Molecular Profile Detail

Profile Name PTEN inact mut
Gene Variant Detail

PTEN inact mut (loss of function)

Relevant Treatment Approaches Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor PI3K Inhibitor (Pan) PIK3CB inhibitor

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
PTEN inact mut estrogen-receptor positive breast cancer sensitive PI3K Inhibitor (Pan) Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a PTEN deficient estrogen-receptor (ER) positive breast cancer cell line demonstrated increased sensitivity to treatment in culture when Pictilisib (GDC-0941) was given at a higher dose for a shorter duration, resulting in inhibition of cell growth (PMID: 26733612). 26733612
PTEN inact mut estrogen-receptor positive breast cancer sensitive PI3K Inhibitor (Pan) Fulvestrant + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, the combination of Faslodex (fulvestrant) and PIctilisib (GDC-0941) resulted in decreased cell viability and increased apoptotic activity in PTEN deficient estrogen-receptor (ER) positive breast cancer cells in culture (PMID: 26733612). 26733612
PTEN inact mut prostate adenocarcinoma sensitive PI3K Inhibitor (Pan) XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited PI3K signaling, growth, and migration of a human prostate adenocarcinoma cell line harboring a PTEN inactivating mutation in culture, and inhibited tumor growth and vascularization in xenograft models (PMID: 25637314). 25637314
PTEN inact mut glioblastoma multiforme sensitive PI3K Inhibitor (Pan) SAR245409 Preclinical - Cell line xenograft Actionable In a preclinical study, a glioblastoma cell line harboring a PTEN inactivating mutation was sensitive to XL765 (SAR245409), demonstrating inhibition of cell proliferation in culture, and inhibition of tumor growth in cell line xenograft models (PMID: 24634413). 24634413
PTEN inact mut Advanced Solid Tumor sensitive Akt Inhibitor (Pan) Capivasertib Preclinical - Cell culture Actionable In a preclinical study, AZD5363 inhibited growth of various solid tumor cell culture models with inactivating Pten mutations (PMID: 22294718). 22294718
PTEN inact mut kidney cancer sensitive PI3K Inhibitor (Pan) LY3023414 Preclinical - Cell line xenograft Actionable In a preclinical study, LY3023414 inhibited proliferation of renal cancer cells harboring PTEN inactivating mutation in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 27439478). 27439478
PTEN inact mut prostate adenocarcinoma sensitive PI3K Inhibitor (Pan) XL147 + Paclitaxel Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of XL147 and Taxol (paclitaxel) inhibited tumor growth and angiogenesis in xenograft models of a human prostate adenocarcinoma cell line harboring an inactivating mutation in PTEN, with increased efficacy compared to either agent alone (PMID: 25637314). 25637314
PTEN inact mut glioblastoma multiforme sensitive PI3K Inhibitor (Pan) SF1126 Preclinical - Cell line xenograft Actionable In a preclinical study, a glioblastoma cell line harboring a PTEN inactivating mutation (PMID: 24634413) was sensitive to SF1126, demonstrating inhibition of tumor growth in cell line xenograft models (PMID: 18172313). 18172313 24634413
Clinical Trial Phase Therapies Title Recruitment Status
NCT02920450 Phase Ib/II Gedatolisib + Paclitaxel + Carboplatin Study of Paclitaxel, Carboplatin, and PF-05212384 in Advanced or Metastatic NSCLC Active, not recruiting
NCT03209401 Phase I Carboplatin + Niraparib Niraparib Plus Carboplatin in Patients With Homologous Recombination Deficient Advanced Solid Tumor Malignancies Recruiting
NCT01884285 Phase I AZD8186 AZD8186 First Time In Patient Ascending Dose Study Recruiting
NCT02189174 Phase Ib/II CLR457 Study of CLR457 Administered Orally in Adult Patients With Advanced Solid Malignancies Terminated
NCT03218826 Phase I AZD8186 + Docetaxel PI3Kbeta Inhibitor AZD8186 and Docetaxel in Treating Patients Advanced Solid Tumors With PTEN or PIK3CB Mutations That Are Metastatic or Cannot Be Removed by Surgery Recruiting
NCT03317119 Phase I Trametinib + trifluridine/tipiracil hydrochloride Trametinib and TAS-102 in Treating Patients With Colon or Rectal Cancer That is Advanced, Metastatic, or Cannot Be Removed by Surgery Recruiting