Lapatinib: a novel dual tyrosine kinase inhibitor

Pickering, Lisa; Ellis, Paul

doi:10.1007/s11523-007-0047-4

Cited by 3 publications

(3 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…There is also evidence that lapatinib can overcome hormone resistance, caused by crosstalk between HER‐2 and ER, in preclinical models 292. A phase III study by Chowdhary et al293 to compare lapatinib in combination with letrozole vs. letrozole alone in postmenopausal women with ER‐positive MBC, is currently ongoing. Patients are randomized to letrozole with or without lapatinib, regardless of HER‐2 status to test if lapatinib treatment prevents the conversion of ER positive/HER‐2 negative to ER positive/HER‐2 positive breast cancer, thus blocking the development of resistance to endocrine therapy.…”

Section: Egfr/her‐2 Inhibitors In Breast Cancer Therapymentioning

confidence: 99%

ErbB family receptor inhibitors as therapeutic agents in breast cancer: Current status and future clinical perspective

Saxena

Dwivedi

2010

Medicinal Research Reviews

View full text Add to dashboard Cite

Breast cancer is the most common cancer diagnosed in women and the second most common cause of female cancer-related deaths, with more than one million new cases diagnosed per year throughout the world. With the recent advances in the knowledge of cellular processes and signaling pathways involved in the pathogenesis of breast cancer, the current focus of researchers and clinicians is to develop novel treatment strategies that can be included in the armamentarium against breast cancer. With the failure of endocrine-targeted therapy and the development of resistance to existing chemotherapy, the most explored pathway as next generation target for breast cancer therapy has been the epidermal growth factor receptor (EGFR) (ErbB-1)/herceptin-2 (HER-2) (ErbB-2) pathway. This review focuses on the rationale for targeting members of ErbB receptor family and numerous agents that are in use for inhibiting the pathway. The mechanism of action, preclinical and clinical trial data of the agents that are in use for targeting the EGFR/HER-2 pathway and the current status, thereof, have been discussed in detail. In addition, the future clinical trial promises these agents hold either as monotherapy or as combination therapy with conventional agents or with other antisignaling agents have been pondered, so as to provide better and more efficacious treatment strategies for breast cancer patients.

show abstract

Section: Egfr/her‐2 Inhibitors In Breast Cancer Therapymentioning

confidence: 99%

ErbB family receptor inhibitors as therapeutic agents in breast cancer: Current status and future clinical perspective

Saxena

Dwivedi

2010

Medicinal Research Reviews

View full text Add to dashboard Cite

show abstract

“…A phase III study of lapatinib combined with letrozole versus letrozole alone in post-menopausal women with estrogen-receptor positive metastatic breast cancer is currently ongoing. Patients are randomized to letrozole with or without lapatinib regardless of HER-2 status to test that hypothesis that lapatinib treatment may prevent the conversion of ER positive/HER-2 negative to ER positive/HER-2 positive breast cancer, thus blocking the development of resistance to endocrine therapy ( Chowdhury et al 2007 ). Two phase II trials in hormone-resistant, ER positive metastatic breast cancer are currently examining lapatinib as single agent (NCT00225758) or in combination with tamoxifen (NCT00118157).…”

Section: Lapatinib Efficacy Studiesmentioning

confidence: 99%

Targeted treatment of advanced and metastatic breast cancer with lapatinib

Corkery

O’Donovan²,

Crown³

2008

OTT

View full text Add to dashboard Cite

Improved molecular understanding of breast cancer in recent years has led to the discovery of important drug targets such as HER-2 and EGFR. Lapatinib is a potent dual inhibitor of HER-2 and EGFR. Preclinical and phase I studies have shown activity with lapatinib in a number of cancers, including breast cancer, and the drug is well tolerated. The main known drug interactions are with paclitaxel and irinotecan. The most signifi cant side-effects of lapatinib are diarrhea and adverse skin events. Rates of cardiotoxicity compare favorably with trastuzumab, a monoclonal antibody against HER-2. This paper focuses on lapatinib in advanced and metastatic breast cancer, which remains an important therapeutic challenge. Phase II and III studies show activity as monotherapy, and in combination with chemotherapy or hormonal agents. Results from these studies suggest that the main benefi t from lapatinib is in the HER-2 positive breast cancer population. Combinations of lapatinib and trastuzumab are also being studied and show encouraging results, particularly in trastuzumab-refractory metastatic breast cancer. Lapatinib may have a specifi c role in treating HER-2 positive CNS metastases. The role of lapatinib as neoadjuvant therapy and in early breast cancer is also being evaluated.

show abstract

“…It also inhibits cyclin D protein levels in human tumors cell lines and xenografts. 1 Lapatinib is a small molecule inhibitor of kinase and a 4-anilinoquinoline 2 derivative. C 29 H 26 ClFN 4 O 4 S is its molecular formula, and chemically it is N- [3-chloro-4-[(3-fluorophenyl) methoxy] phenyl]-6- [5-[(2methylsulfonylethylamino) methyl]-2-furyl] quinazolin-4-amine 3 (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Determination of Lapatinib in Bulk and Tablet Dosage Form using Ultraviolet Spectrophotometric and RP-HPLC Analytical Methods

Mondal¹,

Biswal²,

Acharya³

et al. 2021

JPHI

View full text Add to dashboard Cite

Objectives:The present article involved the development of sensitive and validated Ultraviolet (UV) Spectrophotometric and reverse phase liquid chromatographic and method for the determination of lapatinib in bulk and pharmaceutical dosage form. Materials and Methods: The present UV method is based on measurement of absorption at maximum at 268 nm using methanol as a solvent. In the High Performance Liquid Chromatography (HPLC) method, Waters HPLC with Empower-2 Software with PDA Detector was utilised. Acetonitrile and phosphate buffer in the ratio of 65:35 (v/v) utilised as a mobile phase. Results: In the UV Spectrophotometric method the drug obeyed beer lambert's law in the concentration range of 2-20 μg/ml with regression coefficient 0.999. In HPLC method the linearity level was 20-200 μg/ml. The developed UV and HPLC methods have been successfully applied in the validation study. The percentage purity of the marketed dosage form of lapatinib was found 99.68 % and 99.82% for UV and HPLC method. In both methods, the percent RSD of all the validation parameters examined as recommended in the ICH guidelines was found to be less than 2. The highest degradation (19.58%) occurs in alkaline stressed environments in the force degradation analysis by HPLC technique. The degradation of lapatinib is also associated with remaining stressed conditions. Conclusion: The two methods developed were found to be accurate, simple and validated for estimating lapatinib in the form of bulk and tablet doses.

show abstract

Lapatinib: a novel dual tyrosine kinase inhibitor

Cited by 3 publications

References 33 publications

ErbB family receptor inhibitors as therapeutic agents in breast cancer: Current status and future clinical perspective

ErbB family receptor inhibitors as therapeutic agents in breast cancer: Current status and future clinical perspective

Targeted treatment of advanced and metastatic breast cancer with lapatinib

Determination of Lapatinib in Bulk and Tablet Dosage Form using Ultraviolet Spectrophotometric and RP-HPLC Analytical Methods

Contact Info

Product

Resources

About