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PIK3CA

Also known as PI3K catalytic subunit alpha

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Tumour types

breast cancer

PIK3CA encodes the catalytic alpha subunit of PI3K, a central node in the PI3K/AKT/mTOR signaling pathway.

Hotspot activating mutations cluster in the helical domain (E542K, E545K) and the kinase domain (H1047R).

Clinical significance

  • PIK3CA mutation status is used to select patients with hormone receptor-positive, HER2-negative advanced breast cancer for PI3K-inhibitor-containing therapy.

    fda — FDA-approved product labeling for PI3K inhibitors

FDA-approved treatments

  • Piqray (alpelisib) — PIK3CA-mutated, hormone receptor-positive, HER2-negative advanced or metastatic breast cancer, in combination with fulvestrant [fda]
  • Itovebi (inavolisib) — PIK3CA-mutated, hormone receptor-positive, HER2-negative advanced or metastatic breast cancer, in combination with palbociclib and fulvestrant [fda]

Prevalence

PIK3CA hotspot mutations are found in approximately 40% of hormone receptor-positive, HER2-negative advanced breast cancers. [fda]

Tests / detection method

NGS, PCR-based mutation assays

Therapeutic pipeline

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