- 型号:
- 医药级
- 规格:
- 25kg/桶
Chinese synonyms:---:r >
Everolimus
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--(-)--(-)- (r )
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Heterocyclic signal transduction pathway kinase inhibitors APIs APIs intermediates microbial metabolites pharmaceutical intermediates Everolimus
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Properties of everolimus
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Uses and synthesis methods of everolimus
Sirolimus derivatives ---:r >
Everolimus is a derivative of sirolimus, also known as --(-hydroxyethyl)-rapamycin or --(-hydroxyethyl)-sirolimus, which interferes with cell communication and prevents The kinase drug for tumor cell growth is an oral mammalian rapamycin (r) inhibitor. In the past, it was mainly used clinically to prevent rejection after kidney transplantation and heart transplantation. It can also be used to treat patients with advanced renal cancer who have already used two vascular endothelial growth factor receptor kinase inhibitors: sunitinib (Pfizer Pharmaceuticals) and sorafenib (Bayer Pharmaceuticals), and the side effects are mild.
Sunitinib and sorafenib are multiple kinase inhibitors (acting on multiple cellular targets) while everolimus blocks the mammalian target of rapamycin (r) specifically. The protein interferes with the growth, differentiation and metabolism of cancer cells. This r pathway is dysregulated in some human tumors. Everolimus binds to intracellular proteins to form inhibitory complexes, thereby inhibiting r-kinase activity and reducing the activity of r's downstream effectors, ribosomal protein kinase and eukaryotic elongation factor-binding protein (-). In addition, everolimus inhibits the expression of hypoxia-inducible factors (such as -) and reduces the expression of vascular endothelial growth factor. In vivo and in vitro studies have shown that it can reduce cell proliferation, angiogenesis and glucose uptake.
Remarks:
r is a downstream product of serine-threonine kinase/.
Sirolimus is also called rapamycin.
Target of rapamycin ---:r >
Activation of target of rapamycin (r) will promote the proliferation and survival of tumor cells and also cause vasculogenesis in endothelial cells. Pathway signaling. The product of rapamycin binding to intracellular proteins - () the resulting protein-drug complex can inhibit the activity of r-kinase. Rapamycin also has immunosuppressive, antifungal, antiviral, vascular protection, anti-tumor activity, etc. However, its main application is based on its immunosuppressive effect. In 2008, it was approved by the United States for anti-rejection treatment of organ transplantation. . Many derivatives of rapamycin have been synthesized primarily with the aim of improving its pharmaceutical properties. These efforts have also led to the intravenous use of rapamycin (r) for the treatment of renal cancer and the oral use of everolimus (r). Discovery and research. Everolimus was approved in Europe for the treatment of post-organ transplant rejection and marketed under the trade name Everolimus.
Treatment of advanced kidney cancer---:r >
Kidney cancer accounts for ~% of cancers. In the early stage of kidney cancer, surgery is the main treatment, and in the late stage, chemotherapy is the main treatment. The response to chemotherapy and radiotherapy is often poor. In fact, it is used alone. Interleukin or combined alpha interferon-related immunotherapy has limited clinical use due to its toxicity and generally poor therapeutic response.
Renal cell carcinoma is the most common type of kidney cancer and occurs in renal tubular epithelial cells. Often the cancer cells in these patients become resistant to standard treatments such as radiation and chemotherapy, leading most to have their kidneys removed. If the patient's cancerous site is limited to the kidney - % of people will survive for years. But once the cancer cells metastasize, the patient's survival will be significantly reduced.
Novartis’ original immunosuppressive drug everolimus (r) was approved by the U.S. D for renal cancer on 2019-01-08. The study results show that everolimus can significantly increase the progression-free survival of cancer patients. Everolimus provides a new treatment option for patients with advanced renal cell carcinoma who have failed to respond to sunitinib or sorafenib treatment.
The European Commission has approved Novartis's (everolimus) tablets for the treatment of patients with advanced renal cell carcinoma (R). European Society of Medical Oncology, European Society of Urology, Spanish Genitourinary Oncology Group, European Cancer Several authoritative treatment guidelines in Europe, including the Research and Treatment Organization (R), the European Society of Medical Oncology's treatment guidelines, and the British Consensus Guidelines, have been updated and recommended as a second-line treatment for patients with advanced kidney cancer.
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