^
    2d
    NCI-2022-06209: Testing Copanlisib as a Potential Targeted Treatment in Cancers With PIK3CA Mutations (MATCH-Subprotocol Z1F) (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Jan 2027
    Trial completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Aliqopa (copanlisib)
    3d
    EAY131-Z1G: Testing Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Loss (MATCH - Subprotocol Z1G) (clinicaltrials.gov)
    P2, N=22, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Jan 2027
    Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
    |
    Aliqopa (copanlisib)
    3d
    EAY131-Z1H: Testing Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Expression (MATCH - Subprotocol Z1H) (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Dec 2026
    Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
    |
    PTEN mutation
    |
    Aliqopa (copanlisib)
    25d
    Copanlisib With Ibrutinib for Patients With Recurrent/ Refractory Primary Central Nervous System Lymphoma (PCNSL) (clinicaltrials.gov)
    P1/2, N=18, Completed, Memorial Sloan Kettering Cancer Center | Active, not recruiting --> Completed | Trial completion date: Jul 2026 --> Feb 2026 | Trial primary completion date: Jul 2026 --> Feb 2026
    Trial completion • Trial completion date • Trial primary completion date
    |
    Imbruvica (ibrutinib) • Aliqopa (copanlisib)
    2ms
    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, Terminated, M.D. Anderson Cancer Center | Trial completion date: Feb 2027 --> Dec 2025 | Active, not recruiting --> Terminated; Copanlisib development was discontinued by Bayer following withdrawal of copanlisib in relapsed follicular lymphoma in November 2023.
    Trial completion date • Trial termination
    |
    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)
    |
    PIK3CA mutation • PTEN deletion
    |
    fulvestrant • Aliqopa (copanlisib)
    2ms
    Copanlisib Plus Venetoclax in R/R DLBCL (clinicaltrials.gov)
    P1/2, N=48, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Apr 2026 --> Jul 2026 | Trial primary completion date: Apr 2026 --> Jul 2025
    Trial completion date • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    Venclexta (venetoclax) • Aliqopa (copanlisib)
    2ms
    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 | Trial completion date: Nov 2025 --> Nov 2026 | Trial primary completion date: Nov 2025 --> Nov 2026
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    Opdivo (nivolumab) • Aliqopa (copanlisib)
    2ms
    Copanlisib Plus Venetoclax in R/R DLBCL (clinicaltrials.gov)
    P1/2, N=48, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Dec 2025 --> Apr 2026 | Trial primary completion date: Oct 2025 --> Apr 2026
    Trial completion date • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    Venclexta (venetoclax) • Aliqopa (copanlisib)
    3ms
    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=54, Active, not recruiting, National Cancer Institute (NCI) | N=102 --> 54 | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Oct 2025
    Enrollment change • Trial completion date • Trial primary completion date • Checkpoint inhibition • IO biomarker
    |
    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
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Aliqopa (copanlisib) • ABP 206 (nivolumab biosimilar)
    3ms
    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: Aug 2025 --> Feb 2027
    Trial completion date
    |
    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)
    |
    PIK3CA mutation • PTEN deletion
    |
    fulvestrant • Aliqopa (copanlisib)
    4ms
    BrUOG360: A phase Ib/II study of copanlisib in combination with rucaparib in patients with metastatic castration-resistant prostate cancer (mCRPC). (PubMed, Cancer Res Commun)
    Copa/R had a favorable safety profile with a signal of efficacy supporting future studies of PARPi with PI3Ki.
    P1/2 data • Journal
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • CDK12 (Cyclin dependent kinase 12) • FANCA (FA Complementation Group A) • RAD51C (RAD51 paralog C)
    |
    Rubraca (rucaparib) • Aliqopa (copanlisib)
    4ms
    Alpha-enolase influences ATP pool of cytoplasm and lactate homeostasis by regulating glycolysis in gastric cancer. (PubMed, Signal Transduct Target Ther)
    Furthermore, pharmacological studies revealed that metformin combined with copanlisib significantly inhibited tumors by blocking the energy metabolism pathways PI3K/AKT and AMPK/mTOR. Rationally, targeting multiple nodes along the ENO1-ATP/lactate-AMPK/PI3K/AKT-mTOR axis may be effective for GC treatment, as indicated by the significant suppression of tumor growth by metformin (which inhibits ATP production) plus syrosingopine (which disrupts lactate homeostasis). In conclusion, the complex interplay between metabolism and tumor stemness offers novel therapeutic directions and potential treatment strategies for GC.
    Journal
    |
    ENO1 (Enolase 1)
    |
    Aliqopa (copanlisib) • metformin • syrosingopine