erlotinib and gefitinib, also classified as reversible inhibitors, are small-molecule tyrosine kinase inhibitors [ 27 ]. … Gefitinib arrests the cell cycle at the G1 phase by blocking the mitogen-activated protein kinase pathway (MAPK) and P13K/AKT pathways involved in apoptosis and cell survival. Gefitinib was also reported to be more tolerable and cost-effective as compared to erlotinib. …

The role of Rhizoma Paridis saponins on anti-cancer: The potential mechanism and molecular targets.

Cancer is a disease characterized by uncontrolled cell proliferation, leading to excessive growth and invasion that can spread to other parts of the body. Traditional Chinese medicine has made new advancements in the treatment of cancer, providing new perspectives and directions for cancer treatment. Rhizoma Paridis is a widely used Chinese herbal medicine with documented anti-cancer effects dating back to ancient times. Modern research has shown that Rhizoma Paridis saponins (RPS) have various pharmacological activities. RPS can inhibit cancer in multiple ways, such as suppressing tumor growt

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… Polyphyllin VII can increase the sensitivity of non-small cell lung cancer patients resistant to gefitinib by modulating the levels of p21. … Polyphyllin VII increases sensitivity to gefitinib by modulating the elevation of P21 in acquired gefitinib resistant non-small cell lung cancer J. Pharmacol. Sci. 134 2017 190 196 10.1016/j.jphs.2017.06.005 28757172 58 Li J.-K. Sun H.-T. Jiang X.-L. Chen Y.-F. Zhang Z. Wang Y. Chen W.-Q. Zhang Z. …

The Three Musketeers in Cancer Therapy: Pharmacokinetics, Pharmacodynamics and Personalised Approach.

Cancer therapy is rapidly evolving from a one-size-fits-all paradigm toward highly personalized approaches. Traditional chemotherapies and radiotherapies, while broadly applied, often yield suboptimal outcomes due to tumor heterogeneity and are limited by significant toxicities. In contrast, precision oncology tailors prevention, diagnosis, and treatment to the individual patient's genetic and molecular profile. Key advancements underscore this shift: molecularly targeted drugs (e.g., trastuzumab for HER2-positive breast cancer, EGFR and ALK inhibitors for lung cancer) have improved efficacy a

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… CYP2D6, although not a major pathway for most TKIs, plays a role in metabolising the EGFR inhibitor gefitinib [ 22 ]. … For instance, cancer patients heterozygous for ABCG2 421C>A had significantly higher steady-state accumulation of the EGFR inhibitors gefitinib and erlotinib compared to wild-type patients [ 26 ]. …

Nephrotoxicity in cancer treatment: An overview.

Anticancer drug nephrotoxicity is an important and increasing adverse drug event that limits the efficacy of cancer treatment. The kidney is an important elimination pathway for many antineoplastic drugs and their metabolites, which occurs by glomerular filtration and tubular secretion. Chemotherapeutic agents, both conventional cytotoxic agents and molecularly targeted agents, can affect any segment of the nephron including its microvasculature, leading to many clinical manifestations such as proteinuria, hypertension, electrolyte disturbances, glomerulopathy, acute and chronic interstitial n

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… Rare cases of nephrotic syndrome accompanied by minimal-change disease and membranous nephropathy have been related to the use of gefitinib, an EGFR-TKI[ 72 - 74 ]. Moreover, this drug family might also cause hypomagnesemia, hypophosphatemia, and hypokalemia[ 75 ]. … Nephrotic syndrome associated with gefitinib therapy J Clin Oncol 2004 22 2504 2505 15197213 10.1200/JCO.2004.09.064 73 Maruyama K Chinda J Kuroshima T Kabara M Nakagawa N Fujino T Yamamoto Y Ohsaki Y Ogawa Y Hasebe N Minimal change nephrotic syndrome associated with gefitinib and a successful switch …

A comprehensive tool for tumor precision medicine with pharmaco-omics data analysis.

Background: Cancer precision medicine is an effective strategy to fight cancers by bridging genomics and drug discovery to provide specific treatment for patients with different genetic characteristics. Although some public databases and modelling frameworks have been developed through studies on drug response, most of them only considered the ramifications of the drug on the cell line and the effects on the patient still require a huge amount of work to integrate data from various databases and calculations, especially concerning precision treatment. Furthermore, not only efficacy but also th

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… For example, cisplatin ( Group, 2004 ), gefitinib ( Giaccone, 2004 ), and pemetrexed ( Rossi et al., 2009 ) are three FDA-approved drugs for lung cancer treatment and rank high in the database (in detail, cisplatin reverses 676 genes, gefitinib reverses 646 genes, and pemetrexed reverses 588 genes and … The role of gefitinib in lung cancer treatment. Clin. cancer Res. 10, 4233s–4237s. 10.1158/1078-0432.CCR-040005 Ginsburg G. S., Phillips K. A. (2018). Precision medicine: From science to value. Health Aff. 37, 694–701. 10.1377/hlthaff.2017.1624 Group I. A. L. C. T. …

Trial Watch: combination of tyrosine kinase inhibitors (TKIs) and immunotherapy.

The past decades witnessed the clinical employment of targeted therapies including but not limited to tyrosine kinase inhibitors (TKIs) that restrain a broad variety of pro-tumorigenic signals. TKIs can be categorized into (i) agents that directly target cancer cells, (ii) normalize angiogenesis or (iii) affect cells of the hematologic lineage. However, a clear distinction of TKIs based on this definition is limited by the fact that many TKIs designed to inhibit cancer cells have also effects on immune cells that are being discovered. Additionally, TKIs originally designed to target hematologi

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… NSCLC with EGFR mutation. 92 , 93 Treatment with osimertinib significantly prolonged OS when compared to gefitinib and erlotinib (38.6 months versus 31.8 months). … Gefitinib. Nat Rev Drug Discov. 2003;2(7):515–516. doi: 10.1038/nrd1136. 39. Cohen MH, Williams GA, Sridhara R, Chen G, McGuinn WDJ, Morse D, Abraham S, Rahman A, Liang C, Lostritto R, et al. United States food and drug administration drug approval summary: gefitinib (ZD1839; Iressa) tablets. …

Ten years of marketing approvals of anticancer drugs in Europe: regulatory policy and guidance documents need to find a balance between different pressures.

Despite important progress in understanding the molecular factors underlying the development of cancer and the improvement in response rates with new drugs, long-term survival is still disappointing for most common solid tumours. This might be because very little of the modest gain for patients is the result of the new compounds discovered and marketed recently. An assessment of the regulatory agencies' performance may suggest improvements. The present analysis summarizes and evaluates the type of studies and end points used by the EMEA to approve new anticancer drugs, and discusses the applic

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… The recent results with gefitinib in lung cancer patients with mutations in the EGFR gene are striking but only a minority of the lung cancer population may have this mutation ( Lynch et al , 2004 ; Paez et al , 2004 ). … Correlation with clinical response to gefitinib therapy . …

Analysis of medical malpractice liability disputes related to novel antineoplastic drugs and research on risk prevention and control strategies.

OBJECTIVE: To investigate the general characteristics of litigation cases of medical malpractice liability disputes (MMLDs) related to novel antineoplastic drugs (NADs), the drugs involved, as well as the common types of medical errors related to NADs and their damages in the process of diagnosis and treatment, with the aims of improving the level of rational medication use in the clinical application of NADs and actively prevent medical disputes. METHODS: The China Judgments Online was searched for the cause of action using the key word "MMLDs" along with the name of 77 kinds of NADs. A tota

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… A patient with post-operative metastasis of undifferentiated large cell carcinoma of the (right) lung (upper lobe) received targeted drug therapy with gefitinib. … A patient with adenocarcinoma of the right lung who had previously failed to use gefitinib for treatment outside the hospital, and subsequently switched to other chemotherapy regimens, but was re-treated with gefitinib without a systematic assessment of the patient’s condition by the healthcare services …

Non-conventional dosing of oral anticancer agents in oncology and malignant haematology: a systematic review protocol.

BackgroundRecent advances in cancer therapeutics have resulted in significantly improved overall survival and progression-free survival for patients. Targeted oral systemic anticancer therapies (SACT) offer a range of treatment approaches that differ from traditional cytotoxic chemotherapy: non-cytotoxic oral SACT target malignant disease continuously, have less broad and more favourable safety profiles, which can improve patients' quality of life (QoL). Toxicities associated with daily oral SACT administration can, however, result in non-adherence and a reduced QoL. Non-conventional dosing of

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… Search terms for small molecule targeted therapies are: afatinib, axitinib, bosutinib, cabozantinib, cobimetinib, crizotinib, ceritinib, dabrafenib, dasatinib, erlotinib, everolimus, gefitinib, ibrutinib, idelalisib, imatinib, lapatinib, nilotinib, nintedanib, olaparib, osimertinib, panobinostat, pazopanib … lomustine or mitotane or procarbazine or tegafur or temozolomide or tioguanine or topotecan or treosulfan or tretinoin or trifluridine or vinorelbine or afatinib or axitinib or bosutinib or cabozantinib or cobimetinib or crizotinib or ceritinib or dabrafenib or dasatinib or erlotinib or everolimus or gefitinib …

Radiotherapy in combination with systemic therapies for brain metastases: current status and progress.

Brain metastases (BMs) are the most common cause of intracranial neoplasms in adults with poor prognosis. Most BMs originate from lung cancer, breast cancer, or melanoma. Radiotherapy (RT), including whole brain radiotherapy (WBRT) and stereotactic radiation surgery (SRS), has been widely explored and is considered a mainstay anticancer treatment for BMs. Over the past decade, the advent of novel systemic therapies has revolutionized the treatment of BMs. In this context, there is a strong rationale for using a combination of treatments based on RT, with the aim of achieving both local disease

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… RT+chemo | WBRT | Gefitinib vs. TMZ | Gefitinib vs. … Outcome, quality of life and cognitive function of patients with brain metastases from non-small cell lung cancer treated with whole brain radiotherapy combined with gefitinib or temozolomide. …