High Quality - Low Cost Anti-Cancer Drugs
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*
To determine the resection rate (defined as the fraction of patients who proceed to planned surgery with removal of primary tumor [R0/R1]) following induction treatment with gemcitabine plus erlotinib
ufbk.ru/forum?view=topic&catid=12&id=11517
Retrasa el crecimiento tumora:l Tarceva puede retrasar o detener el crecimiento del cáncer e incluso reducir el tamaño de los tumores en algunos pacientes.
Proporción de riesgo*, mortalidad (erlotinib: placebo) IC de 95% (razón de riesgo)
magmodels.ru/index.php?option=com_kunena...=3&id=1587&Itemid=15
Tarceva (erlotinib) is a cancer chemotherapy medication used in the treatment of non-small cell lung cancer (NSCLC) or pancreatic cancer. Common side effects of Tarceva include:
Gilotrif compared to Tarceva in squamous cell cancers (Lux Lung![8)]( "8)")
will be reported as showing a survival benefit. However, the clinical utility of the one month improvement is likely to be questioned especially given the toxicity of this agent, the widely recognized minimal to modest efficacy of Tarceva in this setting, and the other agents becoming available.
Using erlotinib with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Randomized Study of Bevacizumab/Tarceva and Tarceva/Sulindac in Squamous Cell Carcinoma of the Head and Neck
Cumpar Urmatuarele Medicamente Tarceva Tasigna Nexavar Sutent Sprycel Velcade Glivec Humira Enbrel Avonex Neulasta Contact 0765.367.409 Posibilitate de Deplasare Plata pe loc Fara intermediari. Cuvinte cheie. cumpar. urmatuarele. medicamente. tarceva. tasigna. nexavar. sutent. sprycel
4 rounds of chemo of taxotere and cisplatin seem to have not worked as now he has mets in his liver, bones and adrenal glands. His doctor is aftraid that Tarceva is not recommended to someone with mets to the bone. That is not what I read. Can you please let me know if Tarceva is for him and whether that can hep stop or slow down the disease? Thanks.
ufbk.ru/forum?view=topic&catid=12&id=11520
. First-line erlotinib followed by second-line cisplatin-gemcitabine chemotherapy in advanced non-small-cell lung cancer: The TORCH randomized trial. J Clin Oncol 2012 ; 30. 3002 - 3011.
No phase I studies have been done with the combination of high dose pulse erlotinib therapy with gemcitabine. We propose a phase I dose escalation study of three day oral dosing of erlotinib with standard dose (1000 mg/m2) gemcitabine. The starting dose of erlotinib is 750 mg, approximately 50% of the the dose found to be safe in previous combination studies with carboplatin and paclitaxel and with pemetrexed [Riely et al. 2009, Davies et al. 2009]. Since acquired resistance can occur rapidly and 5 to 7 days of treatment is not better than 3 days of treatment, we will focus on a 3 day high-dose pulse treatment given every 14 days. This will provide 11 days between erlotinib dosing for the recovery of normal tissues. Levels of serum erlotinib will also be monitored due to considerable interpatient variability in the metabolism of erlotinib.
. Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects. Crit Rev Oncol Hematol 2013 ; 89. 300 - 313.
The ISEL data were presented to the scientific community on April 19, 2005, at the Annual Meeting of the American Association of Cancer Research [4 ]. As disclosed previously, gefitinib did not confer an overall survival advantage; however, gefitinib-treated patients survived longer than placebo-treated patients in two specific patient subsets: patients of Asian origin (median, 9.5 versus 5.5 months, respectively; HR, 0.66; p = .010) and never-smokers (median, 8.9 versus 6.1 months, respectively; HR, 0.67; p = .012). As noted in the accompanying review article by Cohen et al. [5 ], the randomized, placebo-controlled study performed by the NCIC comparing erlotinib with placebo in patients after failure of at least one prior chemotherapy regimen did reveal a survival advantage for erlotinib, 6.67 months versus 4.70 months, respectively. The adjusted HR was 0.73 ( p < .001). Erlotinib was also superior to placebo for progression-free survival and objective response rate. Interestingly, the HRs for erlotinib in the two patient subsets in which gefitinib appears to confer benefit, Asians and never-smokers, were 0.61 and 0.42, respectively. Also, in contrast to the ISEL results, erlotinib appears to prolong survival for most of the other patient subsets, although the sample size is too small in some of the subsets to draw a definitive conclusion.
Pure reference standards of celecoxib (CCB), Erlotinib (ERT), and Sitagliptin (SIT) were obtained from Sigma-Aldrich (Germany). Desmethyl erlotinib (OSI-420) was obtained from Selleckchem (USA). Efavirenz (EFV) was obtained from SBC (USA). Acetonitrile (HPLC grade), methanol (HPLC grade), and ammonium acetate (GR-grade) were procured from E Merck (India) Ltd. India. Formic acid was obtained from Sigma-Aldrich (Germany). Ultra pure water of 18 MΩ/cm was obtained from Millipore: Milli-Q purification system (USA).
Erlotinib is extensively metabolized predominantly by CYP3A4 and, to a lesser extent, by CYP1A2, and the extrahepatic isoform CYP1A1 with metabolites excreted by the biliary system (data not shown). A number of metabolites of erlotinib were identified in rats and dogs, with O -demethylation, oxidation of the acetylene moiety, and aromatic hydroxylation as the major biotransformation pathways (Johnson and Prakash, 1997. 1998 ). To our knowledge, the metabolism and excretion of erlotinib in humans has not been characterized. The primary objective of the present study was to characterize the metabolism and excretion and to perform metabolite identification in humans after a 100-mg single oral dose of [ 14 C]erlotinib. Qualitative and quantitative metabolite profiles of erlotinib in humans were achieved using HPLC coupled in-line with a radiochemical detector and a mass spectrometer (LC-RAM-mass spectrometry). The structures of metabolites, where possible, were supported by comparisons of their retention times on HPLC, and mass spectrometry spectra with those of synthetic standards.
gtpartner.by/index.php/component/kunena/...arceva-and-skin-rash
Doses were reduced in 25   mg per day decrements for toxicity. The initial systemic intervention for symptomatic skin toxicity was minocycline 100–150   mg twice daily for at least 7 days, and the initiation of treatment with minocycline for symptomatic rash was at the discretion of the investigator. The use of minocycline preemptively (i.e. to prevent the development of skin rash) was not allowed. In patients treated with minocycline, the erlotinib dose was not increased and could be held until the skin toxicity was felt to be tolerable, at which time, the same erlotinib dose could be resumed, and further dose escalation, as described previously, could be considered. Other interventions for skin toxicity, including short courses of topical corticosteroids, were at the investigators’ discretion. Patients continued erlotinib until disease progression, intolerable toxicity, or withdrawal of consent.
It showed Gilotrif achieved its primary objective of significantly improving progression-free survival when compared against Roche/Astellas' Tarceva (erlotinib). Gilotrif joins several EGFR-targeting therapies already on the market in the US and
It is also important, therefore, to be aware of these interactions and how best to manage them. Drug interactions affecting erlotinib and gefitinib levels occur by two main mechanisms: altered absorption or altered metabolism.
FDA approves Tarceva (erlotinib)
Fluorouracil bevacizumab erlotinib external beam radiation therapy EBRT
bowlangarsk.ru/forum/otchety-i-obsuzhden...eva-roche-prospektüs
(iii) Dissolving Erlotinib base (prepared according to the process given in International Publication No. WO 2007/060691) in dry methylene chloride and adding a solution of dry HCl gas in isopropanol. The crystals of Erlotinib HCl are filtered and dried and designated as Form-P.
23. The process as claimed in claim 1, wherein the erlotinib or a pharmaceutically acceptable salt of erlotinib obtained is having the content of N-methoxyethyl impurity in less than about 0. 1% by weight.
In our study we have used the DAKO antibody kit system for EGFR protein expression assessment. The 10% cutoff level for a positive result was chosen at the outset as the most discriminating cutoff limit based on previous studies. The same antibody and cutoff criteria were used in the erlotinib BR21 study, and both studies showed an association between EGFR protein expression and clinical outcome. 11
[0006] According to the European Patent No. 1044969, erlotinib hydrochloride is prepared, either by (i) reacting 6,7-bis(2-methoxyethoxy)-N-[3-[(trimethylsilyl)ethynyl]phenyl-4-quinazoli- namine monohydrochloride, obtained by the reaction of 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline with a solution of 3-[(trimethylsilyl)ethynyl]aniline in 2-propanol at reflux, with tetra-n-butylammonium fluoride in an aprotic solvent such as tetrahydrofuran, diethyl ether, dimethoxyethane, toluene, dichloromethane and chloroform, and then treating the reaction mass with concentrated hydrochloric acid in 2-propanol; or (ii) reacting 4-[3-[[6,7-bis(2-methoxyethoxy)-4-quinazolinyl]amino]phenyl]-2-methyl-3-b- utyn-2-ol or its monohydrochloride salt, obtained by the reaction of 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline with 4-(3-aminophenyl)-2-methyl-3-butyn-2-ol in acetonitrile at reflux, with an alkali-metal or alkaline-metal hydroxide such as sodium hydroxide, lithium hydroxide, cesium hydroxide, calcium hydroxide, magnesium hydroxide and potassium hydroxide, in an alcoholic solvent such as 1-butanol, 2-butanol and 2-propanol, and then treating the reaction mass with concentrated hydrochloric acid in an alcoholic solvent.
Cost of Erlonat, Erlotinib Tablets in France
Patients received erlotinib initially at a dose of 150 mg/day. Dose reduction to 100, 75 or 50 mg/day and dose interruption were performed when intolerable toxicities were observed. Therapy was continued until disease progression, intolerable toxicity or patient withdrawal.
sadik91.org.ru/forum/2--/5912-posted-by-...uoc-tarceva-150.html
The purpose of this study is to determine whether 100mg erlotinib had similar effect compared with 150mg erlotinib in NSCLC patients with EGFR mutation in China.
Kelly K, Altorki NK, Eberhardt WEE, et al. Adjuvant erlotinib versus placebo in patients with stage IB-IIIA non-small-cell lung cancer (RADIANT): a randomized, double-blind, phase III trial [published online ahead of print on August 31, 2015]. J Clin Oncol . doi: 10.1200/JCO.2015.61.8918.
Erlonat Tablet is available in the following packages and strengths
Erlotinib and medicinal products altering pH
EMA Label for erlotinib and EGFR,UGT1A1
Temonat belongs to a class of medications called Kinase inhibitors and contains erlotinib. It is used for the treatment of non-small cell lung cancer and in combination with. is used for the treatment of pancreatic cancer which spreads to adjacent tissues of the body. The action mechanism of the medicine is as follows:
It is well known that substantial interindividual variability of CYP3A4/1A2-phenotype activity is an important contributor to individual differences in the sensitivity to the frequently used tyrosine kinase inhibitors sunitinib and erlotinib. This study tests the potential for CYP-phenotyping to predict individual pharmacology and derive dosing algorithms for more tailored treatment of these drugs.
russkazka.com/forum/9--/2450-posted-by-e...tarceva-prolong-life
Neal JW, Dahlberg SE, Wakelee HA, et al. Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial. Lancet Oncol . 2016 Nov 4. doi: 10.1016/S1470-2045(16)30561-7 [Epub ahead of print]
Drug: Erlotinib Drug: Cetuximab
More than 8 prospective trials have evaluated gefitinib or erlotinib monotherapy in EGFR-mutated NSCLC.
An eighth aspect of the present invention provides a method of treating non-small cell lung cancer in combination with gemcitabine for first-line treatment of patients with locally advanced, unresectable, or metastatic pancreatic cancer, comprising administering to a patient in need thereof a therapeutically effective amount of erlotinib saccharinate, or erlotinib maleate or hydrates thereof, and a pharmaceutically acceptable carrier.
PC-9 and PC-9/ER3 cells were treated with erlotinib (0.05 μM) for various lengths of time (0–12 h). pEGFR and pMAPK in both cell lines were markedly suppressed by erlotinib. However, pAkt, which is an effector molecule downstream of EGFR, was not inhibited by erlotinib, and pJAK2 increased more in PC-9/ER3 than in the parental PC-9 cells (Fig. 3 ). JAK2 in both PC-9/ER4 and PC-9/ER5 cells was also activated (Fig. S3). Phosphorylation of STAT3, which is a downstream effector of JAK2, increased time-dependently in both PC-9 and PC-9/ER3 cells after treatment with erlotinib. Although expression of survivin, the anti-apoptotic gene that is downstream of STAT3, did not change during erlotinib treatment, PC-9/ER3 cells had more expressions than PC-9 cells as a base line (Fig. 3 ).
Erlotinib hydrochloride was synthesized as described before (7 ). BSA was purchased from Sigma-Aldrich (Dorset, UK). All other reagents were obtained from Merck (Darmstadt, Germany).
*
To determine the resection rate (defined as the fraction of patients who proceed to planned surgery with removal of primary tumor [R0/R1]) following induction treatment with gemcitabine plus erlotinib
ufbk.ru/forum?view=topic&catid=12&id=11517
Retrasa el crecimiento tumora:l Tarceva puede retrasar o detener el crecimiento del cáncer e incluso reducir el tamaño de los tumores en algunos pacientes.
Proporción de riesgo*, mortalidad (erlotinib: placebo) IC de 95% (razón de riesgo)
magmodels.ru/index.php?option=com_kunena...=3&id=1587&Itemid=15
Tarceva (erlotinib) is a cancer chemotherapy medication used in the treatment of non-small cell lung cancer (NSCLC) or pancreatic cancer. Common side effects of Tarceva include:
Gilotrif compared to Tarceva in squamous cell cancers (Lux Lung
will be reported as showing a survival benefit. However, the clinical utility of the one month improvement is likely to be questioned especially given the toxicity of this agent, the widely recognized minimal to modest efficacy of Tarceva in this setting, and the other agents becoming available.Using erlotinib with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Randomized Study of Bevacizumab/Tarceva and Tarceva/Sulindac in Squamous Cell Carcinoma of the Head and Neck
Cumpar Urmatuarele Medicamente Tarceva Tasigna Nexavar Sutent Sprycel Velcade Glivec Humira Enbrel Avonex Neulasta Contact 0765.367.409 Posibilitate de Deplasare Plata pe loc Fara intermediari. Cuvinte cheie. cumpar. urmatuarele. medicamente. tarceva. tasigna. nexavar. sutent. sprycel
4 rounds of chemo of taxotere and cisplatin seem to have not worked as now he has mets in his liver, bones and adrenal glands. His doctor is aftraid that Tarceva is not recommended to someone with mets to the bone. That is not what I read. Can you please let me know if Tarceva is for him and whether that can hep stop or slow down the disease? Thanks.
ufbk.ru/forum?view=topic&catid=12&id=11520
. First-line erlotinib followed by second-line cisplatin-gemcitabine chemotherapy in advanced non-small-cell lung cancer: The TORCH randomized trial. J Clin Oncol 2012 ; 30. 3002 - 3011.
No phase I studies have been done with the combination of high dose pulse erlotinib therapy with gemcitabine. We propose a phase I dose escalation study of three day oral dosing of erlotinib with standard dose (1000 mg/m2) gemcitabine. The starting dose of erlotinib is 750 mg, approximately 50% of the the dose found to be safe in previous combination studies with carboplatin and paclitaxel and with pemetrexed [Riely et al. 2009, Davies et al. 2009]. Since acquired resistance can occur rapidly and 5 to 7 days of treatment is not better than 3 days of treatment, we will focus on a 3 day high-dose pulse treatment given every 14 days. This will provide 11 days between erlotinib dosing for the recovery of normal tissues. Levels of serum erlotinib will also be monitored due to considerable interpatient variability in the metabolism of erlotinib.
. Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects. Crit Rev Oncol Hematol 2013 ; 89. 300 - 313.
The ISEL data were presented to the scientific community on April 19, 2005, at the Annual Meeting of the American Association of Cancer Research [4 ]. As disclosed previously, gefitinib did not confer an overall survival advantage; however, gefitinib-treated patients survived longer than placebo-treated patients in two specific patient subsets: patients of Asian origin (median, 9.5 versus 5.5 months, respectively; HR, 0.66; p = .010) and never-smokers (median, 8.9 versus 6.1 months, respectively; HR, 0.67; p = .012). As noted in the accompanying review article by Cohen et al. [5 ], the randomized, placebo-controlled study performed by the NCIC comparing erlotinib with placebo in patients after failure of at least one prior chemotherapy regimen did reveal a survival advantage for erlotinib, 6.67 months versus 4.70 months, respectively. The adjusted HR was 0.73 ( p < .001). Erlotinib was also superior to placebo for progression-free survival and objective response rate. Interestingly, the HRs for erlotinib in the two patient subsets in which gefitinib appears to confer benefit, Asians and never-smokers, were 0.61 and 0.42, respectively. Also, in contrast to the ISEL results, erlotinib appears to prolong survival for most of the other patient subsets, although the sample size is too small in some of the subsets to draw a definitive conclusion.
Pure reference standards of celecoxib (CCB), Erlotinib (ERT), and Sitagliptin (SIT) were obtained from Sigma-Aldrich (Germany). Desmethyl erlotinib (OSI-420) was obtained from Selleckchem (USA). Efavirenz (EFV) was obtained from SBC (USA). Acetonitrile (HPLC grade), methanol (HPLC grade), and ammonium acetate (GR-grade) were procured from E Merck (India) Ltd. India. Formic acid was obtained from Sigma-Aldrich (Germany). Ultra pure water of 18 MΩ/cm was obtained from Millipore: Milli-Q purification system (USA).
Erlotinib is extensively metabolized predominantly by CYP3A4 and, to a lesser extent, by CYP1A2, and the extrahepatic isoform CYP1A1 with metabolites excreted by the biliary system (data not shown). A number of metabolites of erlotinib were identified in rats and dogs, with O -demethylation, oxidation of the acetylene moiety, and aromatic hydroxylation as the major biotransformation pathways (Johnson and Prakash, 1997. 1998 ). To our knowledge, the metabolism and excretion of erlotinib in humans has not been characterized. The primary objective of the present study was to characterize the metabolism and excretion and to perform metabolite identification in humans after a 100-mg single oral dose of [ 14 C]erlotinib. Qualitative and quantitative metabolite profiles of erlotinib in humans were achieved using HPLC coupled in-line with a radiochemical detector and a mass spectrometer (LC-RAM-mass spectrometry). The structures of metabolites, where possible, were supported by comparisons of their retention times on HPLC, and mass spectrometry spectra with those of synthetic standards.
gtpartner.by/index.php/component/kunena/...arceva-and-skin-rash
Doses were reduced in 25   mg per day decrements for toxicity. The initial systemic intervention for symptomatic skin toxicity was minocycline 100–150   mg twice daily for at least 7 days, and the initiation of treatment with minocycline for symptomatic rash was at the discretion of the investigator. The use of minocycline preemptively (i.e. to prevent the development of skin rash) was not allowed. In patients treated with minocycline, the erlotinib dose was not increased and could be held until the skin toxicity was felt to be tolerable, at which time, the same erlotinib dose could be resumed, and further dose escalation, as described previously, could be considered. Other interventions for skin toxicity, including short courses of topical corticosteroids, were at the investigators’ discretion. Patients continued erlotinib until disease progression, intolerable toxicity, or withdrawal of consent.
It showed Gilotrif achieved its primary objective of significantly improving progression-free survival when compared against Roche/Astellas' Tarceva (erlotinib). Gilotrif joins several EGFR-targeting therapies already on the market in the US and
It is also important, therefore, to be aware of these interactions and how best to manage them. Drug interactions affecting erlotinib and gefitinib levels occur by two main mechanisms: altered absorption or altered metabolism.
FDA approves Tarceva (erlotinib)
Fluorouracil bevacizumab erlotinib external beam radiation therapy EBRT
bowlangarsk.ru/forum/otchety-i-obsuzhden...eva-roche-prospektüs
(iii) Dissolving Erlotinib base (prepared according to the process given in International Publication No. WO 2007/060691) in dry methylene chloride and adding a solution of dry HCl gas in isopropanol. The crystals of Erlotinib HCl are filtered and dried and designated as Form-P.
23. The process as claimed in claim 1, wherein the erlotinib or a pharmaceutically acceptable salt of erlotinib obtained is having the content of N-methoxyethyl impurity in less than about 0. 1% by weight.
In our study we have used the DAKO antibody kit system for EGFR protein expression assessment. The 10% cutoff level for a positive result was chosen at the outset as the most discriminating cutoff limit based on previous studies. The same antibody and cutoff criteria were used in the erlotinib BR21 study, and both studies showed an association between EGFR protein expression and clinical outcome. 11
[0006] According to the European Patent No. 1044969, erlotinib hydrochloride is prepared, either by (i) reacting 6,7-bis(2-methoxyethoxy)-N-[3-[(trimethylsilyl)ethynyl]phenyl-4-quinazoli- namine monohydrochloride, obtained by the reaction of 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline with a solution of 3-[(trimethylsilyl)ethynyl]aniline in 2-propanol at reflux, with tetra-n-butylammonium fluoride in an aprotic solvent such as tetrahydrofuran, diethyl ether, dimethoxyethane, toluene, dichloromethane and chloroform, and then treating the reaction mass with concentrated hydrochloric acid in 2-propanol; or (ii) reacting 4-[3-[[6,7-bis(2-methoxyethoxy)-4-quinazolinyl]amino]phenyl]-2-methyl-3-b- utyn-2-ol or its monohydrochloride salt, obtained by the reaction of 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline with 4-(3-aminophenyl)-2-methyl-3-butyn-2-ol in acetonitrile at reflux, with an alkali-metal or alkaline-metal hydroxide such as sodium hydroxide, lithium hydroxide, cesium hydroxide, calcium hydroxide, magnesium hydroxide and potassium hydroxide, in an alcoholic solvent such as 1-butanol, 2-butanol and 2-propanol, and then treating the reaction mass with concentrated hydrochloric acid in an alcoholic solvent.
Cost of Erlonat, Erlotinib Tablets in France
Patients received erlotinib initially at a dose of 150 mg/day. Dose reduction to 100, 75 or 50 mg/day and dose interruption were performed when intolerable toxicities were observed. Therapy was continued until disease progression, intolerable toxicity or patient withdrawal.
sadik91.org.ru/forum/2--/5912-posted-by-...uoc-tarceva-150.html
The purpose of this study is to determine whether 100mg erlotinib had similar effect compared with 150mg erlotinib in NSCLC patients with EGFR mutation in China.
Kelly K, Altorki NK, Eberhardt WEE, et al. Adjuvant erlotinib versus placebo in patients with stage IB-IIIA non-small-cell lung cancer (RADIANT): a randomized, double-blind, phase III trial [published online ahead of print on August 31, 2015]. J Clin Oncol . doi: 10.1200/JCO.2015.61.8918.
Erlonat Tablet is available in the following packages and strengths
Erlotinib and medicinal products altering pH
EMA Label for erlotinib and EGFR,UGT1A1
Temonat belongs to a class of medications called Kinase inhibitors and contains erlotinib. It is used for the treatment of non-small cell lung cancer and in combination with. is used for the treatment of pancreatic cancer which spreads to adjacent tissues of the body. The action mechanism of the medicine is as follows:
It is well known that substantial interindividual variability of CYP3A4/1A2-phenotype activity is an important contributor to individual differences in the sensitivity to the frequently used tyrosine kinase inhibitors sunitinib and erlotinib. This study tests the potential for CYP-phenotyping to predict individual pharmacology and derive dosing algorithms for more tailored treatment of these drugs.
russkazka.com/forum/9--/2450-posted-by-e...tarceva-prolong-life
Neal JW, Dahlberg SE, Wakelee HA, et al. Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial. Lancet Oncol . 2016 Nov 4. doi: 10.1016/S1470-2045(16)30561-7 [Epub ahead of print]
Drug: Erlotinib Drug: Cetuximab
More than 8 prospective trials have evaluated gefitinib or erlotinib monotherapy in EGFR-mutated NSCLC.
An eighth aspect of the present invention provides a method of treating non-small cell lung cancer in combination with gemcitabine for first-line treatment of patients with locally advanced, unresectable, or metastatic pancreatic cancer, comprising administering to a patient in need thereof a therapeutically effective amount of erlotinib saccharinate, or erlotinib maleate or hydrates thereof, and a pharmaceutically acceptable carrier.
PC-9 and PC-9/ER3 cells were treated with erlotinib (0.05 μM) for various lengths of time (0–12 h). pEGFR and pMAPK in both cell lines were markedly suppressed by erlotinib. However, pAkt, which is an effector molecule downstream of EGFR, was not inhibited by erlotinib, and pJAK2 increased more in PC-9/ER3 than in the parental PC-9 cells (Fig. 3 ). JAK2 in both PC-9/ER4 and PC-9/ER5 cells was also activated (Fig. S3). Phosphorylation of STAT3, which is a downstream effector of JAK2, increased time-dependently in both PC-9 and PC-9/ER3 cells after treatment with erlotinib. Although expression of survivin, the anti-apoptotic gene that is downstream of STAT3, did not change during erlotinib treatment, PC-9/ER3 cells had more expressions than PC-9 cells as a base line (Fig. 3 ).
Erlotinib hydrochloride was synthesized as described before (7 ). BSA was purchased from Sigma-Aldrich (Dorset, UK). All other reagents were obtained from Merck (Darmstadt, Germany).