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ТЕМА: Posted by Tabitha Appleton on 30.11.2016 10:37:27: cara kerja tarceva

Posted by Tabitha Appleton on 30.11.2016 10:37:27: cara kerja tarceva 7 года 5 мес. назад #940

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High Quality - Low Cost Anti-Cancer Drugs

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7. Rosell R, Gervais R, Vergnenegre A, et al. Erlotinib versus chemotherapy ( ct ) in advanced non-small cell lung cancer ( nsclc ) patients (p) with epidermal growth factor receptor ( egfr ) mutations: interim results of the European Erlotinib Versus Chemotherapy ( eurtac ) phase iii randomized trial [abstract 7503]. J Clin Oncol 2011;29. [Available online at: www.asco.org/ASCOv2/Meetings/Abstracts?&...amp;abstractID=78285 ; cited December 8, 2011]
Surgery is the major treatment for most malignant tumors, but recurrence and metastasis often occur after the operations. Systemic chemotherapy can control the recurrence and metastasis effectively, improve the life quality and prolong the survival time of the patients with advance cancers. However, the traditional chemotherapy not only kills tumor cells but also damages the normal cells, resulting in bone marrow suppression, liver and kidney dysfunction, gastrointestinal reactions, decreased immune function and other side effects. Fortunately, this problem can be solved by the molecular targeted drugs. Erlotinib Hydrochloride Tablets (Tarceva) is a new small molecular targeting inhibitor, which inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR)[8]. [9]. It can selectively act on intracellular targets, block EGFR pathway and inhibit the development of tumors, but causes little damage to the normal cells[10]. [11]. Erlotinib monotherapy is indicated for treating the patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen[12]. The most common adverse reactions are rash and diarrhea. Its efficiency can be increased but its toxicity reduced by administering the drugs when they are most effective and/or tolerated. The mechanism may be related to the dosing time-dependent variations in pharmacokinetics, tumor responsiveness, and host immune responsiveness [13]. However, the exact mechanism has not been clarified yet.
Erlotinib has received its official approval from US Food and Drug Administration (FDA) in September 1981.
Erlotinib, which targets a protein called the epidermal growth factor (EGF) receptor, found on tumor cell surfaces, has been approved by the Food and Drug Administration to treat pancreatic cancer and some types of lung cancer. Doxorubicin is used to treat many cancers, including leukemia, lymphoma, and bladder, breast, lung, and ovarian tumors.
Regulation of EGFR and mTOR pathways by erlotinib and RAD001 monotherapy and upon combination
Oral erlotinib 150 mg/day.
streetworkout.org/index.php/forum/kettle...rlotinib-lungenkrebs
Background: First-line maintenance erlotinib in patients with locally advanced or metastatic nonsmall cell lung cancer (NSCLC) has demonstrated significant overall survival and progression-free survival benefits compared with best supportive care plus placebo, irrespective of epidermal growth factor receptor (EGFR) status (SATURN trial). The cost-effectiveness of first-line maintenance erlotinib in the overall SATURN population has been assessed and published recently, but analyses according to EGFR mutation status have not been performed yet, which was the rationale for assessing the cost-effectiveness of first-line maintenance erlotinib specifically in EGFR wild-type metastatic NSCLC. Methods: The incremental cost per life-year gained of first-line maintenance erlotinib compared with best supportive care in patients with EGFR wild-type stable metastatic NSCLC was assessed for five European countries (the United Kingdom, Germany, France, Spain, and Italy) with an area-under-the-curve model consisting of three health states (progression-free survival, progressive disease, death). Log-logistic survival functions were fitted to Phase III patient-level data (SATURN) to model progression-free survival and overall survival. The first-line maintenance erlotinib therapy cost (modeled for time to treatment cessation), medication cost in later lines, and cost for the treatment of adverse events were included. Deterministic and probabilistic sensitivity analyses using Monte Carlo simulation (1000 iterations) were performed. Results: According to the model simulations, first-line maintenance erlotinib compared with best supportive care in EGFR wild-type stable metastatic NSCLC resulted in 4.57 months of life gained (17.82 months for erlotinib versus 13.24 months for best supportive care) and 1.14 months of life without progression gained (erlotinib 4.29 versus best supportive care 3.15), and incremental total costs of erlotinib from €7897 (UK) to €9580 (Germany). The corresponding mean incremental cost per life-year gained of erlotinib ranged between €20,711 (UK) and €25,124 (Germany). Sensitivity analyses confirmed these results. Conclusion: First-line erlotinib maintenance treatment is cost-effective compared with best supportive care in EGFR wild-type stable metastatic NSCLC, irrespective of the country setting.
Respiratory Tract Diseases Carcinoma, Bronchogenic Bronchial Neoplasms Pleural Diseases Pleural Neoplasms Heart Diseases Cardiovascular Diseases Carboplatin Paclitaxel Albumin-Bound Paclitaxel Erlotinib Hydrochloride Antineoplastic Agents Antineoplastic Agents, Phytogenic Tubulin Modulators Antimitotic Agents
A preparation process of erlotinib of formula (I) or a salt thereof,
The most common site of relapse was lung in the ITT population and EGFR m+ subgroup (Appendix Table A2. online only). Among the 66 patients with EGFR m+ tumors who experienced a relapse, a higher rate of brain relapse was reported with erlotinib (n = 13; 37.1%) versus placebo (n = 4; 1.9%), and a lower rate of bone relapse with erlotinib (n = 5; 14.3%) versus placebo (n = 9; 29.0%).
FDA Approves Erlotinib
A process for preparing erlotinib hydrochloride form a WO 2014136126 A2
The synthesis and structure of LG268 (12 ) and CDDO-MA (9. 15 ) have been described. The CDDO-MA used in these experiments was synthesized by Ash Stevens. Erlotinib (16. 17 ) was provided by OSI Pharmaceuticals. Purity was >95% for all compounds as determined by high-performance liquid chromatography.
taekwondo52.ru/forum/8--/5745-posted-by-...ung-cancer.html#5745
FDA package inserts for Tarceva (Erlotinib)
Gender of people who have Diabetes when taking Tarceva *:
Tarceva should be taken on an empty stomach, 1 hour before or 2 hours after eating.
//www.drugs.com/clinical_trials/new-analyses-confirm-nexavar-s-efficacy-safety-multiple-patient-subsets-liver-cancer-6045.html Hepatocellular Carcinoma - University of Nevada School of Medicine AASLD Practice Guidelines on Screening & Surveillance for HCC. Sorafenib* (Nexavar); Erlotinib (Tarceva); Sirolimus (Rapamune); Capecitabine (Xeloda). www.medicine.nevada.edu/homepage/nrg/HCC.ppt Liver Cancer becomes more treatable and Preventable www.easl.
autoamalgama.ru/forum/zadajte-vopros/313...all-cell-lung-cancer
AKT HGF EGFR mutations Erlotinib NSCLC
Finally, besides its invariable association with erlotinib sensitivity in EGFR-WT LCSCs, EGFR tyr1068 was associated with EGFR-sensitizing mutations in cell lines and patient tumors, with relevant diagnostic and therapeutic implication.
Placebo Comparator: Late Erlotinib
9. Erlotinib References
Erlotinib is a small-molecular inhibitor of epidermal growth factor receptor (EGFR). Here, we identify that cancerous inhibitor of protein phosphatase 2A (CIP2A) is a major determinant mediating erlotinib-induced apoptosis in hepatocellular carcinoma (HCC). Erlotinib showed differential effects on apoptosis in 4 human HCC cell lines. Erlotinib induced significant apoptosis in Hep3B and PLC5 cell lines; however, Huh-7 and HA59 T cell lines showed resistance to erlotinib-induced apoptosis at all tested doses. Down-regulation of CIP2A, a cellular inhibitor of protein phosphatase 2A (PP2A), mediated the apoptotic effect of erlotinib in HCC. Erlotinib inhibited CIP2A in a dose- and time-dependent manner in all sensitive HCC cells whereas no alterations in CIP2A were found in resistant cells. Overexpression of CIP2A upregulated phospho-Akt and protected Hep3B cells from erlotinib-induced apoptosis. In addition, silencing CIP2A by siRNA restored the effects of erlotinib in Huh-7 cells. Moreover, adding okadaic acid, a PP2A inhibitor, abolished the effects of erlotinib on apoptosis in Hep3B cells; and forskolin, a PP2A agonist enhanced the effect of erlotinib in resistant HA59 T cells. Combining Akt inhibitor MK-2206 with erlotinib restored the sensitivity of HA59 T cells to erlotinib. Furthermore, in vivo xenograft data showed that erlotinib inhibited the growth of PLC5 tumor but had no effect on Huh-7 tumor. Erlotinib downregulated CIP2A and upregulated PP2A activity in PLC5 tumors, but not in Huh-7 tumors. In conclusion, inhibition of CIP2A determines the effects of erlotinib on apoptosis in HCC. CIP2A may be useful as a therapeutic biomarker for predicting clinical response to erlotinib in HCC treatment.
Another group identified the same mutation in two of five patients with acquired resistance to gefitinib or erlotinib 1 and a sixth patient whose tumor progressed on adjuvant gefitinib after complete resection. The mutation could not be detected in untreated tumor samples. Biochemical analyses of transfected cells and growth-inhibition studies with lung cancer cell lines suggested that the Thr790 Met mutation confers resistance to EGFR mutants that are usually sensitive to gefitinib or erlotinib. 1
chitogrito.ru/index.php/forum/3-nebolsha...va-contre-indication
Drug Name: ERLOTINIB - ORAL
ansb.ru/kunena/dobro-pozhalovat/25726-po...rceva-treatment.html
Pilot Study of EGFR Inhibition With Erlotinib in Cirrhosis to Inhibit Fibrogenesis and Prevent Hepatocellular Carcinoma
Previous preclinical studies showed that the EGFR small molecule inhibitor gefitinib decreases proliferation of tumor cells in a panel of HR NB cell lines, which led to the use of gefitinib as well as erlotinib in Phase I pediatric clinical trials for relapsed pediatric solid tumors, including neuroblastoma. 24,25 Jakacki RI. Hamilton M. Gilbertson RJ. Blaney SM. Tersak J. Krailo MD. Ingle AM. Voss SD. Dancey JE. Adamson PC. Pediatric phase I and pharmacokinetic study of erlotinib followed by the combination of erlotinib and temozolomide: a Children's Oncology Group Phase I Consortium Study. J Clin Oncol 2008 ; 26: 4921 - 7 ; PMID: 18794549 ; dx.doi.org/ 10.1200/JCO.2007.15.2306 Daw NC. Furman WL. Stewart CF. Iacono LC. Krailo M. Bernstein ML. Dancey JE. Speights RA. Blaney SM. Croop JM. et al. Phase I and pharmacokinetic study of gefitinib in children with refractory solid tumors: a Children's Oncology Group Study. J Clin Oncol 2005 ; 23: 6172 - 80 ; PMID: 16135484 ; dx.doi.org/ 10.1200/JCO.2005.11.429 These clinical studies failed to show clear responses in patients with recurrent or refractory NB, and conclusions were made that gefitinib and erlotinib may have little utility in HR NB treatment. 24,25 Jakacki RI. Hamilton M. Gilbertson RJ. Blaney SM. Tersak J. Krailo MD. Ingle AM. Voss SD. Dancey JE. Adamson PC. Pediatric phase I and pharmacokinetic study of erlotinib followed by the combination of erlotinib and temozolomide: a Children's Oncology Group Phase I Consortium Study. J Clin Oncol 2008 ; 26: 4921 - 7 ; PMID: 18794549 ; dx.doi.org/ 10.1200/JCO.2007.15.2306 Daw NC. Furman WL. Stewart CF. Iacono LC. Krailo M. Bernstein ML. Dancey JE. Speights RA. Blaney SM. Croop JM. et al. Phase I and pharmacokinetic study of gefitinib in children with refractory solid tumors: a Children's Oncology Group Study. J Clin Oncol 2005 ; 23: 6172 - 80 ; PMID: 16135484 ; dx.doi.org/ 10.1200/JCO.2005.11.429 Our data suggests that the lack of clinical efficacy of EGFR inhibitors when given as monotherapy to NB patients may be due to the increased role of Bcl - 2 that was not taken into account, as Bcl - 2 sequesters Bim following EGFR inhibitor-mediated displacement of Bim from Mcl - 1 (See Fig. 8B ). Ultimately our results imply that EGFR or ERK small molecule inhibitors will be less effective against HR NBs unless one subverts the Bcl - 2 survival bias by combining these agents with a Bcl - 2 antagonist ( Fig. 8C ).
Successful treatment with erlotinib of severe neutropenia induced by gefitinib in a patient with advanced non-small cell lung cancer
The effect of erlotinib on survivin expression correlates with that on apoptosis
Eligible patients had stage IIIB/IV NSCLC and had failed or were unsuitable for chemotherapy. Erlotinib (150 mg/day orally) was given until disease progression or unacceptable toxicity. Patients were monitored monthly.
Wakelee HA, Gettinger SN, Engelman JA, et al. A phase Ib/II study of XL184 (BMS 907351) with and without erlotinib in patients (pts) with non-small cell lung cancer (NSCLC). J Clin Oncol 2010;28:abstr 3017.
Erlotinib may cause you to become sunburned more easily. Avoid the sun, sunlamps, or tanning booths until you know how you react to erlotinib. Use a sunscreen or wear protective clothing if you must be outside for more than a short time.
maz68.ru/index.php/forum?func=view&catid=3&id=9480
The serum concentration of Erlotinib can be increased when it is combined with Ciprofloxacin.
Shepherd F, Pereira J, Ciuleanu T, et al. A randomised placebo-controlled trial of erlotinib in patients with advanced non-small cell lung cancer (NSCLC) following failure of 1st line or 2nd line chemotherapy [abstract 7022]. J Clin Oncol 2004;22 Suppl 14S.
quickcnc.ru/index.php/forum/13--/887-pos...38-erlotinib-bnf#887
Comparar SLP entre erlotinib vs. quimioterapia con platino
Yamada. K. Takayama, K. Kawakami, S. Saruwatari, K. Morinaga, R. Harada, T. Aragane, N. Nagata, S. Kishimoto, J. Nakanishi, Y. and Ichinose, Y. (2013) Phase II Trial of Erlotinib for Japanese Patients with Previously Treated Non-Small-Cell Lung Cancer Harboring EGFR Mutations: Results of Lung Oncology Group in Kyusyu (LOGiK0803). Japanese Journal of Clinical Oncology, 43, 629-635. dx.doi.org/10.1093/jjco/hyt056
Paronychia severity is graded according to criteria prepared by editorial committee of Erlotinib Rash Management Overview and Specific Treatment Guidelines v3.0.
Progression-free survival in patients with Tarceva dose reductions due to grade III-IV rash; tumor assessments by CT or MRI according to RECIST criteria [ Time Frame: up to 3 years ] [ Designated as safety issue: Yes ]
Non-small cell lung cancer (NSCLC) accounts for 80% of all lung cancer cases. The majority of NSCLC patients have advanced disease at the time of diagnosis, which usually requires treatment beyond standard first-line chemotherapy. Until recently, patients were limited in the number of options available for second-line treatment of NSCLC. In 2004, erlotinib was approved by the FDA for second and third-line treatment of NSCLC. Erlotinib is a cancer chemotherapy medication that slows the growth and spread of cancer cells in the body.
Table. Median OS by Rash Status in Patients on Erlotinib 1
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