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Therapy Name | Apitolisib |
Synonyms | |
Therapy Description |
Apitolisib (GDC-0980) is an inhibitor of both PI3K and mTOR kinases, resulting in decreased phosphorylation of PI3K/Akt/mTOR pathway markers, which may lead to inhibition of tumor growth and tumor regression (PMID: 21998291, PMID: 30914027). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Apitolisib | GDC-0980 | mTOR Inhibitor 51 PI3K Inhibitor (Pan) 42 | Apitolisib (GDC-0980) is an inhibitor of both PI3K and mTOR kinases, resulting in decreased phosphorylation of PI3K/Akt/mTOR pathway markers, which may lead to inhibition of tumor growth and tumor regression (PMID: 21998291, PMID: 30914027). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
PBRM1 inact mut | renal cell carcinoma | no benefit | Apitolisib | Case Reports/Case Series | Actionable | In a retrospective analysis from a Phase II clinical trial, patients with renal cell carcinoma treated with Apitolisib (GDC-0980) had no difference in progression-free survival when stratified by the presence (n=5) or absence (n=17) of deleterious PBRM1 mutations (PMID: 26951309). | 26951309 |
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 E542K | head and neck squamous cell carcinoma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in a partial response in a patient with head and neck squamous cell carcinoma harboring a PIK3CA E542K mutation (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA E545K | head and neck squamous cell carcinoma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in an unconfirmed partial response in a patient with head and neck squamous cell carcinoma harboring PIK3CA E545K (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA E545K | ovarian clear cell carcinoma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in tumor regression by 48.3% in a patient with ovarian clear cell carcinoma harboring PIK3CA E545K, who remained on treatment for 282 days (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA mutant | Advanced Solid Tumor | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in a partial response in 21% (3/14) and stable disease in 64% (9/14) of patients with advanced solid tumors harboring PIK3CA mutations (PMID: 26787751; NCT00854152). | 26787751 |
PIK3CA R88Q | malignant pleural mesothelioma | predicted - sensitive | Apitolisib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Apitolisib (GDC-0980) resulted in a partial response in a patient with malignant pleural mesothelioma harboring PIK3CA R88Q (PMID: 26787751; NCT00854152). | 26787751 |
PTEN mutant | endometrial cancer | sensitive | Apitolisib | Phase II | Actionable | In a Phase II trial, Apitolisib (GDC-0980) was poorly tolerated, but demonstrated efficacy in endometrial cancer patients harboring mutations in PIK3CA, PTEN, or AKT1 (J Clin Oncol 32:5s, 2014 (suppl; abstr 5513)). | detail... |
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 high expression (n=17) and low expression (n=19) of Pten (PMID: 26951309). | 26951309 |
VHL inact mut | 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=5) or absence (n=17) of deleterious VHL mutations (PMID: 26951309). | 26951309 |
PIK3CA mutant | endometrial cancer | sensitive | Apitolisib | Phase II | Actionable | In a Phase II trial, Apitolisib (GDC-0980) was poorly tolerated, but demonstrated efficacy in endometrial cancer patients harboring mutations in PIK3CA, PTEN, or AKT1 (J Clin Oncol 32:5s, 2014 (suppl; abstr 5513)). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT00854152 | Phase I | Apitolisib | A Study Evaluating GDC-0980 Administered Once Daily in Patients With Refractory Solid Tumors or Non-Hodgkin's Lymphoma | Completed | USA | GBR | 0 |
NCT01437566 | Phase II | Apitolisib Fulvestrant Pictilisib | Study of GDC-0941 or GDC-0980 With Fulvestrant Versus Fulvestrant in Advanced or Metastatic Breast Cancer in Patients Resistant to Aromatase Inhibitor Therapy | Completed | USA | NZL | ITA | ISR | GBR | FRA | ESP | DNK | DEU | CAN | BEL | AUS | ARG | 10 |
NCT01485861 | Phase II | Apitolisib Abiraterone Ipatasertib | Study of GDC-0068 Or GDC-0980 With Abiraterone Acetate Versus Abiraterone Acetate in Patients With Castration-Resistant Prostate Cancer Previously Treated With Docetaxel Chemotherapy | Completed | USA | ROU | NLD | ITA | GRC | GBR | FRA | ESP | CZE | 0 |