Lapatinib powder is an oral reversible small-molecule tyrosine kinase inhibitor against HER-1 / HER-2. Lapatinib has a different mechanism from the approved humanized monoclonal antibody drug Herceptin. It can downregulate cell proliferation signals by double blocking the HER-1 / HER-2 pathway. The clinical indication is the combination of capecitabine in the treatment of HER2 overexpression and has received advanced anthracycline, taxanes, and trastuzumab for advanced or metastatic breast cancer. The effective rate of first-line single drug treatment in the late stage is about 12 ~ 24%. The general clinical guidelines recommend second-line drugs. The effective rate of combined treatment with capecitabine is about 26 ~ 33%, and the maximum clinical benefit rate is 71.3%. It is also the most commonly used lapatinib combined chemotherapy regimen.
| Molecular formula |
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Item |
Standard |
Test Results |
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|
Appearance |
White or sticky yellow powder |
Conforms |
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|
Other Amino Acids |
Chromatographically not detectable |
Conforms |
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|
Assay |
99.0~101.0% |
99.5% |
|
|
PH |
4.10~5.60 |
4.90 |
|
|
State of solution (Transmittance) |
≥98.0% |
99.8% |
|
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Chloride(Cl) |
≤0.011% |
0.010% |
|
|
Ammonium(NH4) |
≤0.020% |
0.020% |
|
|
Sulfate(SO4) |
≤0.010% |
0.010% |
|
|
Iron(Fe) |
≤10ppm |
10ppm |
|
|
Heavy metals(Pb) |
≤10ppm |
10ppm |
|
|
Arsenic(As2O3) |
≤1ppm |
1ppm |
|
|
Loss on drying |
≤0.50% |
0.10% |
|
|
Related Substance |
≤0.20% |
0.06% |
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|
Microbial assessment |
Compliance with indicators |
Conforms |
|
|
BSE |
not detected |
not detected |
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GMO |
not detected |
not detected |
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|
Allergen |
not detected |
not detected |
|
|
Radiation |
not detected |
not detected |
|
| Conclusion： |
Conform with enterprise specification . |
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What is the pharmacological action of lapatinib?
Lapatinib powder is a tyrosine kinase inhibitor, which mainly acts on epithelial growth factor receptor (EGFR). EGFR has an important effect on the growth of cancer cells. If the receptors of cancer cells are overexpressed or over-activated, the cancer cells will grow in large numbers, which will increase the difficulty of cure and the probability of recurrence. EGFR receptors can be divided into four kinds of human epithelial growth factor receptors. The first type is usually called EGFR, while the second type is called HER2, and others have types 3 and 4. Among these four types, the existence of type II receptor is the most important, because the overexpression and over activation of type II receptors are inversely proportional to the cure probability of breast cancer patients, that is, if the cancer cells of patients have type II receptor, the lower the cure rate, the higher the recurrence rate and the shorter the predicted survival time.
Lapatinib not only blocks the type I receptor (EGFR) but also blocks the type II receptor (HER2). This dual inhibitory effect can effectively cut off the downstream signal transmission of tyrosine kinase, and then stop the rapid proliferation of cancer cells. About 20 to 30% of breast cancer patients suffer from overexpression of type I and type II receptors, so lapatinib can effectively slow down the progression of cancer.
Another cancer treatment drug similar to lapatinib is trastuzumab. Trastuzumab is similar to lapatinib in that both can block type I and type II receptors under the EGFR family, but the principle of action of lapatinib is slightly different from trastuzumab. EGFR receptors exist outside and inside cells. Trastuzumab can only block extracellular receptors, while lapatinib can block receptors inside and outside cells. Truncated receptors in EGFR receptors are only located in cells, so lapatinib can effectively block this type of receptor, and truncated receptors have stronger activity than general receptors. These two points make lapatinib with a dual inhibitory effect more effective than a single inhibitor like trastuzumab and can avoid cross-resistance.
Studies have shown that breast cancer patients treated with trastuzumab have a higher chance of cancer metastasis to the brain, which may be caused by the cerebrovascular barrier blocking the entry of larger molecules of trastuzumab into the brain. The small molecular properties of lapatinib can make it cross the cerebrovascular barrier and treat metastatic brain tumors.
What are the drug interactions of lapatinib?
In vitro, Lapatinib powder can inhibit CYP3A4 and cyp2c8 at the therapeutic concentration and are mainly metabolized by CYP3A4. Drugs that inhibit this enzyme activity can significantly increase the blood concentration of lapatinib. Ketoconazole, 0.2g each time, twice a day, can increase lapatinib auc3 ~ 7 times and prolong the half-life by 1.7 times after 7 days. Healthy volunteers took the CYP3A4 inducer orally, 100mg each time, twice a day. After 3 days, it was changed to 200mg each time, twice a day for 17 days. The AUC of lapatinib decreased by 72%. Lapatinib is a transporter of P-glycoprotein. Drugs that inhibit glycoprotein may increase the blood concentration of the drug.
Why can lapatinib be authorized in the EU? What are the risks associated with him?
The European Drug Administration decided that the benefits of Lapatinib outweighed its risks and could authorize its use in the EU. The combined use of Lapatinib and other anticancer drugs has been shown to increase the survival rate of breast cancer patients producing large amounts of HER2, and its side effects are considered acceptable.
Lapatinib initially received; conditional approval. This means that there is more evidence to prove the effectiveness of drugs. As the company has provided the necessary additional information, the authorization has changed from conditional approval to full approval.
The most common side effects of Lapatinib (which may affect more than a quarter of patients) are rashes and side effects affecting the stomach and intestines (such as diarrhea, nausea (feeling nausea), and vomiting). When Lapatinib powder is taken with capecitabine, redness and swelling of palms and soles (rashes and numbness on the palms and soles of feet) are also common. For a complete list of Lapatinib's side effects and limitations, please contact us and we will provide relevant materials.
A variety of shipping methods for you to choose
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Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
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3-7 days |
DHL,Germany DHL,Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
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7-15 days |
By Air |
Suitable for more than 50kg. |
|
|
15-60 days |
By Sea |
Suitable for more than 500kg. |
Our strengths:
Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China,Our company can provide Lapatinib Powder etc. at a more favorable price. If you are interested, please leave a message.
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