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Mechanism of action and preclinical development of afatinib


, : Mechanism of action and preclinical development of afatinib. Medicina Clinica 146 Suppl 1: 7-11

Afatinib, together with gefitinib and erlotinib, is approved for first-line treatment of advanced non-small cell lung cancer (NSCLC) with activating mutations of the epidermal growth factor receptor (EGFR). This is an irreversible inhibitor of the ErbB family, acting on EGFR (HER1, ErbB1), ErbB2 (HER2) and ErbB4 (HER4). Covalent attachment to cysteine residues in the catalytic domain of EGFR, HER2 and ErbB4 inhibits the tyrosine kinase activity (TKIs) of these receptors, decreasing auto- and transphosphorylation between ErbB dimers, and thus blocking the activity of downstream signalling pathways related to growth and apoptosis suppression. In preclinical models, this has resulted in a reduction in tumour size. Furthermore, due to its mechanism of action, afatinib may be more potent than the first-generation EGFR TKIs (gefitinib and erlotinib) and may even be able to overcome acquired resistance to such treatments. Finally, because of the demonstrated synergism with other chemotherapeutic and target agents, it could be interesting to enhance its clinical development in combination with other drugs.

US$19.90

PMID: 27426242

DOI: 10.1016/S0025-7753(16)30257-3


Other references

Emrovic, B., 1967: Selecting diameter increment sample trees (from which the increment cores are to be extracted) when using Meyer's method of tariff differences. Describes a method of selecting sample trees so that the standard deviation of the stand volume increment calculated from increment cores from the sample trees is at a minimum. A relationship is derived showing that the size of sample in any diame...

Bivigou-Mboumba, B.; François-Souquière, S.; Deleplancque, L.; Sica, J.; Mouinga-Ondémé, A.; Amougou-Atsama, M.; Chaix, M-Laure.; Njouom, R.; Rouet, Fçois., 2016: Broad Range of Hepatitis B Virus (HBV) Patterns, Dual Circulation of Quasi-Subgenotype A3 and HBV/E and Heterogeneous HBV Mutations in HIV-Positive Patients in Gabon. Integrated data on hepatitis B virus (HBV) patterns, HBV genotypes and mutations are lacking in human immunodeficiency virus type 1 (HIV-1) co-infected patients from Africa. This survey was conducted in 2010-2013 among 762 HIV-1-positive adults fr...

Mihăilă, D.Elena.; Potecă, T.D.; Potecă, A.; Piţuru, S., 2015: Single-centre epidemiological study on the incidence of hepatic hydatid cyst. Echinococcosis is a parasitic disease caused by Echinococcus granulosus tapeworm through its larva infestation. Hydatid cyst has become a health problem interesting by the demographic changes in recent years. If until recently it was a disease of...

Planagumà, Jús.; Díaz-Fuertes, Mía.; Gil-Moreno, A.; Abal, M.; Monge, M.; García, A.; Baró, T.; Thomson, T.M.; Xercavins, J.; Alameda, F.; Reventós, J., 2004: A differential gene expression profile reveals overexpression of RUNX1/AML1 in invasive endometrioid carcinoma. Endometrial carcinoma is the most common gynecological malignant disease in industrialized countries. Two clinicopathological types of endometrial carcinoma have been described, based on estrogen relation and grade: endometrioid carcinoma (EEC) an...

Wu, V.W.; Krzan, M.; Zhao, B.; Schwartz, J.P., 1997: Differential effects of beta-adrenergic receptor stimulation in normal adult and reactive astrocytes. Society for Neuroscience Abstracts 23(1-2): 49

Hsu, Sh, 1978: Study on the dew. 2. Contribut. Journal (new ser103) 59-64

D.Haan, H., 1957: The breeding of agricultural crops in its home and foreign aspects. In this survey of the technical and financial organization of breeding in the Netherlands, the chief topics discussed are: (1) breeding methods used; (2) the distribution of improved varieties; (3) costs of breeding; (4) maintenance of varieties;...

von Houwelingen, R.; Nordøy, A.; van der Beek, E.; Houtsmuller, U.; de Metz, M.; Hornstra, G., 1987: Effect of a moderate fish intake on blood pressure, bleeding time, hematology, and clinical chemistry in healthy males. This paper describes the outline and first results of an international study to investigate the effect of a reasonable amount of dietary fish on some aspects of cardiovascular risk. In Maastricht and Zeist, The Netherlands, and Tromso, Norway, he...

Miller, C.H., 2002: Applied research still needed on infection control procedures. American Journal of Dentistry 13(5): 285-286

Yu, X.Q.ng; Moen, A.; Feet, B.A.ge; Saugstad, O.D.drik, 1996: Nitric oxide synthase inhibition prevents surfactant-induced cerebral vasodilatation in newborn piglets with surfactant deficiency. Pediatric Research 39(4 PART 2): 356A