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Therapy Name GSK2636771
Synonyms
Therapy Description

GSK2636771 is a selective inhibitor of PIK3CB, which potentially increases apoptosis and decreases growth in tumors expressing PI3K beta (PMID: 28645941, PMID: 31371342).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
GSK2636771 GSK-2636771|GSK 2636771 PIK3CB inhibitor 8 GSK2636771 is a selective inhibitor of PIK3CB, which potentially increases apoptosis and decreases growth in tumors expressing PI3K beta (PMID: 28645941, PMID: 31371342).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PTEN dec exp Advanced Solid Tumor sensitive GSK2636771 Phase Ib/II Actionable In a Phase I/II trial, GSK2636771 treatment inhibited Akt signaling, and resulted in partial response in 2% (1/53) and stable disease in 25% (13/53) of patients with PTEN-deficient advanced solid tumors (J Clin Oncol 32:5s, 2014 (suppl; abstr 2514)). detail...
PTEN loss prostate cancer sensitive GSK2636771 Preclinical Actionable In a preclinical study, GSK2636771 inhibited viability of prostate cancer cell lines harboring PTEN deficiency in culture (PMID: 23674493). 23674493
PTEN L152P PTEN neg salivary gland carcinoma resistant GSK2636771 Preclinical - Cell culture Actionable In a preclinical study, salivary ductal carcinoma cells harboring PTEN L152P and loss of Pten protein expression were resistant to GSK2636771-induced inhibition of proliferation in culture (PMID: 30289966). 30289966
PTEN del Advanced Solid Tumor no benefit GSK2636771 Phase I Actionable In a Phase I trial, patients with advanced solid tumors deficient in PTEN lacked benefit from GSK2636771 (PMID: 26117819). 26117819
PTEN loss melanoma sensitive GSK2636771 Preclinical Actionable In a preclinical study, human melanoma cells with PTEN loss were sensitive to GSK2636771, resulting in decreased activation of Akt and some inhibition of tumor growth (PMID: 26645196). 26645196
BRAF mut PTEN loss melanoma no benefit GSK2636771 Preclinical Actionable In a preclinical study, GSK2636771 resulted in no benefit in a melanoma mouse model co-harboring a BRAF mutation and PTEN loss (PMID: 26645196). 26645196
PTEN mutant endometrial cancer resistant GSK2636771 Preclinical Actionable In a preclinical study, endometrioid endometrial cancer cell lines harboring PTEN mutations demonstrated resistance to GSK2636771 induced growth inhibition in culture (PMID: 23674493). 23674493
PTEN loss breast cancer sensitive GSK2636771 Preclinical Actionable In a preclinical study, GSK2636771 inhibited viability of breast cancer cell lines harboring PTEN deficiency in culture (PMID: 23674493). 23674493

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01458067 Phase I GSK2636771 A Phase I/IIa, First Time in Human, Study of GSK2636771 in Subjects With Advanced Solid Tumors With Phosphatase and Tensin Homolog (PTEN) Deficiency Completed USA | GBR 1
NCT02215096 Phase I Enzalutamide GSK2636771 Dose-finding Study of GSK2636771 When Administered in Combination With Enzalutamide in Male Subjects With Metastatic Castration-Resistant Prostate Cancer Completed USA | GBR 0


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