Tykerb (231277-92-2)-The killer of breast caner | AASraw buy Tykerb
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Lapatinib powder video




I.Lapatinib powder basic Characters:


Name: Lapatinib powder
CAS: 231277-92-2
Molecular Formula: C29H26ClFN4O4S
Molecular Weight: 581.05
Melt Point: 136-140°C
Storage Temp: Refrigerator
Color: White or off white Crystalline powder



1.Tykerb powder basic Characters.


Name Tykerb
Cas 231277-92-2
Molecular Formula C29H26CIFN4O4S
Molecular Weight 581.05
Color White or off white Crystalline powder
Other name lapatini



2.What is Tykerb?


Trade names Tykerb and Tyverb is an orally active drug for breast cancer and other solid tumours. It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. It is used in combination therapy for HER2-positive breast cancer. It is used for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 (ErbB2).Mostly U.S caled Tyker and mostly Europe and Russia called Tyverb.In January 2010, Tykerb received accelerated approval for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer Lapatinib inhibits receptor signal processes by binding to the ATP-binding pocket of the EGFR/HER2 protein kinase domain, preventing self-phosphorylation and subsequent activation of the signal mechanism,Tykerb (lapatinib) is a cancer medication used together with another medicine called capecitabine (Xeloda) to treat a certain type of advanced breast cancer that has spread to other parts of the body, and is usually given after other cancer medications have been tried without successful treatment of symptoms




3.How does Tykerb work?


breast Cancer treatment has focused primarily on killing rapidly dividing cells because one feature of breast cancer cells is that they divide rapidly.Targeted therapy is about identifying other features of breast cancer cells.There are different types of targeted therapies, defined in three broad categories. Some targeted therapies focus on the internal components and function of the breast cancer cell. The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die. There are several types of targeted therapy that focus on the inner parts of the cells. Other targeted therapies target receptors that are on the outside of the cell. Therapies that target receptors are also known as monoclonal antibodies. Antiangiogenesis inhibitors target the blood vessels that supply oxygen to the cells, ultimately causing the cells to starve.Pertuzumab is a monoclonal antibody which targets the surface of the cells human epidermal growth factor receptor 2 protein (HER2) on the cancer cell, interfering with HER2 causing breast cancer cell death. Pertuzumab binds to a different area of the HER2 protein than trastuzumab so that when pertuzumab is combined with trastuzumab, a more complete blockage of HER2 signaling occurs.Inside a HER2-positive breast cancer cell, HER2 receptors use protein signals, called kinases, to cause the cell to grown and divide abnormally. Kinases control how much energy the cells have to grow and multiply. Breast cancer cells that overexpress HER2 can have too much kinase activity, so the cancer cells grow too much, too fast.Tykerb works by interfering with HER2-related kinases inside the cell, limiting the amount of energy breast cancer cells have to grow and multiply. By limiting the amount of energy, Tykerb can slow or stop the growth of breast cancer.




4.Will Tykerb Work for You?


Four different tests can be used to figure out if the cancer is HER2-positive and if it will likely respond to Tykerb:


  • IHC (ImmunoHistoChemistry)

IHC is the most commonly used test to see if a tumor has too much of the HER2 receptor protein on the surface of the cancer cells.The IHC test gives a score of 0 to 3+ that indicates the amount of HER2 receptor protein in tumors. If the tumor scores 0 to 1+, it’s called “HER2 negative.” If it scores 2+ or 3+, it’s called “HER2 positive.”Women with IHC positive scores tend to respond favorably to Tykerb. The drug is not considered effective for tumors with IHC scores of 0 or 1+.


  • FISH (Fluorescence In Situ Hybridization)

The FISH test looks for the HER2 gene abnormality. This test is the most accurate, but less available, way to find out if a breast tumor is likely to respond to Tykerb..

With the FISH test, you get a score of either “positive” or “negative” (some hospitals call a negative test “zero”). If the cancer is FISH positive, it will probably respondwell to Tykerb.


The SpoT-Light HER2 CISH test looks for HER2 genes in a breast cancer tissue sample. The SpoT-Light test uses a stain that makes HER2/neu genes change color.With the SPoT-Light test, you get a score of either “positive” or “negative.” If the cancer is SPoT-Light positive, it will probably respond well to Tykerb.


  • Inform HER2 Dual ISH (In Situ Hybridization)

The Inform HER2 Dual ISH test uses a special stain that makes HER2 proteins change color. The stain is applied to the breast cancer tissue sample and viewed under a microscope. This test offers more precise results than the IHC HER test.With the Inform HER2 Dual ISH test, you get a score of either “HER2 positive” or “HER2 negative.”



5.What are Tykerb’s drug interactions?


Tykerb is processed by the liver enzyme CYP3A4. Drugs that inhibit or induce CYP3A4 can affect the concentration of Tykerb in the body. Inhibitors increase blood levels of Tykerb and inducers reduce its blood levels. Dose adjustments of Tykerb should be considered for patients receiving strong CYP3A4 inhibitors or inducers. The following is not a comprehensive list of inhibitors and inducers.Inhibitors: ketoconazole, clarithromycin, atazanavir, nefazodone, nelfinavir (Viracept), telithromycin, and voriconazole.Inducers: dexamethasone, phenytoin, carbamazepine, rifampin, phenobarbital, and St John’s wort.



6.Tykerb Side Effects


Common side effects of Tykerb include:

nausea,vomiting,upset stomach,mouth sores,rash,dry skin,pain or redness on the palms of your hands or soles of your feet,hair loss,problems with your fingernails or toenails, andtrouble sleeping.When Tykerb is given with Xeloda chemotherapy, you may also experience chemotherapy side effects. In particular, Xeloda is associated with neuropathy, or redness and tingling in the hands and feet.When Tykerb is given with Femara, you also may have Femara side effects. Common side effects of Femara are bone thinning and bone and joint pain.Tykerb does not seem to cause the more severe heart and lung problems associated with Herceptin.If you become pregnant or think you may be pregnant, tell your doctor. It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breastfeeding while using this drug is not recommended.



7.What are warnings and precautions for Tykerb?


  • Tykerb may affect how well the heart pumps blood. Confirm normal left ventricular ejection fraction (LVEF) before starting Tykerb and continue to monitor during therapy.
  • Tykerb rarely causes liver dysfunction. Monitor liver function before treatment and every 4-6 weeks during therapy.
  • Tykerb may cause diarrhea. If diarrhea occurs, manage with anti-diarrheal agents and fluid replacement.
  • Tykerb may cause severe lung problems. Discontinue Tykerb if symptoms of this occur.
  • Tykerb may cause severe skin reactions. Discontinue Tykerb if this occurs.




8.What is the dosage of Tykerb?


  • Tykerb is supplied as 250 mg tablets. Five tablets are taken once daily at  every day on an empty stomach for 21 days in a 21-day cycle. Do not crush or chew tablets. Store at room temperature and keep container closed tightly. T Tykerb is given with Xeloda (capecitabine) 2000mg/m2/day administered orally in 2 divided doses, 12 hours apart for the first 14 days of each 21-day treatment cycle. Capecitabine should be taken with food or 30 minutes after food.
  • Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.
  • The dose your doctor recommends may be based on the following:
  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your weight,your height,your age,your gender


The recommended dosage of lapatinib for advanced or metastatic breast cancer is 1,250 mg (5 tablets) given by mouth once daily on Days 1-21.The recommended dose of lapatinib for hormone receptor-positive (HER2-positive) metastatic breast cancer is 1,500 mg (6 tablets) given orally once daily continuously in combination with letrozole.



9.What is the cost of Tykerb?


Average Wholesale Price: $30.10 per 250 mg tablet

21 Day Supply (1 cycle): $3,160.50



10.What are Tykerb’s drug interactions?


Tykerb is processed by the liver enzyme CYP3A4. Drugs that inhibit or induce CYP3A4 can affect the concentration of Tykerb in the body. Inhibitors increase blood levels of Tykerb and inducers reduce its blood levels. Dose adjustments of Tykerb should be considered for patients receiving strong CYP3A4 inhibitors or inducers. The following is not a comprehensive list of inhibitors and inducers.

Inhibitors: ketoconazole, clarithromycin, atazanavir, nefazodone, nelfinavir (Viracept), telithromycin, and voriconazole.

Inducers: dexamethasone, phenytoin, carbamazepine, rifampin, phenobarbital, and St John’s wort.



11.What if i overdoes?


If you overdoes lapatinib, call your doctor or poison control center, or go to the nearest hospital emergency room right away. Take lapatinib tablets with you when possible.



12.Where can i get more information?


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Every effort has been made to ensure that the information provided by AASraw up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. AASraw information has been compiled for use by healthcare practitioners and consumers in the United States and therefore AASraw does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. AASraw’s drug information does not endorse drugs, diagnose patients or recommend therapy. AASraw’s drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. AASraw does not assume any responsibility for any aspect of healthcare administered with the aid of informationAASraw provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.




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