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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, PMID: 31439579).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Taselisib RG7606|GDC-0032|RG-7604|RO5537381 PIK3CA inhibitor 24 PIK3CD inhibitor 27 PIK3CG inhibitor 10 Taselisib (GDC-0032) is a beta isoform-sparing PI3K inhibitor, with greater activity against oncogenic mutants of PIK3CA (PMID: 23662903, PMID: 31439579).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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, resulting in no responses in patients harboring PIK3CA H1047R (n=4) (PMID: 31158500; NCT02785913). 31158500
PIK3CA H1047R PTEN loss breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring a PIK3CA H1047R and PTEN loss was sensitive to treatment with Taselisib (GDC-0032) in culture, demonstrating decreased cell viability (PMID: 31534012). 31534012
PIK3CA I817F PIK3CA H1047R breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). 37916958
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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in a patient harboring PIK3CA E453K (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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no responses in patients harboring PIK3CA E542K (n=6) (PMID: 31158500; NCT02785913). 31158500
PIK3CA N1068Kfs*5 PTEN Y174H PTEN K263* colorectal cancer predicted - sensitive Taselisib Preclinical - Patient cell culture Actionable In a preclinical study, Taselisib (GDC-0032) inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1068Kfs*5, PTEN Y174H, and PTEN K263* in culture (PMID: 32376656). 32376656
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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in a patient harboring PIK3CA G1049R (PMID: 31158500; NCT02785913). 31158500
PIK3CA E542K PTEN loss breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA E542K was sensitive to treatment with Taselisib (GDC-0032) in culture, demonstrating decreased cell viability (PMID: 31534012). 31534012
PIK3CA N1044K colorectal cancer predicted - sensitive Taselisib Preclinical - Patient cell culture Actionable In a preclinical study, Taselisib (GDC-0032) inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1044K, along with KRAS G12D, in culture (PMID: 32376656). 32376656
PIK3CA E545K PIK3CA Q859H breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). 37916958
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 E545K PIK3CA I817F breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). 37916958
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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in only 1 response in the primary analysis population (n=21) (PMID: 31158500; NCT02785913). 31158500
PTEN del head and neck squamous cell carcinoma resistant Taselisib Preclinical Actionable In a preclinical study, head and neck squamous cell carcinoma cells homozygous for PTEN deletion were resistant to Taselisib (GDC-0032) in culture (PMID: 26589432). 26589432
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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in only 1 response of 11 patients harboring PIK3CA E545K (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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in a patient harboring PIK3CA M1043I (PMID: 31158500; NCT02785913). 31158500
PIK3CA H1047R colon cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). 34544753
PIK3CA E545K PIK3CA W780R breast cancer resistant Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). 37916958
PIK3CA Q859K PIK3CA H1047R breast cancer resistant Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). 37916958
PIK3CA E726K PIK3CA H1047R breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K in culture (PMID: 37916958). 37916958
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 its primary endpoint for response rate in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no response in two patients harboring PIK3CA N345K (PMID: 31158500; NCT02785913). 31158500
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...
PIK3CA Q859H PIK3CA H1047R breast cancer resistant Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). 37916958
PIK3CA act mut TSC1 del estrogen-receptor positive breast cancer resistant Taselisib Preclinical - Cell culture Actionable In a preclinical study, PIK3CA-mutant, ESR1 (ER)-positive breast cancer cell lines with knockout of TSC1 were resistant to treatment with Taselisib (GDC-0032) in culture (PMID: 33685991). 33685991
PIK3CA E545K colon cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA E545K in culture (PMID: 34544753). 34544753
PTEN mutant head and neck squamous cell carcinoma resistant Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, head and neck squamous cell carcinoma cell lines and cell line xenograft models with PTEN alterations were resistant to the apoptotic effects of Taselisib (GDC-0032) (PMID: 26589432). 26589432
PIK3CA E545K PIK3CA E726K breast cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). 37916958
PIK3CA W780R PIK3CA H1047R breast cancer resistant Taselisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R was resistant to Taselisib (GDC-0032) in culture (PMID: 37916958). 37916958
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 trial (MATCH), Taselisib (GDC-0032) treatment resulted in limited efficacy in heavily pretreated patients with advanced solid tumors harboring PIK3CA activating mutations, with an objective response rate of 0% (0/61) after a median follow-up of 35.7 months, stable disease in 52% (32/61), a median progression-free survival of 3.1 months, and a median overall survival of 7.2 months (PMID: 35138919; NCT02465060). 35138919
PIK3CA act mut TSC2 del estrogen-receptor positive breast cancer resistant Taselisib Preclinical - Cell culture Actionable In a preclinical study, PIK3CA-mutant, ESR1 (ER)-positive breast cancer cell lines with knockout of TSC2 were resistant to treatment with Taselisib (GDC-0032) in culture (PMID: 33685991). 33685991
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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
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 USA | CAN 0
NCT02154490 Phase II Docetaxel Nivolumab Palbociclib Durvalumab Ipilimumab + Nivolumab Fexagratinib Taselisib Durvalumab + Tremelimumab Erlotinib + Rilotumumab Talazoparib Erlotinib Lung-MAP: Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IV Squamous Cell Lung Cancer Completed USA | CAN 0
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 Completed USA 0
NCT02273973 Phase II Taselisib Study of Neoadjuvant Letrozole + GDC-0032 Versus Letrozole + Placebo in Post-Menopausal Women With Breast Cancer (LORELEI) Completed USA | POL | ITA | HUN | GBR | FRA | ESP | DEU | CZE | CHE | BRA | BEL | AUT | AUS 8
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 Terminated USA | FRA | ESP | CAN 0


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