In metastatic colorectal cancer: lomeguatrib (40 mg) is given together with temozolomide (50-200 mg m(-2)) orally for 5 consecutive days every 4 weeks. Advanced melanoma: lomeguatrib is given at dose of 40 mg, b.i.d. for 10 or 14 days and temozolomide 75-100 mg m(-2) on days 1-5. Drugs are administered orally with cycles repeated every 28 days, for up to six cycles. Advanced solid tumors: lomeguatrib is administered at dose levels of 10 to 40 mg/m2 (orally or intravenously) days 1 to 5, as a single agent, and also in combination with temozolomide.

Anaplastic astrocytoma cell lines were treated with a temozolomide-lomeguatrib combination at concentration of 50 uM.