Recent Publications

Umbralisib

1.  543: Umbralisib Plus Ublituximab (U2) Is Superior to Obinutuzumab Plus Chlorambucil (O+Chl) in Patients with Treatment Naïve (TN) and Relapsed/Refractory (R/R) Chronic Lymphocytic Leukemia (CLL): Results from the Phase 3 Unity-CLL Study. (ASH 2020)
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2.  2934: Umbralisib, the Once Daily Dual Inhibitor of PI3Kδ and Casein Kinase-1ε Demonstrates Clinical Activity in Patients with Relapsed or Refractory Indolent Non-Hodgkin Lymphoma: Results from the Phase 2 Global Unity-NHL Trial. (ASH 2020)
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3.  Umbralisib, a Novel PI3Kδ and Casein Kinase-1ε Inhibitor, in Relapsed or Refractory Chronic Lymphocytic Leukemia and Lymphoma: An Open-label, Phase 1, Dose-escalation, First-in-human Study.
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Tenalisib

1.  1155: A Multi-Center, Open Label, Phase I/II Study to Assess the Safety and Efficacy of Tenalisib Given in Combination with Romidepsin in Patients with Relapsed/Refractory T-Cell Lymphoma. (ASH 2020)Visit Link
2.  Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma.Visit Link | Download
3.  Therapeutic potential of Tenalisib, a PI3K delta/gamma plus SIK-3 inhibitor, in hematological malignancies (EHA 2020)    Download
4.  Targeting cancer cells and tumor 1 microenvironment in preclinical and clinical models of
   Hodgkin lymphoma using the dual PI3Kδ/γ inhibitor RP6530.
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RP 7214 – DHODH Inhibitor

1.  RP7214, a small molecule inhibitor of dihydroorotate dehydrogenase (DHODH), potentiates activity of Gilteritinib and Cytarabine in preclinical models of AML. (AACR 2019)
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2.  Inhibition of Dihydroorotate Dehydrogenase (DHODH) by RP7214 attenuates growth and promotes differentiation of AML cell lines. (AACR 2019)
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Glutaminase Inhibitor

1.  Addition of RP10107, a novel and potent glutaminase inhibitor, accentuates 5-FU activity in lung cancer cell lines in vitro. (AACR 2018)
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2.  Synergistic effects of glutaminase and proteasome inhibition in Multiple Myeloma cell lines. (AACR 2018)
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3.  Anti-oncogenic effects of RP10107, a novel and potent glutaminase inhibitor, in cancer cell lines. (AACR 2015)
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C-Met Inhibitor

1.  Selective Targeting of Met-Kinase by RP1400 Attenuates Tumor Progression in Mouse Models of Gastric Cancer, Glioblastoma,  and Hepatocellular Carcinoma.
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2.  Preclinical profile of novel and potent c-Met Kinase inhibitors. (AACR 2012)
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RP 3128 – SOCE/CRAC Inhibitor

1.  Pharmacodynamic evaluation of RP3128, a novel and potent CRAC channel inhibitor in guinea pig models of allergic asthma.   Visit Link | Download

RP 4010 – SOCE/CRAC Inhibitor

1.  Calcium Release-Activated Calcium (CRAC) Channel Inhibition Suppresses Pancreatic Ductal Adenocarcinoma Cell Proliferation and Patient-Derived Tumor Growth.
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2.  Targeting Orai1-mediated store-operated calcium entry by RP4010 for antitumor activity in esophagus squamous cell carcinoma.
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3.  The Novel Calcium Release-Activated Calcium (CRAC) Channel Inhibitor RP4010 Exerts Potent Antitumor
   Effects in NOD/SCID/IL2Rg-/- Mice with Diffuse Large B Cell Lymphoma (DLBCL) Cell Line Xenografts.
   (ASH 2017)
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RV 1001

1.  Phase I/II evaluation of RV1001, a novel PI3Kδ inhibitor, in spontaneous canine lymphoma.
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