|Product Name:||Sorafenib tosylate|
|Synonyms:||SORAFENIB TOSYLATE;Sorafenib & its intermediates;Sorafinib mesylate;4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide monomethanesulfonate;Sorafenib Tosylate(Bay 43-9006,Nexavar);2-PyridinecarboxaMide, 4-[4-[[[[4-chloro-3-(trifluoroMethyl)phenyl]aMino]carbonyl]aMino]phenoxy]-N-Methyl-, 4-Methylbenzenesulfonate;Sorafenib Tosylate (Nexavar);Sorafenib (Nexavar)|
|Product Categories:||Bay 43-9006;Inhibitors|
|Mol File:||Mol File|
|Sorafenib tosylate Chemical Properties|
|Sorafenib tosylate Usage And Synthesis|
|New multi-targeted anticancer drugs||Toluenesulfonic Sorafenib is a kind of novel multi-targeted anticancer drug and was first successfully developed by the German pharmaceutical company Bayer. It can simultaneously take effect on both the tumor cell and tumor vasculature. It has a dual anti-tumor effect: not only by blocking the RAF/MEK/ERK-mediated cell signaling pathway for direct inhibition of tumor cell proliferation, but also by inhibiting VEGF and platelet-derived growth factor (PDGF) receptor for blocking tumor angiogenesis and indirectly inhibition of the growth of tumor cells. |
It has shown a wide range of anti-tumor activity in preclinical animal studies. In phase III randomized clinical studies for treating patients with advanced kidney cancer in Europe and the United States, 903 cases of patients who had gotten failure upon receiving a systemic therapy (chemotherapy or immune) before for advanced kidney cancer randomly divided into two groups, one group received treatment of toluenesulfonic Sorafenib (referred Sorafenib), the other group received a placebo. 222 cases of deaths have occurred upon the interim analysis with the results showing that the objective effectiveness rate of two groups was 10% and 2%, respectively, and with 74% and 53% of patients, respectively, having their tumor remained stable.
The progression-free survival period of sorafenib group is 2-fold as high as the placebo group (5.8 months vs 2.8 months with hazard ratio being 0.51). Compared with placebo treatment, the sorafenib has significantly improved the quality of life of patients. Sorafenib group facilitated a longer survival period than the placebo group with the risk ratio being 0.72, but this difference did not reach statistical significance. Owing to that this was only the result of the interim analysis; therefore, it is necessary to perform the final comparison analysis upon the final analysis of the test.
Sorafenib treatment has well tolerance with the main adverse effects including controllable diarrhea, rash, fatigue, hand-foot syndrome, hypertension, hair loss, nausea/vomiting and loss of appetite.
In December 2005, the US Food and Drug Administration (FDA) approved it for entering into market as a kind of first-line drugs for treatment of advanced kidney cancer.
In October 2007, the European Medicines Evaluation Agency (EMEA) has approved sorafenib (Nexavar) for the treatment of hepatocellular carcinoma.
In November 2007, the US Food and Drug Administration approved Nexavar for the treatment of unresectable hepatocellular carcinoma.
In August 2009, the Chinese State Food and Drug Administration has approved the toluenesulfonic sorafenib tablet (trade name: Nexavar) developed by the German pharmaceutical company Bayer to officially entered into the Chinese market for liver cancer therapy in order to treat the patients with inoperable advanced liver cancer.
|Advanced liver cancer treatment||The incidence of liver cancer is approximately twenty over one hundred thousand. Owing to insignificance of the early symptoms of early liver cancer, there are already nearly 80% of patents existing at their advanced stage upon seek medication. There are around half of the cases of the world's liver cancer occurring in China while among all the primary factors in China causing liver cancer, hepatitis B is in the first row. This causative factor of liver cancer in China is also quite different from that in Europe and the United States. |
Researchers from several countries have published reports on the new American "New England Journal of Medicine," in which they selected 602 patients with advanced liver cancer from the United States, Europe and Australia and other countries and performed related studies. None of these patients had ever received systemic therapy. The results have showed that compared with placebo, taking toluenesulfonic sorafenib (Nexavar) could prolong the overall survival period of patients with advanced hepatocellular carcinoma or primary liver cancer by about 44% and delay the disease progression time by 73%.
One of the major researcher in charge of the study, the Jordi• Bruning Fox from Clinical Hospital of Barcelona, Spain have said that“because of the prevalence of hepatitis B and hepatitis C, the worldwide death toll of liver cancer is still rising. The new study has showed that Nexavar, as a new option for treating liver cancer, can play the role of prolonging survival period of the patients. This result is "encouraging."
Nexavar is produced by Bayer HealthCare, which can simultaneously take effect on the tumor cell and tumor vasculature. In June of the last year, related researchers has introduced about it in the annual meeting of the American Society of Clinical Oncology. They said that they had selected patients with advanced liver cancer in Asia and the Pacific area for study and had found that Nexavar can prolong the survival period of these patients by about 47%. It is also the only one available drug which had been demonstrated being able to significantly prolong overall survival period in patients with advanced liver cancer drugs.
The drug has been separately approved in the United States and Europe last year for the treatment of liver cancer. In August 2009, the Bayer HealthCare has released a press and said, Nexavar has been approved by China's State Food and Drug Administration for the treatment of patients with inoperable advanced liver cancer.
The above information is edited by the chemicalbook of Dai Xiongfeng.
|Application||It is used for the treatment of advanced liver cancer.
|Usage||Sorafenib Tosylate (Bay 43-9006, Nexavar) is a small molecular inhibitor of VEGFR, PDGFR, c-Raf and B-Raf with IC50s of 18 nM, 10 nM, 3 nM and 15 nM, respectively.|
|Usage||Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively|
|Sorafenib tosylate Preparation Products And Raw materials|