Tipifarnib is an oral, investigational drug candidate we are evaluating in patients with certain head and neck cancers that carry HRAS mutations.
HRAS is a proto-oncogene, which is a normal gene that can become an oncogene due to mutations or increased expression. Proto-oncogenes code for proteins that help to regulate cell growth and differentiation and HRAS is mutated and/or expressed in certain head and neck squamous cell carcinoma (HNSCC) tumors.
Although HRAS was discovered more than 40 years ago, no specific therapies have been developed that target tumors with the mutated form of the protein. Tipifarnib is a potent and highly selective inhibitor of farnesyltransferase, a critical enzyme for the activity of HRAS.
The relapsed and/or refractory HNSCC patient population has an overall survival of approximately six to eight months and existing therapeutic options, including new therapies such as immune therapy, typically show a response rate in the range of 10-20 percent.
Encouraging clinical activity of tipifarnib has been observed in patients with HRAS mutant head and neck squamous cell carcinoma (HNSCC) tumors. We are conducting a Phase 2 clinical trial to evaluate the safety and activity of tipifarnib in patients with relapsed and/or refractory HRAS mutant HNSCC.