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Profile Name | PIK3CA act mut |
Gene Variant Detail | |
Relevant Treatment Approaches | Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
ARID1A mut PIK3CA act mut | ovarian cancer | sensitive | GSK126 | Preclinical - Cell culture | Actionable | In a preclinical study, expression of a constitutively active PIK3CA mutation in ARID1A-mutant ovarian cancer cell lines enhanced growth inhibition by GSK126 in culture (PMID: 25686104). | 25686104 |
PIK3CA act mut PTEN dec exp | renal cell carcinoma | no benefit | Apitolisib | Case Reports/Case Series | Actionable | In a retrospective analysis from a Phase II clinical trial, patients with metastatic renal cell carcinoma treated with Apitolisib (GDC-0980) had no difference in progression-free survival when stratified by the presence (n=21) or absence (n=15) of PIK3CA activating mutation and/or decreased Pten expression (PMID: 26951309). | 26951309 |
PIK3CA act mut PTEN dec exp | renal cell carcinoma | no benefit | Everolimus | Case Reports/Case Series | Actionable | In a retrospective analysis from a Phase II clinical trial, patients with metastatic renal cell carcinoma treated with Afinitor (everolimus) had no difference in progression-free survival when stratified by the presence (n=21) or absence (n=17) of PIK3CA activating mutations (PMID: 26951309). | 26951309 |
PIK3CA act mut PTEN wild-type | breast cancer | sensitive | Everolimus | Preclinical - Cell culture | Actionable | In a preclinical study, 8/9 breast cancer cell lines harboring a PIK3CA activating mutation and PTEN wild-type demonstrated sensitivity to treatment with Afinitor (everolimus) in culture, resulting in decreased cell viability (PMID: 21358673). | 21358673 |
PIK3CA act mut PTEN wild-type | breast cancer | sensitive | Torkinib | Preclinical - Cell culture | Actionable | In a preclinical study, 9/9 breast cancer cell lines harboring a PIK3CA activating mutation and PTEN wild-type demonstrated sensitivity to treatment with Torkinib (PP242) in culture, resulting in decreased cell viability (PMID: 21358673). | 21358673 |
CDKN2A loss PIK3CA act mut | lung squamous cell carcinoma | predicted - 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 patient-derived xenograft (PDX) models of lung squamous cell carcinoma harboring PIK3CA E542K or E545K mutations with p16 (CDKN2A) loss, including models that also had either PIK3CA amplification or PTEN loss (PMID: 30093452). | 30093452 |