Therapy Detail

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Therapy Name Taselisib
Synonyms
Therapy Description

Taselisib (GDC-0032) is a beta isoform-sparing PI3K inhibitor, with greater activity against oncogenic mutants of PIK3CA (PMID: 23662903).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Taselisib RG7606|GDC-0032 PIK3CA inhibitor 16 PIK3CD inhibitor 25 PIK3CG inhibitor 8 Taselisib (GDC-0032) is a beta isoform-sparing PI3K inhibitor, with greater activity against oncogenic mutants of PIK3CA (PMID: 23662903).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA H1047X lung non-small cell carcinoma sensitive Taselisib Phase I Actionable In a Phase I trial, a non-small cell lung carcinoma patient harboring a mutation at PIK3CA H1047 demonstrated a confirmed partial response when treated with Taselisib (GDC-0032) (PMID: 28331003). 28331003
PIK3CA E453K lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, a patients harboring PIK3CA E453K did not demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA M1043I lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, a patients harboring PIK3CA M1043I did not demonstrated response (PMID: 31158500; NCT02785913). 31158500
ERBB2 amp uterine corpus serous adenocarcinoma sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, a uterine serous carcinoma cell line harboring ERBB2 (HER2) amplification demonstrated sensitivity to treatment with Taselisib (GDC-0032) in culture, resulting in inhibition of cell growth (PMID: 26333383). 26333383
PIK3CA N345K lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, none of the 2 patients harboring PIK3CA N345K demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA G1049R lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, a patients harboring PIK3CA G1047R did not demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA H1047R lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, none of the 4 patients harboring PIK3CA H1047R demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA act mut Advanced Solid Tumor conflicting Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, Taselisib (GDC-0032) effectively suppressed growth of multiple tumor types in cell line xenograft models, with greater selectivity for PIK3CA activating mutants (PMID: 23662903). 23662903
PIK3CA act mut Advanced Solid Tumor conflicting Taselisib Phase II Actionable In a Phase II (MATCH) trial, Taselisib (GDC-0032) treatment resulted in no objective response (0/65) but prolonged stable disease (estimated 6-month progression-free survival rate 27%) in patients with advanced solid tumors harboring PIK3CA activating mutations (J Clin Oncol 36, 2018 (suppl; abstr 101); NCT02465060). detail...
ERBB2 amp PIK3CA wild-type uterine corpus serous adenocarcinoma sensitive Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, Taselisib (GDC-0032) did not result in delay of cell cycle activity during treatment of a uterine serous carcinoma cell line harboring PIK3CA wild-type and ERBB2 (HER2) amplification in culture, however, did result in tumor growth inhibition in xenograft models (PMID: 26333383). 26333383
Unknown unknown Advanced Solid Tumor not applicable Taselisib Phase I Actionable In a Phase I trial, Taselisib (GDC-0032) demonstrated safety and preliminary efficacy in patients with advanced solid tumors (Cancer Res Feb 2016 (76) (4 Supplement) P3-14-10). detail...
PIK3CA H1047R breast cancer sensitive Taselisib Phase I Actionable In a Phase I trial, four patients with breast cancer harboring PIK3CA H1047R demonstrated a confirmed partial response when treated with Taselisib (GDC-0032) (PMID: 28331003). 28331003
PIK3CA mutant lung squamous cell carcinoma no benefit Taselisib Phase I Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, with only 1 responder in the primary analysis population (n=21) (PMID: 31158500; NCT02785913). 31158500
PIK3CA E545K lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, only 1 of the 11 patients harboring PIK3CA E545K demonstrated response (PMID: 31158500; NCT02785913). 31158500
PIK3CA E542K lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, none of the 6 patients harboring PIK3CA E542K demonstrated response (PMID: 31158500; NCT02785913). 31158500
ERBB2 pos PIK3CA act mut uterine cancer sensitive Taselisib Preclinical Actionable In a preclinical study, Taselisib (GDC-0032) inhibited growth of HER2 positive uterine cancer cell lines with PIK3CA mutations (PMID: 25172762). 25172762
PIK3CA mutant Advanced Solid Tumor sensitive Taselisib Phase I Actionable In a Phase I trial, Taselisib (GDC-0032) demonstrated activity in patients with PIK3CA-mutant advanced solid tumors, in the absence of alterations in the MAPK or PTEN pathways (Cancer Res October 1, 2014 74:915). detail...

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Clinical Trial Phase Therapies Title Recruitment Status
NCT02340221 Phase III Fulvestrant Taselisib SANDPIPER Study: A Study Of Taselisib + Fulvestrant Versus Placebo + Fulvestrant In Patients With Advanced or Metastatic Breast Cancer Who Have Disease Recurrence or Progression During or After Aromatase Inhibitor Therapy Active, not recruiting
NCT02390427 Phase I Trastuzumab Paclitaxel Pertuzumab Taselisib Phase Ib Dose-escalation Trial of Taselisib (GDC-0032) in Combination With Anti-HER2 Therapies in Participants With Advanced HER2+ Breast Cancer Active, not recruiting
NCT02273973 Phase II Taselisib Study of Neoadjuvant Letrozole + GDC-0032 Versus Letrozole + Placebo in Post-Menopausal Women With Breast Cancer (LORELEI) Completed
NCT02154490 Phase II Docetaxel Palbociclib Durvalumab AZD4547 Taselisib Erlotinib Rilotumumab Lung-MAP: S1400 Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IIIB-IV Squamous Cell Lung Cancer Active, not recruiting
NCT02785913 Phase II Taselisib Lung-MAP: Taselisib as Second-Line Therapy in Treating Patients With Recurrent Stage IV Squamous Cell Lung Cancer and Positive Biomarker Matches Completed
NCT02465060 Phase II Erdafitinib Copanlisib Trametinib Crizotinib Sunitinib Sapanisertib Nivolumab AZD4547 Dasatinib Pertuzumab + Trastuzumab Dabrafenib + Trametinib Binimetinib Adavosertib Osimertinib Palbociclib Afatinib Capivasertib Defactinib GSK2636771 Vismodegib Ado-trastuzumab emtansine Larotrectinib Taselisib Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) Recruiting
NCT01296555 Phase I Fulvestrant Taselisib Letrozole A Dose Escalation Study Evaluating the Safety and Tolerability of GDC-0032 in Patients With Locally Advanced or Metastatic Solid Tumors And in Combination With Endocrine Therapy in Patients With Locally Advanced or Metastatic Hormone Receptor-Positive Breast Cancer Active, not recruiting


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