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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 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 del Advanced Solid Tumor no benefit GSK2636771 Case Reports/Case Series Actionable In a Phase I trial, patients with advanced solid tumors deficient in PTEN lacked benefit from GSK2636771 (PMID: 26117819). 26117819
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
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
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 negative Advanced Solid Tumor no benefit GSK2636771 Phase II Actionable In a Phase II trial (MATCH), GSK2636771 treatment did not meet the primary endpoint of objective response in patients with advanced solid tumors with PTEN protein loss (n=35), resulting in stable disease in 22% (7/35) of the patients, a median progression-free survival of 1.8 months, and a median overall survival of 5.9 months (PMID: 40865033; NCT02465060). 40865033
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 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 mutant Advanced Solid Tumor no benefit GSK2636771 Phase II Actionable In a Phase II trial (MATCH), GSK2636771 treatment did not meet the primary endpoint of objective response in patients with advanced solid tumors harboring PTEN mutation or deletion but retained protein expression, resulting in stable disease in 32% (7/24) of the patients, a median progression-free survival of 1.8 months, and a median overall survival of 7.5 months (PMID: 40865033; NCT02465060). 40865033
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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02465060 Phase II Erdafitinib Trametinib Crizotinib Sapanisertib Fexagratinib Dasatinib Osimertinib Palbociclib Capivasertib Larotrectinib Ulixertinib Nivolumab + Relatlimab Copanlisib Sunitinib Nivolumab Pertuzumab + Trastuzumab Ipatasertib Dabrafenib + Trametinib Binimetinib Adavosertib Afatinib Defactinib GSK2636771 Vismodegib Ado-trastuzumab emtansine Taselisib Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) Active, not recruiting USA 2
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
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


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