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Profile Name PIK3CA E542K
Gene Variant Detail

PIK3CA E542K (gain of function)

Relevant Treatment Approaches Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA E542K PTEN loss breast cancer predicted - sensitive Dactolisib + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA E542K and PTEN loss to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA E542K PTEN loss stomach cancer unknown Sirolimus Phase 0 Actionable In a pilot clinical trial, Rapamune (sirolimus) demonstrated modest clinical activity in patients with PIK3CA-mutant gastric cancer (n=3) or hilar cholangiocarcinoma (n=1), including a gastric cancer patient harboring PIK3CA E542K and PTEN loss, with a 0% response rate, median progression-free survival of 1.9 months, and median overall survival of 3.6 months (PMID: 28685070). 28685070
PIK3CA E542K PIK3CA amp lung squamous cell carcinoma sensitive Buparlisib Preclinical - Pdx Actionable In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PIK3CA amplification (PMID: 30093452). 30093452
PIK3CA E542K PIK3CA amp lung squamous cell carcinoma sensitive Alpelisib Preclinical - Pdx Actionable In a preclinical study, Alpelisib (BYL719) treatment resulted in response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PIK3CA amplification (PMID: 30093452). 30093452
PIK3CA E542K PTEN loss lung squamous cell carcinoma sensitive Alpelisib Preclinical - Pdx Actionable In a preclinical study, Alpelisib (BYL719) treatment resulted in response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PTEN loss (PMID: 30093452). 30093452
CDKN2A loss PIK3CA E542K PTEN loss lung squamous cell carcinoma sensitive Buparlisib + Palbociclib Preclinical - Pdx Actionable In a preclinical study, treatment with the combination of Buparlisib (BYL719) and Ibrance (palbociclib) resulted in increased tumor growth inhibition compared to either agent alone in a patient-derived xenograft (PDX) model of lung squamous cell carcinoma harboring PIK3CA E542K and PTEN loss, with p16 (CDKN2A) loss (PMID: 30093452). 30093452
CDKN2A loss PIK3CA E542K PIK3CA amp lung squamous cell carcinoma sensitive Buparlisib + Palbociclib Preclinical - Pdx Actionable In a preclinical study, treatment with the combination of Buparlisib (BYL719) and Ibrance (palbociclib) resulted in increased tumor growth inhibition compared to either agent alone in a patient-derived xenograft (PDX) model of lung squamous cell carcinoma harboring PIK3CA E542K and PIK3CA amplification, with p16 (CDKN2A) loss (PMID: 30093452). 30093452
PIK3CA E542K PTEN loss breast cancer predicted - sensitive CYH33 Preclinical - Cell culture Actionable In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA E542K and PTEN loss in culture (PMID: 30003928). 30003928
HRAS mut PIK3CA E542K high grade glioma sensitive Buparlisib + Selumetinib Preclinical - Cell culture Actionable In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in growth inhibition of astrocytoma cells with an HRAS mutation expressing PIK3CA E542K in culture, but at a higher drug concentration compared to cells without mutant HRAS (PMID: 29975751). 29975751
PIK3CA E542K PIK3CA F744L head and neck squamous cell carcinoma sensitive Sulindac Preclinical - Pdx Actionable In a preclinical study, Clinoril (sulindac) treatment reduced tumor growth rate in patient-derived xenograft (PDX) models of head and neck squamous cell carcinoma harboring PIK3CA mutations, including a model harboring PIK3CA E542K and PIK3CA F744L (PMID: 30683736). 30683736
PIK3CA E542K PTEN loss breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA E542K was sensitive to treatment with Taselisib (GDC-0032) in culture, demonstrating decreased cell viability (PMID: 31534012). 31534012
PIK3CA E542K PTEN loss lung squamous cell carcinoma sensitive Buparlisib Preclinical - Pdx Actionable In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PTEN loss (PMID: 30093452). 30093452
PIK3CA E542K PIK3CA E674Q urinary bladder cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 increased apoptosis and inhibited viability in a bladder cancer cell line harboring PIK3CA E542K and E674Q in culture (PMID: 25349966). 25349966
PIK3CA E542K PIK3CA H1065L breast cancer sensitive STX-478 Preclinical - Pdx Actionable In a preclinical study, STX-478 inhibited tumor growth of a breast cancer patient-derived xenograft (PDX) model harboring PIK3CA E542K and H1065L (PMID: 37623743). 37623743
BRAF V600E PIK3CA E542K thyroid gland anaplastic carcinoma resistant Dasatinib + Trametinib Preclinical - Cell culture Actionable In a preclinical study, an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K was resistant to the combination of Sprycel (dasatinib) and Mekinist (trametinib) in culture (PMID: 37713162). 37713162
BRAF V600E PIK3CA E542K thyroid gland anaplastic carcinoma sensitive GSK2334470 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the addition of GSK2334470 sensitized an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K to Mekinist (trametinib) treatment as demonstrated by a reduction in viability in culture (PMID: 37713162). 37713162
BRAF V600E PIK3CA W11C PIK3CA E542K thyroid gland papillary carcinoma sensitive Dasatinib + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of a papillary thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K and W11C in culture (PMID: 37713162). 37713162
BRAF V600E PIK3CA E542K thyroid gland anaplastic carcinoma resistant Dasatinib + MK2206 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the addition of MK2206 did not sensitize an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542k to Sprycel (dasatinib) and Mekinist (trametinib) combination treatment in culture (PMID: 37713162). 37713162