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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). |
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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 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 |
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 |
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 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 | 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 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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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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 |