As a kinase inhibitor, Lapatinib Ditosylate, CAS number 388082-78-8 is efficacious when used to treat metastatic breast cancer. The ability of lapatinib ditosylate to inhibit deviating active kinases within cancer cells, and prevent cell division, makes it an effective choice for patients with advanced breast cancer. Also known as Tykerb, which is marketed by GlaxoSmithKline, lapatinib ditosylate is often given to patients in conjunction with capecitabine, for the treatment of advanced breast cancer. Lapatinib Ditosylate is effectual when combined with capecitabine when treating patients whose tumors overexpress HER2, and who have received prior therapy including an anthracycline, a taxane, and trastuzumab. In combination with letrozole for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer, lapatinib ditosylate is extremely capable and effective. Lapatinib Ditosylate joins the kinase inhibitor group of drugs alongside several other powerhouse cancer opponents, such as Gefitinib, Erlotinib, Dasatinib, Nilotinib and Temsirolimus, which LGM Pharma is proud to provide to clients for research and development purposes.
Dosing of lapatinib ditosylate for patients with metastatic breast cancer is a 1,250 milligram tablet, administered once daily for days 1-21, in combination with 2,000 milligrams twice daily of capecitabine. Patients being treated for HER2 positive metastatic breast cancer typically receive a 1500 milligram tablet once daily, alongside 2.5 milligrams of letrozole daily. Lapatinib Ditosylate was approved on January 29, 2010 by the FDA, after a clinical trial deemed EGF30008 showed a meaningful increase in progression free disease and additional survival rates for patients. Adverse effects were reported, albeit in less than 10 percent of patients. Diarrhea, fatigue, nausea and rash were the most commonly reported side effects.
On April 1, 2012 the Pharmaceutical Management Agency Clinicians’ Newsletter published exciting news regarding their decision to fund the use of lapatinib ditosylate. PHARMAC’s Exceptional Circumstances, also known as Named Patient Pharmaceutical Assessment, or NPPA, announced that lapatinib (Tykerb) will be funded as an alternative to trastuzumab (Herceptin) for first line treatment of patients metastatic breast cancer. Both drug treatments, lapatinib and trastuzumab, will also be funded for these patients with HER 2 positive metastatic breast cancer who experience early intolerance to their first choice in the study. The unique method of administration for lapatinib as an oral tablet patients can take at home is an easier and viable option compared to trastuzumab, which must be administered by IV infusion in a hospital. This announcement of funding for lapatinib ditosylate is only the beginning of what is sure to ignite future research with the array of kinase inhibitors.
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