erlotinib hydrochloride


Summary: A quinazoline derivative and ANTINEOPLASTIC AGENT that functions as a PROTEIN KINASE INHIBITOR for EGFR associated tyrosine kinase. It is used in the treatment of NON-SMALL CELL LUNG CANCER.

Top Publications

  1. Vincenzi B, Tonini G, Santini D. Aprepitant for erlotinib-induced pruritus. N Engl J Med. 2010;363:397-8 pubmed publisher
  2. Ciuleanu T, Ahmed S, Kim J, Mezger J, Park K, Thomas M, et al. Randomised Phase 2 study of maintenance linsitinib (OSI-906) in combination with erlotinib compared with placebo plus erlotinib after platinum-based chemotherapy in patients with advanced non-small cell lung cancer. Br J Cancer. 2017;117:757-766 pubmed publisher
    ..This highlights the need for robust biomarkers of response for combinations that incorporate IGFR-targeted therapies in maintenance or other therapeutic settings. ..
  3. Meneses Lorente G, McIntyre C, Hsu J, Thomas M, Jacob W, Adessi C, et al. Accelerating drug development by efficiently using emerging PK/PD data from an adaptable entry-into-human trial: example of lumretuzumab. Cancer Chemother Pharmacol. 2017;79:1239-1247 pubmed publisher
    ..The dose and schedule of lumretuzumab were optimised for concomitant therapy at doses substantially below the highest dose investigated. ..
  4. Liang J, Tong F, Gu F, Liu Y, Zeng Y, Hong X, et al. Marked response to nab-paclitaxel in EGFR mutated lung neuroendocrine carcinoma: A case report. Medicine (Baltimore). 2017;96:e6985 pubmed publisher
    ..This case highlights that EGFR mutated lung neuroendocrine carcinoma is not responsive to single-agent EGFR-TKI. However, combined application with nab-paclitaxel can improve its efficacy and prolong the patient's survival. ..
  5. Tung C, Chen J, Wu C, Peng Y, Chen W, Zheng H, et al. Salinomycin acts through reducing AKT-dependent thymidylate synthase expression to enhance erlotinib-induced cytotoxicity in human lung cancer cells. Exp Cell Res. 2017;357:59-66 pubmed publisher
    ..These results may provide a rationale to combine salinomycin with erlotinib for lung cancer treatment. ..
  6. Haas M, Ormanns S, Baechmann S, Remold A, Krüger S, Westphalen C, et al. Extended RAS analysis and correlation with overall survival in advanced pancreatic cancer. Br J Cancer. 2017;116:1462-1469 pubmed publisher
    ..9 vs 8.3 months, P=0.70). Together with the results of the AIO-PK-0104-trial, the present analysis supports the notion that KRAS mutation status is rather predictive than prognostic in advanced PC. ..
  7. Rókusz A, Veres D, Szücs A, Bugyik E, Mózes M, Paku S, et al. Ductular reaction correlates with fibrogenesis but does not contribute to liver regeneration in experimental fibrosis models. PLoS ONE. 2017;12:e0176518 pubmed publisher
    ..No evidences support the persistent antifibrotic property of imatinib or erlotinib. ..
  8. Guarnieri A, Alfonso Bartolozzi B, Ciufo G, Moreno Montañés J, Gil Bazo I. Plasma rich in growth factors for the treatment of rapidly progressing refractory corneal melting due to erlotinib in nonsmall cell lung cancer. Medicine (Baltimore). 2017;96:e7000 pubmed publisher
  9. Meriggi F, Codignola C, Beretta G, Ceresoli G, Caprioli A, Scartozzi M, et al. Significance of neutrophil-to-lymphocyte ratio in Western advanced EGFR-mutated non-small cell lung cancer receiving a targeted therapy. Tumori. 2017;103:443-448 pubmed publisher
    ..Pretreatment NLR seems to represent a reliable, simple, and easy to reproduce laboratory tool to predict outcome and response to cancer therapies in this setting of Western Caucasian patients with EGFR-mutated NSCLC. ..

More Information


  1. Sinn M, Bahra M, Liersch T, Gellert K, Messmann H, Bechstein W, et al. CONKO-005: Adjuvant Chemotherapy With Gemcitabine Plus Erlotinib Versus Gemcitabine Alone in Patients After R0 Resection of Pancreatic Cancer: A Multicenter Randomized Phase III Trial. J Clin Oncol. 2017;35:3330-3337 pubmed publisher
    ..GemErlo for 24 weeks did not improve DFS or overall survival over Gem. ..
  2. Lucas J, Cooper D, Hwang S, Tinkle C, Li X, Li Y, et al. Prognostic Relevance of Treatment Failure Patterns in Pediatric High-Grade Glioma: Is There a Role for a Revised Failure Classification System?. Int J Radiat Oncol Biol Phys. 2017;99:450-458 pubmed publisher
    ..TTD from failure varied according to RANO type, suggesting that adult RANOc require modification before being applied to pHGG. ..
  3. Ali S, Alpaugh R, Buell J, Stephens P, Yu J, Wu H, et al. Antitumor response of an ERBB2 amplified inflammatory breast carcinoma with EGFR mutation to the EGFR-TKI erlotinib. Clin Breast Cancer. 2014;14:e14-6 pubmed publisher
  4. Motoshima K, Nakamura Y, Sano K, Ikegami Y, Ikeda T, Mizoguchi K, et al. Phase II trial of erlotinib in patients with advanced non?small?cell lung cancer harboring epidermal growth factor receptor mutations: additive analysis of pharmacokinetics. Cancer Chemother Pharmacol. 2013;72:1299-1304 pubmed
    ..The D8/D2 ratio of erlotinib plasma trough levels might be a predictive factor for PFS. ..
  5. Bellissimo T, Ganci F, Gallo E, Sacconi A, Tito C, De Angelis L, et al. Thymic Epithelial Tumors phenotype relies on miR-145-5p epigenetic regulation. Mol Cancer. 2017;16:88 pubmed publisher
    ..Altogether our results suggest that the epigenetic regulation of miR-145-5p expression, as well as the modulation of its functional targets, could be relevant players in tumor progression and treatment response in TETs. ..
  6. Masago K, Miura M, Toyama Y, Togashi Y, Mishima M. Good clinical response to erlotinib in a patient with anaplastic thyroid carcinoma harboring an epidermal growth factor somatic mutation, L858R, in exon 21. J Clin Oncol. 2011;29:e465-7 pubmed publisher
  7. Putora P, Benz G, Rodriguez R, Brutsche M, Fruh M. Tracheal granuloma pyogenicum with erlotinib treatment for lung cancer. Eur Respir J. 2011;38:1228-30 pubmed publisher
  8. Wakelee H, Gettinger S, Engelman J, Jänne P, West H, Subramaniam D, et al. A phase Ib/II study of cabozantinib (XL184) with or without erlotinib in patients with non-small cell lung cancer. Cancer Chemother Pharmacol. 2017;79:923-932 pubmed publisher
    ..Cabozantinib did not appear to re-sensitize these patients to erlotinib. ..
  9. Krämer B, Hock C, Schultz J, Lammert A, Kuhlin B, Birk R, et al. Impact of Small Molecules on ?-Catenin and E-Cadherin Expression in HPV16-positive and -negative Squamous Cell Carcinomas. Anticancer Res. 2017;37:2845-2852 pubmed
    ..Alterations of ?-catenin and E-cadherin could provide novel insights for future targeted therapies of head and neck SCC. ..
  10. Yang K, Shin I, Park J, Kim K, Kim D, Park K, et al. Nanoparticulation improves bioavailability of Erlotinib. Drug Dev Ind Pharm. 2017;43:1557-1565 pubmed publisher
    ..8 for NUFS-Ert and 5.8 for Tarceva®. NUFS-Ert could improve poor bioavailability and reduce fed-fasted bioavailability variances of Ert. NUFS-Ert was more efficacious than Tarceva®. ..
  11. Cui S, Jiang L. Factors associated with efficacy of first-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer. Tumour Biol. 2017;39:1010428317705340 pubmed publisher
    ..In addition, new findings related to clinical practice with respect to epidermal growth factor receptor tyrosine kinase inhibitors efficacy were summarized in this article. ..
  12. Calmon R, Puget S, Varlet P, Beccaria K, Blauwblomme T, Grevent D, et al. Multimodal Magnetic Resonance Imaging of Treatment-Induced Changes to Diffuse Infiltrating Pontine Gliomas in Children and Correlation to Patient Progression-Free Survival. Int J Radiat Oncol Biol Phys. 2017;99:476-485 pubmed publisher
    ..High rCBV values following RT should not be mistaken for progression and could be an indicator of response to therapy. ..
  13. Pirker R. What is the best strategy for targeting EGF receptors in non-small-cell lung cancer?. Future Oncol. 2015;11:153-67 pubmed publisher
    ..Multikinase TKIs are investigational as first- and second-line therapies, as monotherapies and in combination with chemotherapy. This article summarizes the available clinical data for EGFR-targeted therapies. ..
  14. Lebellec L, Chauffert B, Blay J, Le Cesne A, Chevreau C, Bompas E, et al. Advanced chordoma treated by first-line molecular targeted therapies: Outcomes and prognostic factors. A retrospective study of the French Sarcoma Group (GSF/GETO) and the Association des Neuro-Oncologues d'Expression Française (ANOCEF). Eur J Cancer. 2017;79:119-128 pubmed publisher
    ..024). The PFS and OS did not significantly differ between the MTT. The prognostic factors identified require validation in an independent database but are potently useful to guide treatment decisions and design further clinical trials. ..
  15. Protsenko S, Rudakova A. [Gefitinib therapy in advanced non-small cell lung cancer in patients with EGFR mutations: cost-effectiveness analysis]. Vopr Onkol. 2015;61:676-80 pubmed
    ..Thus TKI therapy of both the first-, and second/third-line of patients with NSCLC with EGFR mutations is characterized by acceptable cost-effectiveness. ..
  16. Guisier F, Bohn P, Patout M, Piton N, Farah I, Vera P, et al. In- and ex-vivo molecular imaging of apoptosis to assess sensitivity of non-small cell lung cancer to EGFR inhibitors using probe-based confocal laser endomicroscopy. PLoS ONE. 2017;12:e0180576 pubmed publisher
    ..05) and in vivo (p = 0.01). Real-time in vivo and ex vivo assessment of apoptosis using pCLE differentiates resistant from sensitive NSCLC xenografts to Erlotinib. ..
  17. Dillon B, Naidoo B, Knight H, Clark P. NICE guidance on erlotinib for first-line treatment of EGFR-TK mutation-positive advanced or metastatic non-small-cell lung cancer. Lancet Oncol. 2012;13:764-5 pubmed
  18. Butts C. VeriStrat validated in patients with non-small-cell lung cancer. Lancet Oncol. 2014;15:671-2 pubmed publisher
  19. Hirai F, Takenoyama M, Taguchi K, Toyozawa R, Inamasu E, Toyokawa G, et al. Experience with erlotinib in lung adenocarcinoma harboring a coexisting KIF5B-RET fusion gene and EGFR mutation: report of a rare case. J Thorac Oncol. 2014;9:e37-9 pubmed publisher
  20. Gazdar A. Personalized medicine and inhibition of EGFR signaling in lung cancer. N Engl J Med. 2009;361:1018-20 pubmed publisher
  21. Cho Y, Chen K, Sheen Y, Yang C, Liau J, Cheng Y, et al. Purpuric Drug Eruptions Caused by Epidermal Growth Factor Receptor Inhibitors for Non-Small Cell Lung Cancer: A Clinicopathologic Study of 32 Cases. JAMA Dermatol. 2017;153:906-910 pubmed publisher
    ..The role of bacterial pathogens in this reaction is important and requires further exploration. ..
  22. Chen K, Lin C, Cho Y, Yang C, Sheen Y, Tsai H, et al. Comparison of Skin Toxic Effects Associated With Gefitinib, Erlotinib, or Afatinib Treatment for Non-Small Cell Lung Cancer. JAMA Dermatol. 2016;152:340-2 pubmed publisher
  23. Liu D, Yang Y, Zhao S. Autophagy facilitates the EGFR-TKI acquired resistance of non-small-cell lung cancer cells. J Formos Med Assoc. 2014;113:141-2 pubmed publisher
  24. Fiala O, Hosek P, Pesek M, Finek J, Racek J, Stehlík P, et al. Serum Concentration of Erlotinib and its Correlation with Outcome and Toxicity in Patients with Advanced-stage NSCLC. Anticancer Res. 2017;37:6469-6476 pubmed
    ..We focused on the role of serum concentration of erlotinib and its association with outcome and toxicity in patients with advanced NSCLC harbouring the wild-type EGFR gene or squamous histology...
  25. Baglivo S, Ludovini V, Sidoni A, Metro G, Ricciuti B, Siggillino A, et al. Large Cell Neuroendocrine Carcinoma Transformation and EGFR-T790M Mutation as Coexisting Mechanisms of Acquired Resistance to EGFR-TKIs in Lung Cancer. Mayo Clin Proc. 2017;92:1304-1311 pubmed publisher
    ..In addition, our report highlights the pivotal role of rebiopsy and of molecular profiling at the time of progression to guide clinicians to choose the right therapy for the right patient. ..
  26. van der Wekken A, Kuiper J, Saber A, Terpstra M, Wei J, Hiltermann T, et al. Overall survival in EGFR mutated non-small-cell lung cancer patients treated with afatinib after EGFR TKI and resistant mechanisms upon disease progression. PLoS ONE. 2017;12:e0182885 pubmed publisher
    ..Tumors from patients who had progressive disease during afatinib treatment were enriched for mutations in genes involved in Wnt and PI3K-AKT pathways. ..
  27. Chang S, Chang C, Chen C, Yu C. Successful erlotinib rechallenge after gefitinib-induced acute interstitial pneumonia. J Thorac Oncol. 2010;5:1105-6 pubmed publisher
  28. Chen Y, Yeh M, Yu M, Wei Y, Chen W, Chen J, et al. Lapatinib-induced NF-kappaB activation sensitizes triple-negative breast cancer cells to proteasome inhibitors. Breast Cancer Res. 2013;15:R108 pubmed publisher
    ..These findings suggest that combination therapy of a proteasome inhibitor with lapatinib may benefit TNBC patients. ..
  29. Tarhini A, Rafique I, Floros T, Tran P, Gooding W, Villaruz L, et al. Phase 1/2 study of rilotumumab (AMG 102), a hepatocyte growth factor inhibitor, and erlotinib in patients with advanced non-small cell lung cancer. Cancer. 2017;123:2936-2944 pubmed publisher
    ..In the EGFR WT group, the DCR exceeded published reports for erlotinib alone. High circulating levels of neuregulin 1 may indicate sensitivity to this combination. Cancer 2017;123:2936-44. © 2017 American Cancer Society. ..
  30. Li M, He H, Ruan Z, Zhu Y, Li R, He X, et al. Central nervous system progression in advanced non-small cell lung cancer patients with EGFR mutations in response to first-line treatment with two EGFR-TKIs, gefitinib and erlotinib: a comparative study. BMC Cancer. 2017;17:245 pubmed publisher
    ..If confirmed, our results indicate that erlotinib may play an important role in controlling CNS progression from EGFR mutation-positive NSCLC. ..
  31. Jun I, Park H, Piao H, Han J, An M, Yun B, et al. ANO9/TMEM16J promotes tumourigenesis via EGFR and is a novel therapeutic target for pancreatic cancer. Br J Cancer. 2017;117:1798-1809 pubmed publisher
    ..In addition, high ANO9 expression is a poor prognostic factor in patients with pancreatic cancer. The ANO9/TMEM16J appears to be a clinically useful prognostic marker for pancreatic cancer and a potential therapeutic target. ..
  32. Sun J, Liu N, Zhuang H, Zhao L, Yuan Z, Wang P. Celecoxib-erlotinib combination treatment enhances radiosensitivity in A549 human lung cancer cell. Cancer Biomark. 2017;19:45-50 pubmed publisher
    ..The underlying mechanisms including the enhancement of apoptosis and radiation-induced G0/G1 arrest, possibly via inhibiting the PI3K/AKT signaling pathway. ..
  33. Yip C, Foidart P, Somja J, Truong A, Lienard M, Feyereisen E, et al. MT4-MMP and EGFR expression levels are key biomarkers for breast cancer patient response to chemotherapy and erlotinib. Br J Cancer. 2017;116:742-751 pubmed publisher
    ..We demonstrate that MT4-MMP defines a sub-population of TNBC sensitive to a combination of DNA-targeting chemotherapeutic agents and anti-EGFR drugs. ..
  34. Ai C, Liu Y, Li W, Chen D, Zhu X, Yan Y, et al. Computational explanation for bioactivation mechanism of targeted anticancer agents mediated by cytochrome P450s: A case of Erlotinib. PLoS ONE. 2017;12:e0179333 pubmed publisher
    ..The understanding of the subtle mechanism of bioactivation of Erlotinib will provide theoretical support for toxicological mechanism of EGFR inhibitors. ..
  35. Gao W, Wang M, Wang L, Lu H, Wu S, Dai B, et al. Selective antitumor activity of ibrutinib in EGFR-mutant non-small cell lung cancer cells. J Natl Cancer Inst. 2014;106: pubmed publisher
    ..8 days (95% CI = 26.0 to 33.6 days, P = .008). Our results indicate that ibrutinib could be a candidate drug for treatment of EGFR-mutant NSCLC, including erlotinib-resistant tumors. ..
  36. Goyal S, Jamal S, Shanker A, Grover A. Structural investigations of T854A mutation in EGFR and identification of novel inhibitors using structure activity relationships. BMC Genomics. 2015;16 Suppl 5:S8 pubmed publisher
    ..We report two novel compounds having high predicted inhibitory activity to EGFR TK domain with both wild-type and mutant structure. ..
  37. Ferte C, Besse B, Dansin E, Parent F, Buisine M, Copin M, et al. Durable responses to Erlotinib despite KRAS mutations in two patients with metastatic lung adenocarcinoma. Ann Oncol. 2010;21:1385-7 pubmed publisher
  38. Alexander P, Yuan L, Yang P, Sun T, Chen R, Xiang H, et al. EGF promotes mammalian cell growth by suppressing cellular senescence. Cell Res. 2015;25:135-8 pubmed publisher
  39. Qin X, Lu J, Wang P, Xu P, Liu M, Wang X. Cytochrome P450 3A selectively affects the pharmacokinetic interaction between erlotinib and docetaxel in rats. Biochem Pharmacol. 2017;143:129-139 pubmed publisher
    ..A better understanding of this DDI with CYP3A may help the regulation of the use of these two drugs, avoid potential problems, and adjust dose carefully and early in clinic. ..
  40. Sun H, Ma H, Wang J, Xia L, Zhu G, Wang Z, et al. Phosphatase and tensin homolog deleted on chromosome 10 degradation induced by NEDD4 promotes acquired erlotinib resistance in non-small-cell lung cancer. Tumour Biol. 2017;39:1010428317709639 pubmed publisher
    ..Targeted decrease in NEDD4 expression may be a potential therapeutic strategy for tyrosine kinase inhibitor-resistant non-small-cell lung cancer. ..
  41. Proto C, Lo Russo G, Corrao G, Ganzinelli M, Facchinetti F, Minari R, et al. Treatment in EGFR-mutated non-small cell lung cancer: how to block the receptor and overcome resistance mechanisms. Tumori. 2017;103:325-337 pubmed publisher
    ..The aim of this review is to report recent advances and future perspectives in the treatment of EGFR-mutated NSCLC, highlighting the resistance mechanisms that underlie disease progression. ..
  42. Pool M, Terwisscha van Scheltinga A, Kol A, Giesen D, de Vries E, Lub de Hooge M. 89Zr-Onartuzumab PET imaging of c-MET receptor dynamics. Eur J Nucl Med Mol Imaging. 2017;44:1328-1336 pubmed publisher
    ..001) following NVP-AUY-922 treatment. The results show that 89Zr-onartuzumab PET effectively discriminates relevant changes in c-MET levels and could potentially be used clinically to monitor c-MET status. ..
  43. Zhao Z, Li J, Ye R, Wu X, Gao L, Niu B. A phase II clinical study of combining FOLFIRI and bevacizumab plus erlotinib in 2nd-line chemotherapy for patients with metastatic colorectal cancer. Medicine (Baltimore). 2017;96:e7182 pubmed publisher
    ..5%), bleeding (n?=?31, 25.4%), neutropenia (n?=?23, 18.9%), and platelets (n?=?14, 11.5%).Combining FOLFIRI and BV plus ER in 2nd-line chemotherapy is efficient to treat mCRC patients with acceptable safety. ..
  44. Chen J, Huang Y, Song M, Zhang Z, Xue J. Silicon Phthalocyanines Axially Disubstituted with Erlotinib toward Small-Molecular-Target-Based Photodynamic Therapy. ChemMedChem. 2017;12:1504-1511 pubmed publisher
    ..Various poly(ethylene glycol) (PEG) linker lengths were shown to have an effect on the photophysical/photochemical properties and on in?vitro phototoxicity. ..
  45. Ciardiello F. Maintenance therapy for metastatic colorectal cancer. Lancet Oncol. 2015;16:1444-1445 pubmed publisher
  46. Tanaka H, Inomata M, Hayashi R, Shimokawa K, Tokui K, Okazawa S, et al. [A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity]. Gan To Kagaku Ryoho. 2017;44:595-597 pubmed
    ..4 months, respectively. This clinical course suggests activity of afatinib for central nervous system lesions of EGFRmutated lung cancer. ..
  47. Covell D. A data mining approach for identifying pathway-gene biomarkers for predicting clinical outcome: A case study of erlotinib and sorafenib. PLoS ONE. 2017;12:e0181991 pubmed publisher
    ..Collectively these results suggest complementary roles for biomarker genes and biomarker pathways when predicting clinical responses from preclinical data. ..
  48. Hamaguchi R, Okamoto T, Sato M, Hasegawa M, Wada H. Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC. Anticancer Res. 2017;37:5141-5145 pubmed
    ..Urine pH was significantly increased after the alkaline diet (6.00±0.38 vs. 6.95±0.55; p<0.05). An alkaline diet may enhance the effect of EGFR-TKI treatment in NSCLC patients with EGFR mutations. ..
  49. Schrag D. Optimizing Treatment for Locally Advanced Pancreas Cancer: Progress but No Precision. JAMA. 2016;315:1837-8 pubmed publisher
  50. Jain A, Kameswaran M, Pandey U, Prabhash K, Sarma H, Dash A. 68Ga labeled Erlotinib: A novel PET probe for imaging EGFR over-expressing tumors. Bioorg Med Chem Lett. 2017;27:4552-4557 pubmed publisher
  51. Gutteridge E, Robertson J. Are current drug development programmes realising the full potential of new agents? Tyrosine kinase inhibitors. Breast Cancer Res. 2009;11 Suppl 3:S24 pubmed publisher