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    DRUG:

    tenalisib (RP6530)

    i
    Other names: RP6530, RP-6530, CN401
    Company:
    Curon Biopharma, Rhizen
    Drug class:
    PI3K inhibitor, PI3Kδ inhibitor, PI3Kγ inhibitor, SIK3 inhibitor
    Related drugs:
    28d
    Osteosarcoma-on-a-chip model mimicking intra-tumoral heterogeneity to interrogate tumor-associated macrophage reprogramming for immunotherapeutics. (PubMed, Biomaterials)
    Additionally, we employed pexidartinib and tenalisib to evaluate TAMs reversal in the iTC-OS-on-a-chip model by selectively inhibiting CSF1R and PI3Kγ, respectively. TAMs reprogramming from tumor promoting M2 to tumor suppressing M1 phenotype is confirmed through gene expression analysis of M1 (CCR7, IL-1β, IL-6) and M2 (CD206, CD163, IL-10) macrophage markers, alongside quantification of secreted cytokines via ELISA assay. This advanced iTC-OS-on-a-chip model offers a robust platform for investigating OS-immune cell interactions, enabling pre-clinical evaluation of chemo/immunotherapeutics and improving the translational relevance in OS research.
    Journal • IO biomarker
    |
    IL6 (Interleukin 6) • CD163 (CD163 Molecule) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • IL10 (Interleukin 10) • CCR7 (Chemokine (C-C motif) receptor 7) • CSF1R (Colony stimulating factor 1 receptor) • IL1B (Interleukin 1, beta) • MRC1 (Mannose Receptor C-Type 1)
    |
    Turalio (pexidartinib) • tenalisib (RP6530)
    2ms
    Efficacy and Safety of Tenalisib in Patients With Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=40, Recruiting, Rhizen Pharmaceuticals SA | Trial completion date: Mar 2026 --> Mar 2027 | Trial primary completion date: Oct 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    tenalisib (RP6530)
    10ms
    Efficacy and Safety of Tenalisib in Patients With Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=40, Recruiting, Rhizen Pharmaceuticals SA | Trial completion date: Mar 2025 --> Mar 2026 | Trial primary completion date: Oct 2024 --> Oct 2025
    Trial completion date • Trial primary completion date
    |
    tenalisib (RP6530)
    almost2years
    Efficacy and Safety of Tenalisib in Patients With Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=40, Recruiting, Rhizen Pharmaceuticals SA | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    tenalisib (RP6530)
    2years
    Efficacy and Safety of Tenalisib in Patients With Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Rhizen Pharmaceuticals SA
    New P2 trial • Metastases
    |
    tenalisib (RP6530)
    over2years
    Safety and efficacy of tenalisib in combination with romidepsin in patients with relapsed/refractory T-cell lymphoma: results from a phase I/II open-label multicenter study. (PubMed, Haematologica)
    Coadministration of tenalisib and romidepsin did not significantly alter the pharmacokinetics of romidepsin. Overall, tenalisib and romidepsin combination demonstrated a favorable safety and efficacy profile supporting its further development for relapsed/refractory TCL.
    Clinical • P1/2 data • Journal • Combination therapy
    |
    Istodax (romidepsin) • tenalisib (RP6530)
    over2years
    Compassionate Use Study of Tenalisib (RP6530) (clinicaltrials.gov)
    P1/2, N=17, Completed, Rhizen Pharmaceuticals SA | Trial primary completion date: Mar 2022 --> Mar 2023
    Trial primary completion date
    |
    tenalisib (RP6530)
    over2years
    Efficacy and Safety of Tenalisib (RP6530), a PI3K δ/γ and SIK3 Inhibitor, in Patients With Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=40, Completed, Rhizen Pharmaceuticals SA | Active, not recruiting --> Completed | Trial completion date: Dec 2022 --> Mar 2023 | Trial primary completion date: Dec 2022 --> Mar 2023
    Trial completion • Trial completion date • Trial primary completion date • Metastases
    |
    tenalisib (RP6530)
    over3years
    Study to Evaluate the Efficacy and Safety of Tenalisib, Given With CHOP Therapy for Front Line Treatment in Patients With PTCL (clinicaltrials.gov)
    P2, N=0, Withdrawn, Rhizen Pharmaceuticals SA | N=40 --> 0 | Not yet recruiting --> Withdrawn
    Enrollment change • Trial withdrawal
    |
    ALK (Anaplastic lymphoma kinase) • TNFRSF8 (TNF Receptor Superfamily Member 8)
    |
    ALK positive
    |
    doxorubicin hydrochloride • cyclophosphamide • vincristine • prednisone • tenalisib (RP6530)
    over3years
    Study to Evaluate the Efficacy and Safety of Tenalisib, Given With CHOP Therapy for Front Line Treatment in Patients With PTCL (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Rhizen Pharmaceuticals SA | Initiation date: May 2022 --> Jan 2023
    Trial initiation date
    |
    ALK (Anaplastic lymphoma kinase) • TNFRSF8 (TNF Receptor Superfamily Member 8)
    |
    ALK positive
    |
    doxorubicin hydrochloride • cyclophosphamide • vincristine • prednisone • tenalisib (RP6530)
    almost4years
    Study to Evaluate the Efficacy and Safety of Tenalisib, Given With CHOP Therapy for Front Line Treatment in Patients With PTCL (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Rhizen Pharmaceuticals SA
    New P2 trial
    |
    ALK (Anaplastic lymphoma kinase) • TNFRSF8 (TNF Receptor Superfamily Member 8)
    |
    ALK positive
    |
    doxorubicin hydrochloride • cyclophosphamide • vincristine • prednisone • tenalisib (RP6530)
    over5years
    Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma. (PubMed, Cancers (Basel))
    With an acceptable safety and promising clinical activity, Tenalisib can be a potential therapeutic option for relapsed/refractory TCL. Currently, a phase I/II combination study with romidepsin is ongoing.
    Clinical • P1 data • Journal
    |
    TNFRSF8 (TNF Receptor Superfamily Member 8)
    |
    Istodax (romidepsin) • tenalisib (RP6530)