taselisib (GDC-0032) / Roche 
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 6 Diseases   4 Trials   4 Trials   346 News 


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  • ||||||||||  tamoxifen / Generic mfg., taselisib (GDC-0032) / Roche, everolimus / Generic mfg.
    Journal, Circulating tumor DNA:  PI3K inhibition in combination with tamoxifen in patients with metastatic HR+/HER2- breast cancer: clinical and circulating tumor DNA results. (Pubmed Central) -  Feb 3, 2026   
    Our findings suggest efficacy of PI3K inhibition + tamoxifen beyond second-line treatment and after prior targeted therapies, including CDK4/6 inhibition in metastatic HR+/HER2- breast cancer although the magnitude of benefit did not outweigh the tolerability of this combination. Exploratory biomarker analysis indicates that tumor fraction determined in ctDNA differentiates patients based on prognosis and may help to optimize patient selection for targeted treatment strategies.
  • ||||||||||  taselisib (GDC-0032) / Roche, AZD8186 / AstraZeneca, serabelisib (MLN1117) / Takeda, Eli Lilly
    Review, Journal:  PI3K inhibitors: Efficacy in diverse cancer forms. (Pubmed Central) -  Dec 13, 2025   
    Research on the clinical development, therapeutic utility, and structural insights of new PI3K inhibitors is the main emphasis of this review. The inhibitors have been shown promising anticancer activity relationships.
  • ||||||||||  taselisib (GDC-0032) / Roche
    Mechanisms of Acquired Resistance to PI3K Inhibitors in Breast Cancer: The Central Role of Autophagy (Exhibit Hall) -  Oct 30, 2025 - Abstract #SABCS2025SABCS_672;    
    Taken together, our findings suggest that autophagy activation serves as a key adaptive mechanism driving acquired resistance to PI3K inhibitors such as taselisib in breast cancer. Targeting autophagy-related pathways may represent a promising therapeutic strategy to overcome or delay resistance and enhance the clinical efficacy of PI3K-targeted treatments.
  • ||||||||||  Ibrance (palbociclib) / Pfizer, taselisib (GDC-0032) / Roche, fulvestrant / Generic mfg.
    Clinical data, Journal:  Disease Modeling and External Model Evaluation Through Clinical Data Sharing Platform for HR+/HER2- Breast Cancer. (Pubmed Central) -  Sep 16, 2025   
    The TGI-OS model showed large underestimation for the OS for PALOMA-3; nevertheless, the predicted treatment effect (hazard ratio of OS) was in good agreement with the observation for both studies, suggesting its potential as a tool to support drug development decisions. While integrating shared clinical trial data from multiple sources, facilitated by platforms like Vivli, is crucial for advancing predictive modeling efforts, caution should be exercised when such models are applied for new studies, especially when there are breakthroughs in the treatment landscape.
  • ||||||||||  taselisib (GDC-0032) / Roche
    PIK3CA helical but not kinase mutations and enrichment of M2 macrophages predict response to taselisib in the LORELEI phase II randomized trial (Cologne Auditorium - CityCube A) -  Jul 24, 2025 - Abstract #ESMO2025ESMO_1719;    
    P2
    Table: 116MO ORR taselisib (%) ORR placebo (%) Odd ratio, CI95% P-value univariate P-value multivariate Helical domain PIK3CA- mutants All (68/159, 43%) 69% 33% 4.7 (1.8-12.5) < 0.01 < 0.01 E542K 83% 10% 34 (2.7-2119) < 0.01 0.02 E545K 59% 44% 1.86 (0.52-6.61) 0.34 - Kinase domain PIK3CA-mutants All (58/159, 36%) 47% 43% 1.2 (0.5-2.9) 0.98 - H1047R 42% 43% 0.98 (0.35-7.77) 0.94 - Invasive lobular breast cancers All (80/334, 24%) 63% 47% 1.9 (0.8-4.6) 0.21 - PIK3CA- mutants 64% 48% 1.72 (0.4-6.9) 0.54 - PIK3CA wild-type 62% 47% 1.82 (0.4-8.7) 0.50 - Breast cancer of NST All (209/334, 63%) 46% 38% 1.4 (0.8-2.4) 0.22 - PIK3CA- mutant 51% 34% 2.0 (0.9-4.8) 0.08 - PIK3CA wild-type (116/334, 35%) 42% 41% (0.5-2.2) 0.93 - Conclusions PIK3CA HDmt but not KDmt predict response to taselisib in early-stage ER+/HER2- BCs. In ILC, macrophage polarization and T cell reinvigoration may contribute to taselisib efficacy.
  • ||||||||||  Estybon (rigosertib) / Traws Pharma, SymBio Pharma, Knight Therap
    Unlocking therapeutic potential of rigosertib as a selective therapy for ovarian cancer (Section 34; Poster Board No: 28) -  Mar 25, 2025 - Abstract #AACR2025AACR_7782;    
    This combination showed synergy across ovarian cancer cell lines, organoids, and xenograft models, with xenograft studies showing a significant reduction in tumor burden. These findings highlight the potential of rigosertib, especially when paired with PI3K inhibitors, to target the unique mutational landscape of ovarian cancer, offering a promising direction for more effective treatments.
  • ||||||||||  Ibrance (palbociclib) / Pfizer, taselisib (GDC-0032) / Roche, pictilisib (GDC-0941) / Roche
    Trial completion:  PIPA: Combination of PI3 Kinase Inhibitors and PAlbociclib (clinicaltrials.gov) -  Sep 26, 2024   
    P1,  N=79, Completed, 
    Active, not recruiting --> Completed Unknown status --> Completed
  • ||||||||||  Inlyta (axitinib) / Pfizer, taselisib (GDC-0032) / Roche
    Journal:  Kinome expression profiling improves risk stratification and therapeutic targeting in myelodysplastic syndromes. (Pubmed Central) -  May 20, 2024   
    By investigating the Genomics of Drug Sensitivity in Cancer (GDSC) database, we identified axitinib and taselisib as candidate compounds that could potentially target the KISS-high myeloblasts. Altogether, our findings suggest that KISS holds the potential to improve the current prognostic scheme of MDS and inform novel therapeutic opportunities.
  • ||||||||||  taselisib (GDC-0032) / Roche, pictilisib (GDC-0941) / Roche
    Journal, Gene Signature, IO biomarker:  Assessing of programmed cell death gene signature for predicting ovarian cancer prognosis and treatment response. (Pubmed Central) -  Jun 25, 2023   
    In addition, we found that patients in the low-risk group responded better to immunotherapy. Risk Score of 9-gene composition of PCD signature possesses promising clinical potential in OV prognosis, immunotherapy, immune microenvironment activity, and chemotherapeutic drug selection, and our study provides the basis for an in-depth investigation of the PCD mechanism in OV.
  • ||||||||||  taselisib (GDC-0032) / Roche
    Preclinical, Journal:  Taselisib moderates neuropathic pain through PI3K/AKT signaling pathway in a rat model of chronic constriction injury. (Pubmed Central) -  Jun 20, 2023   
    Risk Score of 9-gene composition of PCD signature possesses promising clinical potential in OV prognosis, immunotherapy, immune microenvironment activity, and chemotherapeutic drug selection, and our study provides the basis for an in-depth investigation of the PCD mechanism in OV. Taselisib can alleviate neuropathic pain by inhibiting the pro-inflammatory response, potentially through the PI3K/AKT signaling pathway.
  • ||||||||||  MEN1611 / Menarini, Herceptin (trastuzumab) / Roche
    Journal:  Antitumor activity of the PI3K ?-sparing inhibitor MEN1611 in PIK3CA mutated, trastuzumab-resistant HER2?+?breast cancer. (Pubmed Central) -  May 1, 2023   
    P1
    The profile of MEN1611 and its antitumoral activity suggest an improved profile as compared to pan-inhibitors, which are limited by a less than ideal safety profile, and isoform selective molecules, which may potentially promote development of resistance mechanisms. The compelling antitumor activity in combination with trastuzumab in HER2?+?trastuzumab-resistant, PIK3CA mutated breast cancer models is at the basis of the ongoing B-Precise clinical trial (NCT03767335).
  • ||||||||||  Journal:  Synthetic methodologies and SAR of quinazoline derivatives as PI3K inhibitors. (Pubmed Central) -  Jan 18, 2023   
    Lapatinib, afatinib, gefitinib, erlotinib, idelalisib and copanlisib are quinazoline-based, FDA-approved PI3K inhibitors, while compounds like NVPBYL719, GDC-0032, AZD8186, AZD-6482, etc. are under different stages of clinical trials. In light of the above-mentioned facts, in the present study, we have reported different synthetic approaches, mechanisms of anticancer action, and structure-activity relationship analysis of reported quinazoline derivatives as PI3K inhibitors to help researchers working in the field in designing better and isoform-selective PI3K inhibitors.
  • ||||||||||  taselisib (GDC-0032) / Roche, AZD8186 / AstraZeneca, serabelisib (MLN1117) / Takeda
    Journal:  Recent Advances of PI3 Kinase Inhibitors: Structure Anticancer Activity Relationship Studies. (Pubmed Central) -  Dec 7, 2022   
    The PI3K inhibitors which are under clinical trial studies include GDC-0032, INK1117 for PI3K-α, and AZD8186 for PI3K-β. This review primarily focuses on the structural insights and structure anticancer activity relationship studies of recent PI3K inhibitors including their clinical stages of development and therapeutic values.
  • ||||||||||  taselisib (GDC-0032) / Roche, PD-407824 / Weill Cornell Medical College
    Journal, BRCA Biomarker:  Integrative analysis of m3C associated genes reveals METTL2A as a potential oncogene in breast Cancer. (Pubmed Central) -  Oct 28, 2022   
    Overall, our research conducts a holistic view of the expression level and prognostic signature of m3C-related genes with multiple malignancies. Importantly, METTL2A has been intensely explored as a potential oncogene in BRCA, to aid the development of potential drug agents for precision therapy in breast cancer patients.
  • ||||||||||  taselisib (GDC-0032) / Roche
    Trial completion, Enrollment change, Trial completion date:  Poseidon: Clinical Trial to Evaluate the Safety and Effectiveness of GDC-0032 When Given Alongside Tamoxifen (clinicaltrials.gov) -  Oct 12, 2022   
    P2,  N=189, Completed, 
    Importantly, METTL2A has been intensely explored as a potential oncogene in BRCA, to aid the development of potential drug agents for precision therapy in breast cancer patients. Suspended --> Completed | N=290 --> 189 | Trial completion date: Dec 2022 --> May 2022
  • ||||||||||  LOXO-783 / Eli Lilly
    LOXO-783: A potent, highly mutant selective and brain-penetrant allosteric PI3Kα H1047R inhibitor in combination with standard of care (SOC) treatments in preclinical PI3Kα H1047R-mutant breast cancer models (Hall 1) -  Oct 10, 2022 - Abstract #SABCS2022SABCS_1159;    
    P1
    Results Combining LOXO-783 with either fulvestrant (FUL; CI at 50% inhibition = 0.28) or imlunestrant (CI at 50% inhibition = 0.43) showed increased efficacy in cell proliferation assays using the HR+, HER2-, PI3Kα H1047R- mutant T47D model...Similar results were observed in a T47D model engineered to express ESR1 D538G, as well as in an HR+, HER2- PI3Kα double in-cis mutant model (H1047R/D350G) also harboring ESR1 D538G and derived from a patient who had progressed on prior letrozole plus taselisib...Extending these studies to additional treatment settings, LOXO-783 was similarly efficacious as a single agent in abemaciclib-resistant and abemaciclib/FUL double-resistant models, and was additive in combination with paclitaxel in a triple negative breast cancer model in vitro and in vivo...LOXO-783 is also efficacious in ESR1 mutant as well as in abemaciclib and abemaciclib/FUL double-resistant models. A phase 1 trial of LOXO-783 alone or in combination with anticancer therapies is ongoing (PIKASSO-01; NCT05307705).
  • ||||||||||  taselisib (GDC-0032) / Roche, AZD8186 / AstraZeneca, serabelisib (MLN1117) / Takeda, Petra Pharma, Faeth Therap
    Journal:  Recent Advances of PI3 Kinase Inhibitors: Structure Anticancer Activity Relationship Studies. (Pubmed Central) -  Sep 20, 2022   
    The PI3K inhibitors which are under clinical trial studies include GDC-0032, INK1117 for PI3K-α, and AZD8186 for PI3K-β. This review primarily focuses on the structural insights and structure anticancer activity relationship studies of recent PI3K inhibitors including their clinical stages of development and therapeutic values.
  • ||||||||||  Mekinist (trametinib) / Novartis, taselisib (GDC-0032) / Roche, Cotellic (cobimetinib) / Exelixis, Roche
    Journal:  Dual inhibition of the MEK/ERK and PI3K/AKT pathways prevents pulmonary GVHD suppressing perivenulitis and bronchiolitis. (Pubmed Central) -  Apr 26, 2022   
    Imaging mass cytometry of human pGVHD revealed that T cells around bronchioles were positive for phosphorylated ERK, while B cells were positive for phosphorylated AKT. Thus, perivascular inflammation and bronchiolitis mediated by activation of the MEK/ERK and PI3K/AKT pathways are essential for pGVHD and represent a potential novel therapeutic target in humans.
  • ||||||||||  Mekinist (trametinib) / Novartis
    Journal:  Functional proteomics of patient derived head and neck squamous cell carcinoma cells reveal novel applications of trametinib. (Pubmed Central) -  Apr 5, 2022   
    The combination regimen of trametinib and AXL/MET/VEGFR inhibitor glesatinib showed initial efficacy both in vitro and in vivo (92% reduction in tumor volume)...Furthermore, resistant cell lines showed a compensatory mechanism via increases in MAPK and non-MAPK pathway proteins that may represent targets for future combination regimens. Intrinsic-targeted options have potential to address paucity of medical treatment options for HNSCC cancer patients, enhance response to extrinsic targeted agents, and/or reduce morbidity as neoadjuvant to surgical treatments.
  • ||||||||||  inavolisib (GDC-0077) / Roche
    Clinical, Journal:  RTK-dependent inducible degradation of mutant PI3Kα drives GDC-0077 (Inavolisib) efficacy. (Pubmed Central) -  Mar 31, 2022   
    Both are more effective than other PI3K inhibitors at maintaining prolonged pathway suppression. This study establishes a new strategy for identifying inhibitors that specifically target mutant tumors by selective degradation of the mutant oncoprotein and provide a strong rationale for pursuing PI3Kα degraders in patients with HER2-positive breast cancer.