Therapy Detail

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Therapy Name Tenalisib
Synonyms
Therapy Description

Tenalisib (RP6530) is an inhibitor of PIK3CG and PIK3CD, which blocks PI3K/AKT signaling to prevent cell proliferation and also may modulate the tumor microenvironment and induce macrophage phenotype conversion from M2 to M1 (PMID: 30352904).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Tenalisib RP6530 PIK3CD inhibitor 24 PIK3CG inhibitor 8 Tenalisib (RP6530) is an inhibitor of PIK3CG and PIK3CD, which blocks PI3K/AKT signaling to prevent cell proliferation and also may modulate the tumor microenvironment and induce macrophage phenotype conversion from M2 to M1 (PMID: 30352904, PMID: 31761713, PMID: 32824175).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown cutaneous T cell lymphoma not applicable Tenalisib Phase I Actionable In a Phase I trial, Tenalisib (RP6530) demonstrated safety in patients with relapsed or refractory cutaneous T-cell lymphoma, and resulted in an overall response rate of 45% (9/20), including nine partial responses with a median duration of response of 3.8 months, and a further nine patients achieved stable disease (PMID: 32824175; NCT02567656). 32824175
Unknown unknown peripheral T-cell lymphoma not applicable Tenalisib Phase I Actionable In a Phase I trial, Tenalisib (RP6530) demonstrated safety in patients with relapsed or refractory peripheral T-cell lymphoma, and resulted in an overall response rate of 46.7% (7/15), including three complete responses and four partial responses with a median duration of response of 6.5 months, and a further two patients achieved stable disease (PMID: 32824175; NCT02567656). 32824175
Unknown unknown hematologic cancer not applicable Tenalisib Phase I Actionable In a Phase I trial, Tenalisib (RP6530) treatment in patients with relapsed/refractory hematologic malignancies resulted in an overall response rate of 19% (6/35), including two complete responses and six partial responses, a disease control rate of 61% (19/35), with 13 patients achieving stable disease, and a 5.7 month duration of response (PMID: 31761713). 31761713
Unknown unknown Hodgkin's lymphoma not applicable Tenalisib Preclinical - Cell line xenograft Actionable In a preclinical study, Tenalisib (RP6530) decreased phosphorylation of ERK and AKT, reduced proliferation, and increased cell-cycle arrest and apoptosis in Hodgkin's lymphoma cell lines in culture, and decreased tumor-associated macrophages, reduced VEGF expression, increased tumor endothelial cell apoptosis, and reduced tumor growth in xenograft models (PMID: 30352904). 30352904
Unknown unknown mature T-cell and NK-cell lymphoma not applicable Tenalisib Phase I Actionable In a Phase I trial, Tenalisib (RP6530) demonstrated safety in patients with relapsed or refractory peripheral and cutaneous T-cell lymphomas, and resulted in an overall response rate of 45.7% (16/35), including three complete responses and 13 partial responses with a median duration of response of 4.9 months, and a further 31% (11/35) patients achieved stable disease (PMID: 32824175; NCT02567656). 32824175

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Clinical Trial Phase Therapies Title Recruitment Status
NCT02567656 Phase I Tenalisib Safety and Efficacy Study of a Dual PI3K Delta/Gamma Inhibitor in T-cell Lymphoma Completed
NCT03711578 Phase II Tenalisib Efficacy and Safety Study of Tenalisib (RP6530), a Novel PI3K delta/gamma Dual Inhibitor in Patients With Relapsed/Refractory Indolent Non-Hodgkin's Lymphoma (iNHL) Active, not recruiting
NCT03711604 Phase Ib/II Tenalisib Compassionate Use Study of Tenalisib (RP6530) Enrolling by invitation


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