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tenalisib

a dual PI3Kdelta and gamma inhibitor

Also Known As:

3-(3-fluorophenyl)-2-((1S)-1-(7H-purin-6-ylamino)propyl)chromen-4-one; RP6530

Networked: 4 relevant articles (2 outcomes, 4 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyrans: 130
    - Benzopyrans: 195
      - tenalisib: 4
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Purines: 651
      - tenalisib: 4
    - Benzopyrans: 195
      - tenalisib: 4

Experts

1.	Vakkalanka, Swaroop: 3 articles (08/2020 - 01/2019)
2.	Viswanadha, Srikant: 3 articles (08/2020 - 01/2019)
3.	Barde, Prajak J: 2 articles (08/2020 - 01/2020)
4.	Nair, Ajit: 2 articles (08/2020 - 01/2020)
5.	Carlo-Stella, Carmelo: 2 articles (01/2020 - 01/2019)
6.	Locatelli, Silvia L: 2 articles (01/2020 - 01/2019)
7.	Devata, Sumana: 1 article (08/2020)
8.	Haverkos, Bradley M: 1 article (08/2020)
9.	Huen, Auris: 1 article (08/2020)
10.	Iyer, Swaminathan P: 1 article (08/2020)

Related Diseases

1.	T-Cell Lymphoma (Lymphoma, T Cell) 07/13/2023 - "Tenalisib, a selective phosphoinositide-3-kinase δ/γ, and salt-inducible-kinase-3 inhibitor has shown efficacy and was well-tolerated in patients with T-cell lymphoma (TCL). " 07/13/2023 - "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." 08/15/2020 - "Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma."
2.	Hematologic Neoplasms (Hematological Malignancy) 01/01/2020 - "This was a phase I, open-label, 3 + 3 dose escalation, maximum tolerated dose determination study to evaluate the safety, pharmacokinetics, and efficacy of tenalisib in patients with relapsed/refractory hematologic malignancies. " 01/01/2020 - "A First-in-human Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor, in Patients With Relapsed/Refractory Hematologic Malignancies: Results From the European Study."
3.	Neoplasms (Cancer) 01/01/2019 - "Furthermore, we show in human tumor xenografts that RP6530 repolarizes TAMs into proinflammatory macrophages and inhibits tumor vasculature, leading to tumor regression. " 01/01/2019 - "Targeting Cancer Cells and Tumor Microenvironment in Preclinical and Clinical Models of Hodgkin Lymphoma Using the Dual PI3Kδ/γ Inhibitor RP6530." 07/13/2023 - "In vitro studies suggest a synergistic anti-tumor potential for the combination of tenalisib with the histone-deacetylase inhibitor, romidepsin. "
4.	Cutaneous T-Cell Lymphoma (Lymphoma, T Cell, Cutaneous) 08/15/2020 - "Tenalisib (RP6530), a dual phosphoinositide 3-kinase δ/γ inhibitor was evaluated in a phase I/Ib study for maximum tolerated dose (MTD), pharmacokinetics, and efficacy in patients with relapsed/refractory peripheral and cutaneous T-Cell Lymphoma (TCL). "
5.	Hodgkin Disease (Hodgkin's Disease) 01/01/2019 - "Hodgkin lymphoma cell lines (L-540, KM-H2, and L-428) and primary human macrophages were used to investigate the activity of RP6530 in vitro and in vivo in Hodgkin lymphoma cell line xenografts. " 01/01/2019 - "Targeting Cancer Cells and Tumor Microenvironment in Preclinical and Clinical Models of Hodgkin Lymphoma Using the Dual PI3Kδ/γ Inhibitor RP6530." 01/01/2019 - "Interestingly, patients with Hodgkin lymphoma experiencing objective responses (complete response and partial response) in a phase I trial using RP6530 showed a significant inhibition of circulating myeloid-derived suppressor cells and an average mean reduction in serum thymus and activation-regulated chemokine levels of 40% (range, 4%-76%). " 01/01/2019 - "In vitro, RP6530 besides killing and inhibiting the proliferation of Hodgkin lymphoma cells, downregulated lactic acid metabolism, switching the activation of macrophages from an immunosuppressive M2-like phenotype to a more inflammatory M1-like state. "

Related Drugs and Biologics

1.	romidepsin (FK228)
2.	tenalisib
3.	Histone Deacetylase Inhibitors
4.	Chemokine CCL17
5.	Phosphatidylinositols (Phosphatidylinositol)
6.	Lactic Acid (Lactate)
7.	Aspartate Aminotransferases (Aspartate Transaminase)
8.	Alanine Transaminase (SGPT)