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Literature DB >> 18409020

Lapatinib: a sword with two edges.

Abstract

Lapatinib is an oral dual tyrosine kinase inhibitor targeting EGFR1 and EGFR2 (HER2). Phase I trials have shown that lapatinib is well tolerated, with mild diarrhea and skin rush as common adverse effects, and low cardiotoxicity. Phase II and III trials provided evidences on clinical effectiveness in advanced or metastatic breast cancer and potential against brain metastases. Lapatinib is active in combination with trastuzumab and in trastuzumab-resistant patients, moreover it has synergistic action with capecitabine. Several clinical trials are in progress to explore the effectiveness of lapatinib in other combinations and against several tumor types.

Entities: Chemical Disease Gene Species

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Year: 2008 PMID： 18409020 DOI： 10.1007/s12253-008-9018-z

Source DB: PubMed Journal: Pathol Oncol Res ISSN： 1219-4956 Impact factor: 3.201

26 in total

1. Insulin-like growth factor-I receptor/human epidermal growth factor receptor 2 heterodimerization contributes to trastuzumab resistance of breast cancer cells.

Authors: Rita Nahta; Linda X H Yuan; Bing Zhang; Ryuji Kobayashi; Francisco J Esteva
Journal: Cancer Res Date: 2005-12-01 Impact factor: 12.701

2. Lapatinib moves forward in inflammatory and early HER2-positive breast cancer trials.

Authors: Rabiya S Tuma
Journal: J Natl Cancer Inst Date: 2007-03-07 Impact factor: 13.506

3. A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer.

Authors: Wenle Xia; Sarah Bacus; Priti Hegde; Intisar Husain; Jay Strum; Leihua Liu; Georgina Paulazzo; Ljuba Lyass; Patricia Trusk; Jason Hill; Jennifer Harris; Neil L Spector
Journal: Proc Natl Acad Sci U S A Date: 2006-05-08 Impact factor: 11.205

4. Efficacy and safety of trastuzumab as a single agent in first-line treatment of HER2-overexpressing metastatic breast cancer.

Authors: Charles L Vogel; Melody A Cobleigh; Debu Tripathy; John C Gutheil; Lyndsay N Harris; Louis Fehrenbacher; Dennis J Slamon; Maureen Murphy; William F Novotny; Michael Burchmore; Steven Shak; Stanford J Stewart; Michael Press
Journal: J Clin Oncol Date: 2002-02-01 Impact factor: 44.544

5. The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer.

Authors: Isabel Chu; Kimberly Blackwell; Susie Chen; Joyce Slingerland
Journal: Cancer Res Date: 2005-01-01 Impact factor: 12.701

6. Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor I signaling.

Authors: Rita Nahta; Linda X H Yuan; Yi Du; Francisco J Esteva
Journal: Mol Cancer Ther Date: 2007-02 Impact factor: 6.261

7. Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy.

Authors: Lynsey A McHugh; Marina Kriajevska; John K Mellon; Thomas R Griffiths
Journal: Urology Date: 2007-02 Impact factor: 2.649

8. Delineation of molecular mechanisms of sensitivity to lapatinib in breast cancer cell lines using global gene expression profiles.

Authors: Priti S Hegde; David Rusnak; Melissa Bertiaux; Krystal Alligood; Jay Strum; Robert Gagnon; Tona M Gilmer
Journal: Mol Cancer Ther Date: 2007-05 Impact factor: 6.261

9. A phase III randomized comparison of lapatinib plus capecitabine versus capecitabine alone in women with advanced breast cancer that has progressed on trastuzumab: updated efficacy and biomarker analyses.

Authors: David Cameron; Michelle Casey; Michael Press; Deborah Lindquist; Tadeusz Pienkowski; C Gilles Romieu; Stephen Chan; Agnieszka Jagiello-Gruszfeld; Bella Kaufman; John Crown; Arlene Chan; Mario Campone; Patrice Viens; Neville Davidson; Vera Gorbounova; Johannes Isaac Raats; Dimosthenis Skarlos; Beth Newstat; Debasish Roychowdhury; Paolo Paoletti; Cristina Oliva; Stephen Rubin; Steven Stein; Charles E Geyer
Journal: Breast Cancer Res Treat Date: 2008-01-11 Impact factor: 4.872

10. Protein kinase Calpha determines HER2 fate in breast carcinoma cells with HER2 protein overexpression without gene amplification.

Authors: Alessandra Magnifico; Luisa Albano; Stefano Campaner; Manuela Campiglio; Silvana Pilotti; Sylvie Ménard; Elda Tagliabue
Journal: Cancer Res Date: 2007-06-01 Impact factor: 12.701

13 in total

Review 1. Omics and therapy - a basis for precision medicine.

Authors: Joseph P Garay; Joe W Gray
Journal: Mol Oncol Date: 2012-03-08 Impact factor: 6.603

2. Cytochrome P450 3A4 and CYP3A5-Catalyzed Bioactivation of Lapatinib.

Authors: Joanna K Towles; Rebecca N Clark; Michelle D Wahlin; Vinita Uttamsingh; Allan E Rettie; Klarissa D Jackson
Journal: Drug Metab Dispos Date: 2016-07-22 Impact factor: 3.922

3. Additive impact of HER2-/PTK6-RNAi on interactions with HER3 or IGF-1R leads to reduced breast cancer progression in vivo.

Authors: Natalie Falkenberg; Nataša Anastasov; Ines Höfig; Ksenia Bashkueva; Katrin Lindner; Heinz Höfler; Michael Rosemann; Michaela Aubele
Journal: Mol Oncol Date: 2014-09-06 Impact factor: 6.603

Lapatinib: a sword with two edges.

1. Insulin-like growth factor-I receptor/human epidermal growth factor receptor 2 heterodimerization contributes to trastuzumab resistance of breast cancer cells.

2. Lapatinib moves forward in inflammatory and early HER2-positive breast cancer trials.

3. A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer.

4. Efficacy and safety of trastuzumab as a single agent in first-line treatment of HER2-overexpressing metastatic breast cancer.

5. The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer.

6. Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor I signaling.

7. Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy.

8. Delineation of molecular mechanisms of sensitivity to lapatinib in breast cancer cell lines using global gene expression profiles.

9. A phase III randomized comparison of lapatinib plus capecitabine versus capecitabine alone in women with advanced breast cancer that has progressed on trastuzumab: updated efficacy and biomarker analyses.

10. Protein kinase Calpha determines HER2 fate in breast carcinoma cells with HER2 protein overexpression without gene amplification.

Review 1. Omics and therapy - a basis for precision medicine.

2. Cytochrome P450 3A4 and CYP3A5-Catalyzed Bioactivation of Lapatinib.

3. Additive impact of HER2-/PTK6-RNAi on interactions with HER3 or IGF-1R leads to reduced breast cancer progression in vivo.

4. In vitro assessment of the photo(geno)toxicity associated with Lapatinib, a Tyrosine Kinase inhibitor.

Review 5. Targeted therapy in HER2-positive breast cancer.

6. Lapatinib induces autophagy, apoptosis and megakaryocytic differentiation in chronic myelogenous leukemia K562 cells.

7. Lapatinib induces autophagic cell death and differentiation in acute myeloblastic leukemia.

8. Integrating diverse information to gain more insight into microarray analysis.

9. Lapatinib induces autophagic cell death and inhibits growth of human hepatocellular carcinoma.

10. Synthesis, Biological Evaluation and Docking Analysis of Some Novel Quinazolin Derivatives as Antitumor Agents.