- Male and female patients (18 years old and above), with a histologically proven,
measurable, locally recurrent, and/or metastatic head and neck tumor.
- > 4 weeks since major surgery
- > 4 weeks since prior chemotherapy
- > 3 weeks since prior therapy with biological agents (Interleukin-2 [IL-2],
interferon, other molecular-targeted therapies [except Ras/Raf inhibitors]).
- Performance status < 2
- Life expectancy > 3 months.
- At least one uni-dimensional measurable lesion by computed tomography (CT)-scan or
magnetic resonance imaging (MRI) according to Response Evaluation Criteria in Solid
- Adequate liver, pancreatic, renal, and coagulation function
- A slide or paraffin-block from a tumor biopsy MUST be available at the time of
screening. If the original diagnostic biopsy is not available at the time of
screening, an additional biopsy is required.
- Severe preexisting conditions
- Evidence of bone marrow suppression
- Frequent vomiting or medical condition, which could interfere with oral medication
- Lack of resolution of all toxic manifestations of prior chemotherapy, biologic, or
radiation therapy (alopecia excluded).
- Known HIV positivity or AIDS-related illness.
- Previous exposure to a Ras/Raf inhibitor
- Previous malignancy (except for cervical carcinoma in situ, adequately treated basal
cell carcinoma, or superficial bladder tumors [Ta, Tis and T1] or other malignancies
curatively treated > 2 years prior to entry)
- Congestive heart failure
- Cardiac arrhythmias requiring anti-arrhythmics
- Active coronary artery disease or ischaemia
- Active clinically serious bacterial or fungal infections
- Known brain or meningeal metastases
- Patients with seizure disorder requiring medication (such as anti-epileptics)
- Substance abuse, medical, psychological, or social conditions that may interfere with
the patient’s participation in the study or evaluation of the study results
- Known or suspected allergy to the investigational agent or any agent given in
association with this trial
- Pregnant or breast-feeding patients. Women of childbearing potential must have a
negative pregnancy test.
- Concurrent anti-cancer chemotherapy or immunotherapy is excluded
- Significant surgery within four weeks prior to start of study drug
- Investigational drug therapy outside of this trial, or any chemotherapy during or
within 4 weeks prior to start of study drug
- Myelosuppressive radiotherapy within four weeks prior to start of study drug
(short-course non-myelosuppressive radiotherapy may be allowed based on approval of
- Concomitant treatment with ketoconazole, itraconazole, ritonavir, or use of