EKB-569 is a potent low molecular weight, selective, irreversible inhibitor of the receptor for epidermal growth factor (EGFR), which is developed as an anticancer agent. A Phase 1 dose escalation was conducted in Japanese patients. EKB-569 was administered once a day orally, the 28-day cycles overexpressed in cancer patients with a known advanced EGFR. Two patients with non-small cell cancer of the lung with advanced EGFR mutation and resistance to gefitinib acquired by the Phase 1 study are described in detail. Case 1 is a 63 year old man with history of smoking. He received treatment from March 4, 2004 because he had no serious adverse events, a total of 10 treatment cycles have been completed by December 16 Grade 2 rash and elevation of ALT and grade 1 diarrhea and nail changes. A chest CT, August 4, 2003 revealed multiple pulmonary metastases, which had decreased in size. Case 2 is a 49 year old woman with no history of smoking. She received treatment on February 9, 2004. She received a total of five therapy classes until June 22, 2004 State 3 nausea and vomiting and grade 1 diarrhea and dry skin develops. A chest CT, March 3 revealed multiple pulmonary metastases, which had decreased in size. An MRI of the brain, March 4 showed multiple brain metastases were also reduced in size. Based on RECIST, they had stable disease, but the radiographic tumor regression was observed.
