^
    15d
    Integrated mutational landscape analysis of poorly differentiated high-grade neuroendocrine carcinoma of the uterine cervix. (PubMed, Proc Natl Acad Sci U S A)
    However, combinations of copanlisib/afatinib and copanlisib/elimusertib were significantly more effective in controlling NETc tumor growth. These findings define the genetic landscape of NETc and suggest that a large subset of these highly lethal malignancies might benefit from existing targeted therapies.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • PTEN (Phosphatase and tensin homolog) • RB1 (RB Transcriptional Corepressor 1) • ARID1A (AT-rich interaction domain 1A) • KMT2D (Lysine Methyltransferase 2D) • NOTCH2 (Notch 2) • MLL2 (Myeloid/lymphoid or mixed-lineage leukemia 2) • MBD4 (Methyl-CpG Binding Domain 4, DNA Glycosylase) • PVT1 (Pvt1 Oncogene) • RPL10 (Ribosomal Protein L10)
    |
    KRAS mutation • PIK3CA mutation • ARID1A mutation • KMT2D mutation
    |
    Gilotrif (afatinib) • Aliqopa (copanlisib) • elimusertib (BAY 1895344)
    24d
    Testing Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Loss (MATCH - Subprotocol Z1G) (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, National Cancer Institute (NCI)
    New P2 trial
    |
    Aliqopa (copanlisib)
    1m
    BrUOG 360: A Study of Copanlisib Combined With Rucaparib in Patients With Metastatic Castration-resistant Prostate Cancer (clinicaltrials.gov)
    P1/2, N=13, Active, not recruiting, Brown University | Trial completion date: May 2024 --> Jan 2027 | Trial primary completion date: Jan 2024 --> Jan 2027
    Trial completion date • Trial primary completion date • Metastases
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • CDK12 (Cyclin dependent kinase 12) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D) • CHEK1 (Checkpoint kinase 1) • BARD1 (BRCA1 Associated RING Domain 1) • RAD54L (DNA Repair And Recombination Protein RAD54) • FANCL (FA Complementation Group L) • PPP2R2A (Protein Phosphatase 2, Regulatory Subunit B, Alpha)
    |
    BRIP1 mutation
    |
    Rubraca (rucaparib) • Aliqopa (copanlisib)
    1m
    Copanlisib and Avelumab as a Maintenance Therapy for Advanced Bladder Cancer (clinicaltrials.gov)
    P1/2, N=29, Not yet recruiting, VA Office of Research and Development | Phase classification: P2 --> P1/2 | Trial completion date: Jun 2028 --> Dec 2028 | Trial primary completion date: Dec 2027 --> Jun 2028
    Phase classification • Trial completion date • Trial primary completion date • Metastases
    |
    Bavencio (avelumab) • Aliqopa (copanlisib)
    2ms
    Testing the Addition of Copanlisib to Usual Treatment (Fulvestrant and Abemaciclib) in Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2; N=204 --> 24 | Trial completion date: Nov 2024 --> Mar 2025 | Trial primary completion date: Nov 2024 --> Jun 2023
    Combination therapy • Trial completion date • Trial primary completion date • Enrollment change • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog)
    |
    HER-2 amplification • HER-2 negative • PGR positive
    |
    Prosigna™ Breast Cancer Prognostic Gene Signature Assay
    |
    Verzenio (abemaciclib) • fulvestrant • Aliqopa (copanlisib)
    2ms
    Alternative-C: A Prospective Multicenter Phase 2 Study of the Chemotherapy-Free Combination of the Intravenous Phosphatidylinositol-3-Kinase (PI3K) Inhibitor Copanlisib in Combination With Obinutuzumab in Patients With Previously Untreated Follicular Lymphoma (FL) and a High Tumor Burden (clinicaltrials.gov)
    P2, N=98, Active, not recruiting, Ludwig-Maximilians - University of Munich | Recruiting --> Active, not recruiting | Trial primary completion date: Oct 2022 --> Sep 2023
    Enrollment closed • Trial primary completion date • Combination therapy
    |
    Gazyva (obinutuzumab) • Aliqopa (copanlisib)
    2ms
    Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial (clinicaltrials.gov)
    P1, N=2, Terminated, OHSU Knight Cancer Institute | Active, not recruiting --> Terminated; Low accrual
    Trial termination
    |
    Keytruda (pembrolizumab) • Opdivo (nivolumab) • Avastin (bevacizumab) • Venclexta (venetoclax) • Lynparza (olaparib) • Mekinist (trametinib) • erlotinib • Gilotrif (afatinib) • Yervoy (ipilimumab) • Ibrance (palbociclib) • dasatinib • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • carboplatin • Imfinzi (durvalumab) • sorafenib • Rozlytrek (entrectinib) • imatinib • Sutent (sunitinib) • everolimus • Nerlynx (neratinib) • Iclusig (ponatinib) • Kadcyla (ado-trastuzumab emtansine) • Cotellic (cobimetinib) • Lorbrena (lorlatinib) • Lenvima (lenvatinib) • bortezomib • doxorubicin hydrochloride • capecitabine • Verzenio (abemaciclib) • Xtandi (enzalutamide capsule) • Cabometyx (cabozantinib tablet) • albumin-bound paclitaxel • Stivarga (regorafenib) • abiraterone acetate • oxaliplatin • Aliqopa (copanlisib) • Vizimpro (dacomitinib) • Zydelig (idelalisib) • daunorubicin • Zolinza (vorinostat) • Idhifa (enasidenib) • Farydak (panobinostat) • Erivedge (vismodegib) • Nubeqa (darolutamide) • bicalutamide • leucovorin calcium • cabazitaxel • Vesanoid (tretinoin) • fluorouracil topical
    2ms
    Vemurafenib Plus Copanlisib in Radioiodine-Refractory (RAIR) Thyroid Cancers (clinicaltrials.gov)
    P1, N=8, Completed, Memorial Sloan Kettering Cancer Center | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Sep 2023
    Trial completion • Trial completion date
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation • BRAF V600
    |
    Zelboraf (vemurafenib) • Aliqopa (copanlisib)
    3ms
    Expanded Access to Provide Copanlisib for Patients With Cancer Who Are Experiencing a Positive Response, as Determined by Their Doctors (clinicaltrials.gov)
    P=N/A, N=0, No Longer Available, Bayer
    New trial
    |
    Aliqopa (copanlisib)
    3ms
    LCD: Lung Cancer With Copanlisib and Durvalumab (clinicaltrials.gov)
    P1, N=11, Active, not recruiting, Zhonglin Hao | Recruiting --> Active, not recruiting | N=18 --> 11 | Trial completion date: Jun 2031 --> Jun 2025 | Trial primary completion date: Jun 2031 --> Jun 2025
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Metastases
    |
    Imfinzi (durvalumab) • Aliqopa (copanlisib)
    3ms
    β1 integrin mediates unresponsiveness to PI3Kα inhibition for radiochemosensitization of 3D HNSCC models. (PubMed, Biomed Pharmacother)
    Here, we investigated the radiochemosensitizing potential and adaptation mechanisms of four PI3K inhibitors, Alpelisib, Copanlisib, AZD8186, and Idelalisib in eight HNSCC models grown under physiological, three-dimensional matrix conditions. Finally, we demonstrate that targeting of the cell adhesion molecule β1 integrin on top of Alpelisib sensitizes non-responders to radiochemotherapy. Taken together, our study demonstrates the sensitizing potential of Alpelisib and other PI3K inhibitors in HNSCC models and uncovers a novel β1 integrin-dependent mechanism that may prove useful in overcoming resistance to PI3K inhibitors.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Piqray (alpelisib) • Aliqopa (copanlisib) • Zydelig (idelalisib) • AZD8186
    3ms
    Lung Fibroblasts Take up Breast Cancer Cell-derived Extracellular Vesicles Partially Through MEK2-dependent Macropinocytosis. (PubMed, Cancer Res Commun)
    Among the drugs identified to inhibit EV uptake without exerting significant cytotoxicity, we validated the dose-dependent effect of Trametinib (a MEK1/2 inhibitor) and Copanlisib (a PI3K inhibitor). Through a phenotypic screen, we found that MEK inhibitor Trametinib suppressed EV uptake and macropinocytosis in lung fibroblasts, and that EV uptake is mediated by MEK2 in these cells. Our results suggest that MEK2 inhibition could serve as a strategy to block cancer EV uptake by lung fibroblasts.
    Journal
    |
    MAP2K2 (Mitogen-activated protein kinase kinase 2)
    |
    Mekinist (trametinib) • Aliqopa (copanlisib)
    3ms
    A Study of Copanlisib in Combination With Degarelix in People With Prostate Cancer (clinicaltrials.gov)
    P1/2, N=37, Recruiting, Memorial Sloan Kettering Cancer Center
    New P1/2 trial • Combination therapy
    |
    Aliqopa (copanlisib) • Firmagon (degarelix)
    4ms
    Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations (clinicaltrials.gov)
    P2, N=7, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Oct 2026 --> Aug 2024 | Trial primary completion date: Oct 2026 --> Aug 2024
    Trial completion date • Trial primary completion date • Combination therapy
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • PI3K (Phosphoinositide 3-kinases)
    |
    ER positive • PIK3CA mutation • PTEN deletion • PIK3R1 mutation
    |
    fulvestrant • Aliqopa (copanlisib)
    4ms
    Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis. (PubMed, Mol Oncol)
    Combination treatment with the AR inhibitor darolutamide led to enhanced apoptosis in these cell lines, the effects being most pronounced upon cotreatment with the pan-PI3K inhibitor copanlisib. Importantly, immunohistochemistry analysis of these treated tumors showed increased apoptosis, as revealed by elevated levels of cleaved caspase 3 and Bcl-2-binding component 3 (BBC3). In conclusion, these data demonstrate that concurrent blockade of the PI3K/AKT/mTOR and AR pathways has superior antitumor efficacy and induces apoptosis in androgen-sensitive prostate cancer cell lines and PDX models.
    Preclinical • Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • AR (Androgen receptor) • CASP3 (Caspase 3) • CASP7 (Caspase 7) • BBC3 (BCL2 Binding Component 3)
    |
    Aliqopa (copanlisib) • Nubeqa (darolutamide)
    4ms
    Study of PI3Kinase Inhibition (Copanlisib) and Anti-PD-1 Antibody Nivolumab in Relapsed/Refractory Solid Tumors With Expansions in Mismatch-repair Proficient (MSS) Colorectal Cancer (clinicaltrials.gov)
    P1/2, N=48, Active, not recruiting, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Trial completion date: Dec 2023 --> Jun 2025
    Trial completion date • Mismatch repair
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene)
    |
    KRAS wild-type • BRAF wild-type • NRAS wild-type
    |
    Opdivo (nivolumab) • Aliqopa (copanlisib)
    4ms
    NCI-2018-01880: Copanlisib and Nivolumab in Treating Patients With Richter's Transformation or Transformed Indolent Non-Hodgkin Lymphoma (clinicaltrials.gov)
    P1, N=27, Active, not recruiting, City of Hope Medical Center | Recruiting --> Active, not recruiting | Trial completion date: Dec 2023 --> Jul 2024 | Trial primary completion date: Dec 2023 --> Jul 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    Opdivo (nivolumab) • Aliqopa (copanlisib)
    4ms
    COPA-R-CHOP: Copanlisib in Combination With Rituximab and CHOP Chemotherapy in Patients With Previously Untreated DLBCL (clinicaltrials.gov)
    P2, N=62, Active, not recruiting, University Hospital Muenster | Recruiting --> Active, not recruiting | Trial completion date: Jun 2024 --> Apr 2025 | Trial primary completion date: Jun 2024 --> Apr 2025
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    BCL6 rearrangement • BCL2 rearrangement
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • Aliqopa (copanlisib)
    4ms
    Testing the Addition of Copanlisib to Eribulin for the Treatment of Advanced-Stage Triple Negative Breast Cancer (clinicaltrials.gov)
    P1/2, N=106, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog)
    |
    HER-2 amplification • HER-2 negative • PIK3CA mutation • PTEN mutation
    |
    Halaven (eribulin mesylate) • Aliqopa (copanlisib)
    4ms
    Testing the Addition of an Anti-cancer Drug, Copanlisib, to the Usual Immunotherapy (Nivolumab With or Without Ipilimumab) in Patients With Advanced Solid Cancers That Have Changes in the Following Genes: PIK3CA and PTEN (clinicaltrials.gov)
    P1/2, N=102, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date • Checkpoint inhibition • IO biomarker • Metastases
    |
    PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation • PTEN mutation • PIK3CA E545 • PIK3CA H1047 • PIK3CA E542
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Aliqopa (copanlisib) • ABP 206 (nivolumab biosimilar)
    4ms
    Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations (clinicaltrials.gov)
    P2, N=7, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting | N=78 --> 7
    Enrollment closed • Enrollment change • Combination therapy
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • PI3K (Phosphoinositide 3-kinases)
    |
    ER positive • PIK3CA mutation • PTEN deletion • PIK3R1 mutation
    |
    fulvestrant • Aliqopa (copanlisib)
    5ms
    Testing the Combination of the Anti-cancer Drugs Copanlisib, Olaparib, and MEDI4736 (Durvalumab) in Patients With Advanced Solid Tumors With Selected Mutations (clinicaltrials.gov)
    P1, N=108, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2024 --> Dec 2024 | Trial primary completion date: Jun 2024 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • CD4 (CD4 Molecule) • RAD51D (RAD51 paralog D) • BARD1 (BRCA1 Associated RING Domain 1) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin))
    |
    PIK3CA mutation • PTEN mutation • PALB2 mutation • CDK12 mutation • PIK3CA E545 • PIK3CA H1047 • BARD1 mutation • PIK3CA E542 • RAD51 mutation
    |
    Lynparza (olaparib) • Imfinzi (durvalumab) • Aliqopa (copanlisib)
    5ms
    Window Trial to Evaluate Molecular Response to PI3K Inhibition With Copanlisib in r/r Adult B-cell ALL (clinicaltrials.gov)
    P1, N=3, Terminated, Dorothy Sipkins, MD, PhD | N=10 --> 3 | Trial completion date: May 2024 --> Apr 2023 | Recruiting --> Terminated | Trial primary completion date: May 2024 --> Apr 2023; Sponsor halted clinical development of study drug
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    ITGA6 (Integrin, alpha 6)
    |
    Aliqopa (copanlisib)
    5ms
    Testing the Combination of the Anti-cancer Drugs Copanlisib, Olaparib, and MEDI4736 (Durvalumab) in Patients With Advanced Solid Tumors With Selected Mutations (clinicaltrials.gov)
    P1, N=108, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • CD4 (CD4 Molecule) • RAD51D (RAD51 paralog D) • BARD1 (BRCA1 Associated RING Domain 1) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin))
    |
    PIK3CA mutation • PTEN mutation • PALB2 mutation • CDK12 mutation • PIK3CA E545 • PIK3CA H1047 • BARD1 mutation • PIK3CA E542 • RAD51 mutation
    |
    Lynparza (olaparib) • Imfinzi (durvalumab) • Aliqopa (copanlisib)
    5ms
    Copanlisib With Ibrutinib for Patients With Recurrent/ Refractory Primary Central Nervous System Lymphoma (PCNSL) (clinicaltrials.gov)
    P1/2, N=18, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=45 --> 18
    Enrollment closed • Enrollment change
    |
    Imbruvica (ibrutinib) • Aliqopa (copanlisib)
    5ms
    FIL_Copa-RB: Copanlisib With Rituximab-Bendamustine in Patients With Relapsed-Refractory Diffuse Large B-cell Lymphoma (clinicaltrials.gov)
    P2, N=37, Active, not recruiting, Fondazione Italiana Linfomi - ETS | Trial primary completion date: Jul 2023 --> Aug 2024
    Trial primary completion date • Combination therapy
    |
    BCL2 (B-cell CLL/lymphoma 2) • CD20 (Membrane Spanning 4-Domains A1) • BCL6 (B-cell CLL/lymphoma 6)
    |
    CD20 positive • BCL6 rearrangement • BCL2 rearrangement
    |
    Rituxan (rituximab) • Aliqopa (copanlisib) • bendamustine
    5ms
    Copanlisib and Venetoclax for the Treatment of Relapsed or Refractory Mantle Cell Lymphoma (clinicaltrials.gov)
    P1/2, N=23, Suspended, City of Hope Medical Center | Trial completion date: Dec 2023 --> Nov 2024 | Recruiting --> Suspended | Trial primary completion date: Dec 2023 --> Nov 2024
    Trial completion date • Trial suspension • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • CD20 (Membrane Spanning 4-Domains A1) • CCND1 (Cyclin D1) • PAX5 (Paired Box 5) • CD5 (CD5 Molecule)
    |
    Chr t(11;14) • CCND1 overexpression • PAX5 overexpression
    |
    Venclexta (venetoclax) • Aliqopa (copanlisib)
    5ms
    CHRONOS-3: Copanlisib and Rituximab in Relapsed Indolent B-cell Non-Hodgkin's Lymphoma (iNHL) (clinicaltrials.gov)
    P3, N=458, Active, not recruiting, Bayer | Trial completion date: Jan 2027 --> May 2024
    Trial completion date • Combination therapy
    |
    CD20 positive
    |
    Rituxan (rituximab) • Aliqopa (copanlisib)
    5ms
    Copanlisib With Dose-Adjusted EPOCH-R in Relapsed and Refractory Burkitt Lymphoma and Other High-Grade B-cell Lymphomas (clinicaltrials.gov)
    P1, N=8, Completed, National Cancer Institute (NCI) | Active, not recruiting --> Completed | N=39 --> 8 | Trial completion date: Jul 2025 --> Nov 2023
    Trial completion • Enrollment change • Trial completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    BCL6 rearrangement • BCL2 rearrangement
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • Aliqopa (copanlisib) • vincristine
    5ms
    Suppression of tumor cell lactate-generating signaling pathways eradicates murine PTEN/p53-deficient aggressive-variant prostate cancer via macrophage phagocytosis. (PubMed, Clin Cancer Res)
    Abrogation of lactate-mediated cross-talk between cancer cells and TAM results in durable ADT-independent tumor control in PTEN/p53-deficient AVPC, and warrants further investigation in clinical trials.
    Preclinical • Journal • Tumor cell
    |
    PTEN (Phosphatase and tensin homolog)
    |
    Mekinist (trametinib) • Aliqopa (copanlisib)
    5ms
    A Systematic Literature Review (SLR) and Meta-Analysis of Clinical Evidence of Second Line or Later (2L+) Treatments for Follicular Lymphoma (FL) in Adult Patients (ASH 2023)
    Eligible treatments included CAR T cell therapies (axicabtagene ciloleucel, lisocabtagene maraleucel, and tisagenlecleucel), T cell engagers (mosunetuzumab, glofitamab, epcoritamab, odronextamab), phosphatidylinositol 3-kinase (PI3K) inhibitors (copanlisib, duvelisib, idelalisib), HSCT, yttrium-90 (90Y) ibritumomab tiuxetan, tazemetostat, and conventional therapies (immunochemotherapies, single- or multiagent chemo- or immunotherapies, and alkylating agents). This SLR demonstrated an evolving FL treatment landscape, with new agents such as CAR T cell therapies and T cell engagers exhibiting potential for improving effectiveness of treatment for patients in 3L+, 4L+, and 2L+ POD24 populations.
    Retrospective data • Review
    |
    Aliqopa (copanlisib) • Zydelig (idelalisib) • Copiktra (duvelisib) • Yescarta (axicabtagene ciloleucel) • Breyanzi (lisocabtagene maraleucel) • Tazverik (tazemetostat) • Kymriah (tisagenlecleucel-T) • Epkinly (epcoritamab-bysp) • Zevalin (ibritumomab tiuxetan) • Lunsumio (mosunetuzumab-axgb) • Columvi (glofitamab-gxbm) • odronextamab (REGN1979)
    5ms
    CHRONOS-4: Study of Copanlisib in Combination With Standard Immunochemotherapy in Relapsed Indolent Non-Hodgkin's Lymphoma (iNHL) (clinicaltrials.gov)
    P3, N=547, Terminated, Bayer | The addition of copanlisib to standard immunochemo therapy did not improve progression-free survival compared to the control arm. Base on the study results, company decided to terminate the study.
    Trial completion date • Trial termination • Combination therapy
    |
    CD20 positive
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • Aliqopa (copanlisib) • vincristine • bendamustine
    5ms
    Testing the Addition of Copanlisib to Eribulin for the Treatment of Advanced-Stage Triple Negative Breast Cancer (clinicaltrials.gov)
    P1/2, N=106, Active, not recruiting, National Cancer Institute (NCI) | Suspended --> Active, not recruiting
    Enrollment closed
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog)
    |
    HER-2 amplification • HER-2 negative • PIK3CA mutation • PTEN mutation
    |
    Halaven (eribulin mesylate) • Aliqopa (copanlisib)
    5ms
    Testing the Addition of Copanlisib to Usual Treatment (Fulvestrant and Abemaciclib) in Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2; Suspended --> Active, not recruiting
    Enrollment closed
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog)
    |
    HER-2 amplification • HER-2 negative • PGR positive
    |
    Prosigna™ Breast Cancer Prognostic Gene Signature Assay
    |
    Verzenio (abemaciclib) • fulvestrant • Aliqopa (copanlisib)
    5ms
    The ATR inhibitor elimusertib exhibits anti-lymphoma activity and synergizes with the PI3K inhibitor copanlisib. (PubMed, Br J Haematol)
    In several tumour models, elimusertib demonstrated widespread anti-tumour activity stronger than ceralasertib, another ATR inhibitor. This activity is present in both DDR-proficient and DDR-deficient lymphoma models. Furthermore, a combination of ATR and PI3K inhibition by treatment with elimusertib and copanlisib has in vitro and in vivo anti-tumour activity, providing a potential new treatment option for lymphoma patients.
    Journal
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A)
    |
    Aliqopa (copanlisib) • ceralasertib (AZD6738) • elimusertib (BAY 1895344)
    6ms
    Testing the Addition of Copanlisib to Eribulin for the Treatment of Advanced-Stage Triple Negative Breast Cancer (clinicaltrials.gov)
    P1/2, N=106, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension • Combination therapy • Metastases
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog)
    |
    HER-2 amplification • HER-2 negative • PIK3CA mutation • PTEN mutation
    |
    Halaven (eribulin mesylate) • Aliqopa (copanlisib)
    6ms
    Response-Adapted Therapy With Copanlisib and Rituximab in Untreated Follicular Lymphoma (clinicaltrials.gov)
    P2, N=22, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting | N=65 --> 22
    Enrollment closed • Enrollment change
    |
    Rituxan (rituximab) • Aliqopa (copanlisib)
    6ms
    Testing the Combination of the Anti-cancer Drugs Copanlisib, Olaparib, and MEDI4736 (Durvalumab) in Patients With Advanced Solid Tumors With Selected Mutations (clinicaltrials.gov)
    P1, N=108, Recruiting, National Cancer Institute (NCI) | Phase classification: P1b --> P1
    Phase classification • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • CD4 (CD4 Molecule) • RAD51D (RAD51 paralog D) • BARD1 (BRCA1 Associated RING Domain 1) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin))
    |
    PIK3CA mutation • PTEN mutation • PALB2 mutation • CDK12 mutation • PIK3CA E545 • PIK3CA H1047 • BARD1 mutation • PIK3CA E542 • RAD51 mutation
    |
    Lynparza (olaparib) • Imfinzi (durvalumab) • Aliqopa (copanlisib)
    6ms
    Copanlisib With Dose-Adjusted EPOCH-R in Relapsed and Refractory Burkitt Lymphoma and Other High-Grade B-cell Lymphomas (clinicaltrials.gov)
    P1, N=39, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting | Trial primary completion date: Jul 2025 --> Jan 2024
    Enrollment closed • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    BCL6 rearrangement • BCL2 rearrangement
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • Aliqopa (copanlisib) • vincristine
    6ms
    Pan-PI3K inhibition with copanlisib overcomes Treg- and M2-TAM-mediated immune suppression and promotes anti-tumor immune responses. (PubMed, Clin Exp Med)
    Importantly, in an ICI-sensitive model, combination therapy resulted in complete remission and prevention of tumor recurrence. Thus, the combination of ICIs with PI3K inhibition by intermittently dosed copanlisib represents a promising new strategy to increase sensitivity to ICI therapies and to treat human solid cancers.
    Journal
    |
    CD8 (cluster of differentiation 8)
    |
    Aliqopa (copanlisib)
    6ms
    Testing the Addition of an Anti-cancer Drug, Copanlisib, to the Usual Maintenance Treatment (Trastuzumab and Pertuzumab) After Initial Chemotherapy in a Phase Ib/II Trial for Advanced HER2 Positive Breast Cancer (clinicaltrials.gov)
    P1/2, N=2, Terminated, National Cancer Institute (NCI) | N=12 --> 2 | Recruiting --> Terminated; Inadequate accrual rate
    Enrollment change • Trial termination • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    HR positive • PIK3CA mutation • PTEN mutation
    |
    Herceptin (trastuzumab) • Aliqopa (copanlisib) • Trazimera (trastuzumab-qyyp) • TQB2440 (pertuzumab biosimilar) • BCD-178 (pertuzumab biosimilar) • EG1206A (pertuzumab biosimilar)