• Alias: AZD0530
    • An orally available 5-, 7-substituted anilinoquinazoline that is a dual-specific inhibitor of SRC and ABL
    • Specifically inhibits SRC kinase–mediated osteoclast bone resorption
    • Currently under investigation in phase 2 clinical trials for hormone receptor–positive breast cancer, NSCLC, and osteosarcoma in the lung; phase 3 for ovarian cancer
    • Phase 1 studies suggest saracatinib may have therapeutic benefit in metastatic bone disease.
    • Recommended phase 2 dose: 175 mg/d
    • Half-life: â™40 hours
    • Common side effects: Anemia, diarrhea, asthenia
    (Baselga et al., 2010; Hannon et al., 2012)
    Other topics in Targeted and Immunotherapy Agents