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Association details:
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Title:

The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations

Excerpt:
...combining CH5132799 with trastuzumab induced remarkable antitumor activity, resulting in the disappearance of the tumors. Surprisingly, the disappearance was maintained through the follow-up period—more than 1 month—without any additional administration, indicating that CH5132799 overcomes trastuzumab insensitivity in tumors with PIK3CA mutation through PI3K inhibition. Daily oral administration of CH5132799 showed remarkable antitumor activity in the xenograft model of breast cancer KPL-4 cells harboring the PIK3CA H1047R mutation.
DOI:
10.1158/1078-0432.CCR-10-2882