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, PMID: 31439579). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Taselisib | RG7606|GDC-0032|RG-7604|RO5537381 | PIK3CA inhibitor 23 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 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 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 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 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 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 |
| 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 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 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 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 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 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 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 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 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 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 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 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 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 |
| 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 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 | 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 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 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 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 |
| 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 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 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 |
| 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 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 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02273973 | Phase II | Taselisib | Study of Neoadjuvant Letrozole + GDC-0032 Versus Letrozole + Placebo in Post-Menopausal Women With Breast Cancer (LORELEI) | Completed | USA | ITA | GBR | FRA | ESP | DEU | BEL | AUT | AUS | 13 |
| 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 | USA | 0 |
| 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 |
| 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 | Completed | USA | FRA | ESP | CAN | 0 |
| NCT02154490 | Phase II | Docetaxel Nivolumab Palbociclib Durvalumab Ipilimumab + Nivolumab AZD4547 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 |
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