Therapy Detail

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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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Apitolisib GDC-0980 mTOR Inhibitor 51 PI3K Inhibitor (Pan) 40 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).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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...
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 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 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 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
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 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
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
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

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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
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 | NLD | ITA | GBR | FRA | ESP 3
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 | GBR | FRA | ESP | DEU | CAN | BEL | AUS 13


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