What are the implications of TAK-285's activity in a brain metastasis model?

Label:chem

Topic
Brain metastases are a significant challenge in cancer treatment due to the blood-brain barrier's (BBB) restriction of drug access. TAK-285's ability to penetrate the BBB and inhibit tumor growth in the CNS is a critical aspect of its potential therapeutic value.
Answer
In a murine intracranial injection model of brain metastasis using BT-474-derived cerebral xenografts, TAK-285 significantly inhibited intracranial tumor growth with a T/C value of 44% on day 41, compared to lapatinib, which showed a T/C value of 73% and was not significantly different from control-treated animals. This suggests that TAK-285 is more effective than lapatinib in treating brain metastases due to its ability to penetrate the BBB and lack of Pgp substrate activity.
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