A phase I study of GW572016 in patients with solid tumors

Role of lapatinib in the first-line treatment of patients with metastatic breast cancer

“…Pharmacokinetic (PK) studies reveal peak serum lapatinib concentrations 3 to 6 hours after dosing. [4][5][6][7] Serum concentrations increase with increased dose, although variability is high. Lapatinib displays a time dependent increase in systemic exposure with repeated dosing, with serum concentrations accumulating approximately 2-fold with daily administration.…”

“…In phase I and II studies, lapatinib monotherapy was associated with transient grade 1-2 rash, diarrhea, nausea/vomiting, stomatitis, fatigue and anorexia reported as the most frequent adverse events (AE). [4][5][6][7]13,15,16 Grade 3 toxicities were uncommon, but included diarrhea, rash, abnormal liver function and gastrointestinal events. [5][6][7] No grade 4 toxicity attributable to lapatinib was reported.…”

“…[4][5][6][7]13,15,16 Grade 3 toxicities were uncommon, but included diarrhea, rash, abnormal liver function and gastrointestinal events. [5][6][7] No grade 4 toxicity attributable to lapatinib was reported. [5][6][7]13,16 No drug-related cardiac toxicity was observed.…”

“…Phase I and II studies reveal good tolerance and preliminary single agent clinical activity for lapatinib monotherapy despite multiple lines of prior chemotherapy and trastuzumab, indicating lapatinib activity beyond failure of standard therapies. [5][6][7]15 In a pivotal phase III study in MBC assessing capecitabine with or without lapatinib in trastuzumab pre-treated patients, an interim analysis of time to progression (TTP) showing superiority of the combination and lack of safety concerns led to early reporting. 11 Longer median TTP was seen for capecitabine and lapatinib versus capecitabine alone …”

Epidermal growth factor receptor‐targeted treatment for advanced colorectal carcinoma

“…Lapatinib also has been evaluated in Japanese patients (six patients) with evidence of activity that warranted a Phase II study. 98 Uniformly, monotherapy has been tolerated well. Combination therapies that have shown activity in a variety of solid tumors, including CRC, are lapatinib plus FOLFOX4, 99 lapatinib plus paclitaxel, 100 and lapatinib plus capecitabine.…”