Study of Oral AEE788 in Adults With Advanced Cancer

A Phase I/II, Multicenter, Randomized Dose-Escalation Study of Oral AEE788 on Intermittent Dosing Schedules in Adult Patients With Advanced Cancer (Effective Amendment 5) Previously Entitled A Phase IA, Multicenter, Dose-Escalating Study of Oral AEE788 on a Continuous Daily Dosing Schedule in Adult Patients With Advanced Cancer

AEE788 is an orally active, reversible, small-molecule, multi-targeted kinase inhibitor with potent inhibitory activity against ErbB and VEGF receptor family of tyrosine kinases. It has an IC50 of less than 100 nM against p-EGFR, p-ErbB2, and p-KDR (VEGFR2). This study will assess the safety, pharmacokinetic (PK)/pharmacodynamic (PD) profiles and clinical activity of AEE788 in advanced cancers.

Inclusion Criteria:

• Histologically confirmed solid tumor
• Adequate hematologic, renal and hepatic function
• Age ≥ 18 years
• Karnofsky performance status score ≥ 70%
• Life expectancy ≥ 12 weeks

Exclusion Criteria:

• Active brain metastases
• Peripheral neuropathy > grade 2
• Diarrhea > grade 1
• Gastrointestinal (GI) dysfunction
• Compromised cardiac function
• Concurrent severe and/or uncontrolled medical conditions