Sorafenib tosylate

Sorafenib Tosylate (BAY 43-9006 tosylate) is an orally active multikinase inhibitor approved for the treatment of advanced renal cancer, hepatocellular carcinoma, and thyroid cancer. Sorafenib Tosylate works by inhibiting the VEGFR-2/PDGFR-β signaling cascade, thereby blocking tumor angiogenesis. Sorafenib Tosylate also targets Raf-1 and B-RAF (IC₅₀ = 6 and 22 µM, respectively), as well as receptor tyrosine kinases VEGFR2. As an API, Sorafenib Tosylate is manufactured under strict quality controls to ensure consistent therapeutic efficacy. In pharmaceutical quality control, Sorafenib Tosylate reference standards are essential for analytical method development and impurity profiling. The tosylate salt form of Sorafenib Tosylate provides the active pharmaceutical ingredient in the marketed formulation.

Product Parameters

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Parameter	Specification
Product Name	Sorafenib Tosylate
CAS Number	475207-59-1
Molecular Formula	C₂₈H₂₄ClF₃N₄O₆S
Molecular Weight	637.03 g/mol
Melting Point	229–232 °C
Physical Form	Solid
Storage Condition	2–8 °C (protect from light)

Effect

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Sorafenib Tosylate can simultaneously inhibit multiple kinases present both within and on the surface of cells, including RAF kinase, vascular endothelial growth factor receptor-2 (VEGFR-2), vascular endothelial growth factor receptor-3 (VEGFR-3), platelet-derived growth factor receptor-β (PDGFR-β), KIT, and FLT-3. This demonstrates that sorafenib Tosylate exhibits a dual antitumor effect: on one hand, it directly inhibits tumor growth by suppressing the RAF/MEK/ERK signaling pathway; on the other hand, it indirectly suppresses tumor cell proliferation by blocking tumor angiogenesis through inhibition of VEGFR and PDGFR. Sorafenib Tosylate remains the most effective systemic agent currently available for treating advanced hepatocellular carcinoma and is poised to become a new standard therapy for this disease.

 

Pharmacological Action

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Sorafenib Tosylate was initially identified during biochemical analyses conducted to evaluate the structure-activity relationship of c-RAF kinase inhibitor lead compounds. Sorafenib exhibits potent inhibitory effects against both wild-type and mutant forms of c-RAF and b-RAF, suppressing their serine/threonine kinase activities. It also inhibits the tyrosine kinase activities of human VEGFR-2, murine VEGFR-2, VEGFR-3, PDGFR-β, FLT3, and c-KIT. The dual antitumor efficacy of sorafenib is achieved through inhibition of these kinase activities. Daily oral administration of sorafenib demonstrated broad antitumor activity in animal transplantation models of human tumors, including colon cancer, non-small cell carcinoma, breast cancer, melanoma, pancreatic cancer, leukemia, and ovarian cancer, as well as in murine renal cell carcinoma models (RENCA).

 

Treatment of advanced liver cancer

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The incidence rate of liver cancer is approximately 20 per 100,000 people. Due to the lack of obvious early symptoms, nearly 80% of patients are diagnosed at an advanced stage. Half of all liver cancer cases worldwide occur in China, where hepatitis B ranks as the leading cause of liver cancer—a factor that also differs significantly from those observed in European and American countries.

Researchers from multiple countries published a report in the latest issue of the New England Journal of Medicine, reporting that they conducted a study involving 602 patients with advanced hepatocellular carcinoma across countries and regions including the United States, Europe, and Australia.

 

None of these patients had received systematic treatment prior to the study. The results demonstrated that compared with placebo, administration of sorafenib toluenesulfonate (Sorafenib) prolonged overall survival by approximately 44% and delayed disease progression by 73% in patients with advanced or primary hepatocellular carcinoma.

 

One of the principal investigators of this study, Jordi Brux from Barcelona Clinical Hospital in Spain, stated that global liver cancer mortality continues to rise due to the prevalence of hepatitis B and C. The new research findings demonstrate that Sorafenib Tosylate, as a novel therapeutic option for liver cancer, can effectively prolong patient survival, a result described as "encouraging."

 

Sorafenib Tosylate (Tislelizumab) is manufactured by Bayer Healthcare AG in Germany and exerts dual effects on both tumor cells and tumor vasculature. Researchers presented findings at the American Society of Clinical Oncology annual meeting in June last year, demonstrating that a study conducted among patients with advanced hepatocellular carcinoma in the Asia-Pacific region showed Sorafenib could prolong survival by approximately 47%. It remains the only drug proven to significantly extend overall survival in patients with advanced hepatocellular carcinoma.

 

This drug was approved in the United States and Europe respectively last year for the treatment of liver cancer. In August 2009, Bayer Healthcare issued a press release stating that Torotredimab had received approval from the China National Medical Products Administration for the treatment of patients with advanced liver cancer who are not candidates for surgery.

 

Contact Us

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Need a trusted partner for Sorafenib Tosylate supply? Cosperpharm is ready to support your API manufacturing or analytical development program. Contact our team today for a quote.