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Updated: Jul 19, 2026

An Oncogenic Hepatocyte-Induced Orthotopic Mouse Model of Hepatocellular Cancer Arising in the Setting of Hepatic Inflammation and Fibrosis
Published on: September 12, 2019
Discovery and development of sorafenib: a multikinase inhibitor for treating cancer
Scott Wilhelm1, Christopher Carter, Mark Lynch
1Department of Cancer Research, Bayer Pharmaceuticals Corp., West Haven, Connecticut 06516, USA. scott.wilhelm.b@bayer.com
Abstract:
Since the molecular revolution of the 1980s, knowledge of the aetiology of cancer has increased considerably, which has led to the discovery and development of targeted therapies tailored to inhibit cancer-specific pathways. The introduction and refinement of rapid, high-throughput screening technologies over the past decade has greatly facilitated this targeted discovery and development process. Here, we describe the discovery and continuing development of sorafenib (previously known as BAY 43-9006), the first oral multikinase inhibitor that targets Raf and affects tumour signalling and the tumour vasculature. The discovery cycle of sorafenib (Nexavar; Bayer Pharmaceuticals) - from initial screening for a lead compound to FDA approval for the treatment of advanced renal cell carcinoma in December 2005 - was completed in just 11 years, with approval being received approximately 5 years after the initiation of the first Phase I trial.
Insights
Sorafenib, an oral multikinase inhibitor, targets cancer pathways and vasculature. Its rapid development cycle highlights advancements in targeted cancer therapy discovery and drug approval processes.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Cancer aetiology knowledge has grown significantly since the 1980s molecular revolution.
- Targeted therapies inhibiting cancer-specific pathways have been developed.
- High-throughput screening technologies accelerate drug discovery and development.
Purpose of the Study:
- To describe the discovery and development of sorafenib (BAY 43-9006).
- To highlight sorafenib as the first oral multikinase inhibitor targeting Raf.
- To detail the drug's impact on tumor signaling and vasculature.
Main Methods:
- Initial screening for a lead compound.
- Utilizing rapid, high-throughput screening technologies.
- Clinical trials including Phase I, leading to regulatory approval.
Main Results:
- Sorafenib identified as an oral multikinase inhibitor targeting Raf.
- Demonstrated effects on tumor signaling and vasculature.
- Achieved FDA approval for advanced renal cell carcinoma in 11 years.
Conclusions:
- Sorafenib represents a successful targeted therapy developed through advanced screening.
- The drug's expedited development showcases efficient drug discovery and approval pipelines.
- Sorafenib offers a new treatment option for advanced renal cell carcinoma.
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