We supply Lapatinib 

We're proud to offer our guests Lapatinib API. This high- quality product is a vital element used in the manufacturing of cancer treatment specifics. With its effectiveness in treating hormone receptor positive bone cancer, it has come a sought- after component in the pharmaceutical assiduity. Our Lapatinib base is strictly tested to insure its chastity and energy, giving you the confidence you need when producing life- saving specifics. We're devoted to furnishing our guests with dependable and safe products, and Lapatinib  is no exception. Let us help you take the first step towards giving stopgap to cancer cases around the world.

What's Lapatinib base?

Lapatinib powder, trade name Tykerb, is an oral, reversible small patch tyrosine kinase asset targeting HER- 1/ HER- 2. it has a different medium of action from the approved humanized monoclonal antibody medicine Herceptin, and can downregulate cell proliferation signals by binary blocking the HER- 1/ HER- 2 pathway. The clinical suggestion is the combination with capecitabine for the treatment of advanced or metastatic bone cancer with HER2 overexpression and former treatment with anthracyclines, taxanes, and trastuzumab. The efficacity of monotherapy in the first- line of advanced stage is about 12~24% The general clinical guidelines recommend alternate- line drug. The efficacity of concerted treatment with capecitabine is about 26~ 33%, and the clinical benefit rate can reach up to 71.3%. It's also the most generally used it combined chemotherapy authority.

Basic Information

Product Name: Lapatinib

CAS: 231277-92-2

MF: C29H26ClFN4O4S

MW: 581.06

EINECS: 1806241-263-5

MDL No.: MFCD09264194

Structural formula:

Origin: China

Delivery Time: in stock

Technical Specification

Package: 10g; 100g; 1kg or according to your demands

Storage: Preserve in tight,light-resistant containers in cool place

Shelf Life: 2 years

Indications

Lapatinib API, in combination with capecitabine, is suitable for the treatment of cases with advanced or metastatic bone cancer who have HER2( ErbB- 2 overexpression) and have preliminarily entered treatments including anthracyclines, paclitaxel, and trastuzumab.

Drug interactions

In vitro, lapatinib tablets can inhibit CYP3A4 and CYP2C8 at remedial attention, and are substantially metabolized by CYP3A4. medicines that inhibit the exertion of this enzyme can significantly increase the tube attention of lapatinib. Ketoconazole, 0.2 g each time, 2 times/ d, can increase the AUC of lapatinib by 3 to 7 times after 7 days, and extend the half- life by 1.7 times. Healthy levies took the CYP3A4 debaser orally, 100 mg twice a day, and also changed to 200 mg twice a day after 3 days for 17 days. The AUC of lapatinib was reduced by 72%. Lapatinib is a transporter of P- glycoprotein, and medicines that inhibit glycoprotein may increase the blood attention of the medicine.

Pharmacology and toxicology

Lapatinib tosylate tablets are a small patch 4- anilinoquinazoline receptor tyrosine kinase asset that inhibits epidermal growth factor receptor( ErbB1) and mortal epidermal factor receptor 2( ErbB2). Among the four bone cancer cell lines, BT474 and SKBr3 are sensitive to lapatinib, with half inhibitory attention of 25 and 32 nmol/ L. MDA- MB- 468 and T47D cell lines are asleep, with half inhibitory attention at the micromolar position. For bladder Two cancer cell lines, RT112( high expression of ErbB1 and ErbB2) and J82( low expression of ErbB1 and ErbB2), enhance the efficacity of cisplatin. It can inhibit epidermal factor- driven excrescence growth in a variety of creatures. Lapatinib is effective against trastuzumab- resistant excrescence cell lines.

New drugs for targeted treatment of breast cancer

Lapatinib powder is a new targeted treatment medicine for bone cancer developed by the British company GlaxoSmithKline. It's a tyrosine kinase asset that can effectively inhibit mortal epidermal growth factor receptor- 1( ErbB1) and mortal epidermal growth factor. Receptor- 2( ErbB2) tyrosine kinase exertion. It's unique in that it works through multiple pathways to help bone cancer cancer cells from entering the signals they need to grow. The medium of action is to inhibit the ATP spots of intracellular EGFR( ErbB- 1) and HER2( ErbB- 2) to help the phosphorylation and activation of excrescence cells, through the homogeneous conflation of EGFR( ErbB- 1) and HER2( ErbB- 1). Heterodimers block downregulatory signals. Molecular targeted remedy of bone cancer refers to the treatment of oncogenes and their affiliated expression products related to the circumstance and development of bone cancer. Molecular targeted medicines control changes in cell gene expression by blocking signal transduction of excrescence cells or related cells, thereby inhibiting or killing excrescence cells. On March 14, 2007, the U.S. Food and Drug Administration approved the combination of lapatinib and Xeloda( capecitabine) for the treatment of mortal epidermal factor receptor 2( ErbB2) overexpression and treatment with anthracyclines, paclitaxel, and tretinib. Cases with advanced or metastatic bone cancer treated with tocilizumab. Clinical trials have shown that this product also has good clinical goods for cases with HER2- type bone cancer who have developed resistance to Roche's Herceptin. Lapatinib is a new type of targetedanti-cancer medicine. It can act on both Her- 1 and Her- 2 targets contemporaneously. The natural effect of inhibiting excrescence cell proliferation and growth produced by this mode of action is far lesser than inhibiting only one of the targets. The so- called targeted remedy medicines relate to medicines that target certain receptors, genes or crucial proteins to kill applicable excrescence cells in a targeted manner.

mortal ErbB receptors belong to the type I receptor tyrosine kinase( TK) family. Including ErbB1( EGFR), ErbB2( HER2), ErbB3( HER3) and ErbB4( HER4). ErbB- 1( EGFR) and ErbB- 2( HER- 2) receptors are frequently overexpressed or else altered in cancer cases. It's presently known that mortal epidermal growth factor receptor- 2( ErbB- 2, HER- 2) is a well- understood mortal oncogene nearly related to bone cancer. Its high expression in bone cancer frequently indicates that it's easy to develop lymph bumps. Metastasis and excrescence isolation are poor, and the prognostic is poor. With the deepening of exploration on HER- 2, it has come one of the target motes for bone cancer-specific treatment.

Adverse reactions

The most common adverse responses of lapatinib are gastrointestinal responses, which include nausea, puking, diarrhea and other symptoms. In addition, adverse skin responses may do, similar as rashes. The adverse responses are fairly mild, and serious adverse responses, similar as cardiotoxicity and interstitial lung complaint/ pneumonitis, infrequently do. Although it's a small probability event, we should n't relax our alert. thus, left ventricular ejection bit should be estimated before taking lapatinib and continue to be tested during the drug to help cardiotoxicity.However, drug should be taken or discontinued under the guidance of a croaker , If the left ventricular ejection bit is abnormal.

Biological activity

Lapatinib( GSK572016, GW2016), used as LapatinibDitosylate, is a potent asset of EGFR and ErbB2 with IC50 of 10.2 and 9.8 nM, independently, in cell-free assays. Lapatinib induces ferroptosis and autophagy.

Target

In vitro studies

With the exception of ErbB- 4, Lapatinib was further than300-fold further picky against EGFR and ErbB- 2 than against other kinases tested, similar as c- Src, MEK and ERK. Lapatinib treatment inhibits EGFR and ErbB- 2 receptor autophosphorylation. This effect is cure-dependent. When acting on BT474 and HN5 cells, the IC50 is 0.17 and 0.08 μM independently. Lapatinib acts on EGFR- and ErbB-2-overexpressing excrescence cells and inhibits EGFR and ErbB- 2 autophosphorylation, which is about 10 times lower effective than purified enzymes. Lapatinib inhibits the growth of cells overexpressing EGFR- and ErbB- 2, while OSI- 774 and Iressa( both EGFR picky impediments) preferentially inhibit the growth of cells overexpressing EGFR. Lapatinib is about 100 times further effective on excrescence cells than on normal fibroblasts. bone epithelial cells HB4ac 5.2 transfected with ErbB- 2 are roughly 40 times more sensitive to Lapatinib than untransfected maternal control cells HB4a. After cultivating the HN5 cell population in a Lapatinib-free medium for about 2 weeks, a brief treatment with 30 μL Lapatinib fully inhibited cell growth. Inhibits growth by 50 at attention> 3.3 μM. Inhibits growth by 20 at a attention of 0.37 μM. Another EGFR- overexpressing cell,A-431, responded also to HN5. Lapatinib is analogous to OSI- 774 in inhibiting the growth of cells overexpressing EGFR.

In vivo studies

Lapatinib effectively inhibits the growth of BT474 and HN5 mortal xenograft excrescences. Orally administered Lapatinib at 30 and 100 mg/ kg doubly daily inhibited excrescence growth in excrescence- bearing mice in a cure-dependent manner. Treatment at a cure of 100mg/ kg fully inhibited excrescence growth. At this cure, there was <10% tumor loss over 21 days of treatment.

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Yihui takes pride in being a trusted Lapatinib API manufacturer and supplier. To acquire this groundbreaking product or discuss your specific requirements, contact us immediately at sales@yihuipharm.com. Rest assured, with Yihui, you're accessing a product of unparalleled quality, backed by certifications that underscore our commitment to excellence in the global market.