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DRUG CLASS:

PI3Kγ inhibitor

3d
Can Duvelisib and Eganelisib work for both cancer and COVID-19? Molecular-level insights from MD simulations and enhanced samplings. (PubMed, Phys Chem Chem Phys)
Finally, analyses implied Duvelisib and Eganelisib as promising dual-purposed anti-COVID and anticancer drugs, potentially targeting Mpro and PI3Kγ to stop virus replication and cytokine storms concomitantly. We also distinguished hotspot residues imparting significant interactions.
Journal
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PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
Copiktra (duvelisib) • eganelisib (IPI-549)
6d
The cell death-related genes machine learning model for precise therapy and clinical drug selection in hepatocellular carcinoma. (PubMed, J Cell Mol Med)
Moreover, our investigation has shown that AZD2014, SB505124, LJI308 and OSI-207 show a greater efficacy in patients in the low-risk category. Conversely, for the high-risk group patients, PD173074, ZM447439 and CZC24832 exhibit a stronger response...This innovative model provides a novel approach for forecasting prognosis and assessing drug sensitivity in HCC patients, driving a more personalized and efficacious treatment paradigm, elevating clinical outcomes. Nonetheless, additional research endeavours are required to confirm the model's precision and assess its potential to inform clinical decision-making for HCC patients.
Journal • Tumor mutational burden • Machine learning
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TMB (Tumor Mutational Burden)
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TMB-L
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vistusertib (AZD2014) • CZC24832 • ZM 447439
16d
Duvelisib Following Chimeric Antigen Receptor T-Cell Therapy (clinicaltrials.gov)
P1, N=43, Recruiting, Washington University School of Medicine | Trial completion date: Oct 2029 --> May 2030 | Trial primary completion date: May 2025 --> Dec 2025
Trial completion date • Trial primary completion date • CAR T-Cell Therapy
|
Copiktra (duvelisib)
23d
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)
1m
BR-101801-CT-101: BR101801 in Adult Patients With Advanced Hematologic Malignancies( Phase I) (clinicaltrials.gov)
P1, N=30, Active, not recruiting, Boryung Pharmaceutical Co., Ltd | Recruiting --> Active, not recruiting
Enrollment closed
|
BR101801
1m
Intermittent Duvelisib Dosing in Treating Patients With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma (clinicaltrials.gov)
P2, N=15, Active, not recruiting, City of Hope Medical Center | Trial completion date: Dec 2023 --> Jun 2024 | Trial primary completion date: Dec 2023 --> Jun 2024
Trial completion date • Trial primary completion date
|
BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • FCER2 (Fc Fragment Of IgE Receptor II)
|
Chr t(11;14) • CCND1 overexpression
|
Copiktra (duvelisib) • ETP-47187
1m
Design, synthesis, molecular modelling and biological evaluation of novel 6-amino-5-cyano-2-thiopyrimidine derivatives as potent anticancer agents against leukemia and apoptotic inducers. (PubMed, J Enzyme Inhib Med Chem)
Molecular analysis of Duvelisib and compound 1c in PI3K was performed. Finally, these results suggest that 2-thiopyrimidine derivative 1c might serve as a model for designing novel anticancer drugs in the future.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CASP3 (Caspase 3)
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Copiktra (duvelisib)
2ms
Trial completion
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Copiktra (duvelisib)
2ms
KLRG1 Cell Depletion As A Novel Therapeutic Strategy In Patients With Mature T-cell lymphoma Subtypes. (PubMed, Clin Cancer Res)
Our findings suggest the potential benefit of a broader treatment strategy combining therapeutic antibodies with PI3Ki for the treatment of patients with mature T-cell and NK-cell neoplasms.
Journal
|
CD8 (cluster of differentiation 8) • NCAM1 (Neural cell adhesion molecule 1) • KLRG1 (Killer Cell Lectin Like Receptor G1) • B3GAT1 (Beta-1,3-Glucuronyltransferase 1)
|
KLRG1 expression
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Copiktra (duvelisib)
3ms
BR101801 enhances the radiosensitivity of p53-deficient colorectal cancer cells by inducing G2/M arrest, apoptosis, and senescence in a p53-independent manner. (PubMed, Am J Cancer Res)
Moreover, BR101801 exerted robust synergistic effects on IR-induced cell cycle arrest, apoptosis, and tumor growth inhibition, even in radioresistant HCT116 p53 cells. Overall, these findings provide a scientific rationale for combining BR101801 with IR as a new therapeutic strategy to overcome radioresistance induced by p53 deficiency.
Journal
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PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
BR101801
3ms
Therapeutic potential of anti-PIK3CG treatment for multiple myeloma via inhibiting c-Myc pathway. (PubMed, Heliyon)
The combination of PIK3CG inhibitor and the chemotherapy Melphalan could effectively inhibit the proliferation and migration of MM cells, promote the cell apoptosis, and decrease the ratio of Bcl-2/Bax and the expression of vimentin. The expression of proto-oncogene c-Myc was decreased and the sensitivity of cells to chemotherapeutic drugs was enhanced. Collectively, PIK3CG regulates growth of MM via c-Myc pathway, thus emerging as a promising molecular targeted therapy.
Journal • IO biomarker
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • BAX (BCL2-associated X protein) • VIM (Vimentin)
|
MYC expression • BAX expression • VIM expression
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melphalan
3ms
New P2 trial • Metastases
|
tenalisib (RP6530)
3ms
PRIMO: A Study of Duvelisib in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (PTCL) (clinicaltrials.gov)
P2, N=160, Active, not recruiting, SecuraBio | N=120 --> 160 | Trial primary completion date: Oct 2023 --> Dec 2023
Enrollment change • Trial primary completion date
|
Copiktra (duvelisib)
4ms
Duvelisib Plus Docetaxel In Recurrent/Metastatic HNSCC (clinicaltrials.gov)
P2, N=26, Active, not recruiting, Glenn J. Hanna | Recruiting --> Active, not recruiting | Trial completion date: Jan 2024 --> Jan 2025
Enrollment closed • Trial completion date • Metastases
|
PD-L1 (Programmed death ligand 1)
|
PD-L1 expression
|
docetaxel • Copiktra (duvelisib)
4ms
Phase II Trial of Duvelisib Maintenance after Autologous Stem Cell Transplant in T-Cell and B-Cell Non-Hodgkin Lymphomas: Results of Safety Lead in (ASH 2023)
ConclusionsDuvelisib maintenance for up to one year after consolidative autoSCT in patients with TCL or B-NHL is safe and well tolerated at a dose schedule of 25 mg twice daily for 14 days on/ 14 days off, of 28-day cycles. Enrollment of patients undergoing consolidative autoSCT for TCL is ongoing to evaluate the efficacy of duvelisib maintenance.
Clinical • P2 data
|
PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
Copiktra (duvelisib)
4ms
A Phase II Study of Intermittent Duvelisib Dosing in Patients with Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) (ASH 2023)
Adverse events in general were manageable and mainly related to gastrointestinal and liver toxicity, and patient died during treatment from complications from COVID-19 pneumonia. After an initial 12 weeks of continuous duvelisib treatment, the incorporation of intermittent dosing appears to be a viable option for patients with previously treated CLL/SLL.
Clinical • P2 data
|
TP53 (Tumor protein P53) • IGH (Immunoglobulin Heavy Locus) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
Chr del(11q)
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Copiktra (duvelisib)
4ms
XPO1 Inhibitor Triggers Autophagy of TP53-Mutated Burkitt's Lymphoma Cells (ASH 2023)
To confirm whether KPT330 effects the generation or degradation of LC3B-II, we used the late autophagy inhibitor chloroquine (CQ) to cells and observed the p62 protein level reduced and LC3B-II protein level increased with additional use of CQ compared with only KPT330 treatment ( Fig1, d). However, none synergistic effect was observed according to KPT330 combined with Cytarabine, Doxorubicin, Azacitidine, Decitabine, Rapamycin, Bortezomib, Duvelisib or Venetoclax, respectively ( Fig2, d). CONCLUSIONXPO1 Inhibitor, KPT330 can restrict nuclear export of autophagy-related proteins thus regulate autophagy and stabilize p53 function in TP53-mutated Burkitt's lymphoma cells, which revealed a promising treatment.
IO biomarker
|
SQSTM1 (Sequestosome 1) • CTSD (Cathepsin D) • TFEB (Transcription Factor EB 2)
|
TP53 mutation • MYC rearrangement
|
Venclexta (venetoclax) • cytarabine • bortezomib • doxorubicin hydrochloride • azacitidine • Xpovio (selinexor) • decitabine • Copiktra (duvelisib) • sirolimus
5ms
Defining a Targetable Leukemia Intrinsic Dependency on Noncanonical PI3Kgamma Signaling (ASH 2023)
We conclude that inflammatory signaling-activated PIK3R5 is a biomarker for sensitivity to PI3Kγ inhibition via an unappreciated PI3Kγ-PAK1 axis. Synergy with cytarabine unmasked eganelisib sensitivity in additional leukemias, expanding the therapeutic potential of targeting PI3Kγ.
IO biomarker
|
PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • SPI1 (Spi-1 Proto-Oncogene)
|
cytarabine • eganelisib (IPI-549)
5ms
Mechanistic Studies of Cytokine Release Syndrome (CRS) with Roles of Interferon-Gamma (IFN-g) and Tumor Necrosis Factor Alpha (TNF-α) While Maintaining CAR-T Function in Vitro (ASH 2023)
In contrast to dasatinib which completely blocked both CRS and CART killilng (data not shown), no significant attenuation of CAR-T killing efficacy was found with any of these kinase inhibitors or the neutralizing antibodies...CRS (in vitro production of IL-6) was dependent on the presence of GM-CSF/IL-4 "primed" iDC and abolished by duvelisib while maintaining blinatumomab-induced Ramos killing (Fig 2)...Marked increase in secreted mouse IL-6 was observed which was completely inhibited by duvelisib, ruxolitinib, anti-IFNγ and anti-TNFα... We have developed in vitro CRS co-culture models using cells from both man and mouse and tested the role of multiple effector cell types including CART cells, CARMLNK cells, and CAR-iNK cells and multiple inhibitors on CRS and CART function in vitro. We show that JAK1/2 and PI3Kg/d kinase inhibitors as well as neutralizing antibodies to IFNγ and TNFα all block in vitro CRS without attenuating the anti-tumor efficacy of CAR-T cells. Our result suggests IFNγ, TNFα, JAK1/2 and PI3Kg/d kinases inhibitors are rational targets for CRS mitigation approaches without compromising CART-mediated anti-tumor efficacy in the clinic.
Preclinical • IO biomarker
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IFNG (Interferon, gamma) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL10 (Interleukin 10) • CSF2 (Colony stimulating factor 2) • IL4 (Interleukin 4)
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dasatinib • Jakafi (ruxolitinib) • Blincyto (blinatumomab) • Copiktra (duvelisib)
5ms
A Novel PI3K γ/δ and DNA-PK Triple Inhibitor, BR101801, for r/r PTCL: A Phase 1a/b, Multi-Center, Open-Label Clinical Trial (ASH 2023)
Preliminary results showed the ORR of 31.6% and a CR rate of 21.1%. Phase 2 study is warranted further investigate the safety and efficacy of BR101801 in r/r PTCL and Nodal TFH cell lymphoma at 200 mg QD orally.
Clinical • P1 data
|
MYC (V-myc avian myelocytomatosis viral oncogene homolog) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
BR101801
5ms
Clinical • P2 data
|
TNFRSF8 (TNF Receptor Superfamily Member 8)
|
TNFRSF8 negative
|
Copiktra (duvelisib) • Onureg (azacitidine oral)
5ms
PRIMO: A Study of Duvelisib in Patients With Relapsed or Refractory Peripheral T Cell Lymphoma (PTCL) (clinicaltrials.gov)
P2, N=120, Active, not recruiting, SecuraBio | Trial completion date: Sep 2023 --> Dec 2024
Trial completion date
|
Copiktra (duvelisib)
5ms
Duvelisib in Combination With CC-486 in Lymphoid Malignancy (clinicaltrials.gov)
P1, N=30, Recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial completion date: Sep 2024 --> Oct 2025 | Trial primary completion date: Sep 2024 --> Oct 2025
Trial completion date • Trial primary completion date • Combination therapy
|
ALK (Anaplastic lymphoma kinase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2) • CD8 (cluster of differentiation 8) • TNFRSF8 (TNF Receptor Superfamily Member 8) • BCL6 (B-cell CLL/lymphoma 6)
|
BCL6 rearrangement • BCL2 rearrangement
|
Copiktra (duvelisib) • Onureg (azacitidine oral)
6ms
Duvelisib and Nivolumab for the Treatment of Stage IIB-IVB Mycosis Fungoides and Sezary Syndrome (clinicaltrials.gov)
P1, N=29, Recruiting, National Cancer Institute (NCI) | Suspended --> Recruiting
Enrollment open
|
Opdivo (nivolumab) • Copiktra (duvelisib) • ABP 206 (nivolumab biosimilar) • ETP-47187
6ms
FGFR3 alterations in bladder cancer stimulate serine synthesis to induce immune-inert macrophages that suppress T-cell recruitment and activation. (PubMed, Cancer Res)
Targeting PI3K in aFGFR3 tumors with duvelisib achieved promising efficacy by reversing the macrophage phenotype, and combination therapy with duvelisib and erdafitinib demonstrated increased antitumor activity. Overall, these findings reveal the critical role of enhanced serine synthesis efflux from cancer cells with mutant FGFR3 in shifting macrophages to an immune-inert phenotype. Reversing the macrophage phenotype holds promise for enhancing erdafitinib efficacy.
Journal
|
FGFR3 (Fibroblast growth factor receptor 3)
|
FGFR3 mutation
|
Balversa (erdafitinib) • Copiktra (duvelisib)
6ms
Polymorphonuclear myeloid-derived suppressor cells and phosphatidylinositol-3 kinase gamma are critical to tobacco-mimicking oral carcinogenesis in mice. (PubMed, J Immunother Cancer)
Overall, our data suggest that recruitment of PMN-MDSCs to sites of dysplasia is critical to immune suppression of CD8 T cells, thereby permitting malignancy, and PI3Kγ inhibitors are one mechanism to reduce PMN-MDSC recruitment, immunosuppression and tumorigenesis in OSCC.
Preclinical • Journal
|
CD8 (cluster of differentiation 8) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
6ms
Duvelisib Plus Docetaxel In Recurrent/Metastatic HNSCC (clinicaltrials.gov)
P2, N=26, Recruiting, Glenn J. Hanna | Trial primary completion date: Sep 2023 --> Dec 2023
Trial primary completion date • Metastases
|
PD-L1 (Programmed death ligand 1)
|
PD-L1 expression
|
docetaxel • Copiktra (duvelisib)
7ms
Preclinical • Journal
|
PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta)
|
Copiktra (duvelisib)
7ms
Size-tunable Nanoregulator-Based Radiofrequency Ablation Suppresses MDSCs And Their Compensatory Immune Evasion in Hepatocellular Carcinoma. (PubMed, Adv Healthc Mater)
To address this issue, a novel size-tunable hybrid nano-micro-liposome was designed to co-deliver MDSCs inhibitor (IPI549) and αPD-L1 antibody (LPIP) for multi-pathway activation of immune responses...The combined strategy of LPIP+iRFA effectively ablated the primary tumor by activating immune responses in the transition zone while suppressing the compensatory immune evasion of surviving MDSCs. This approach avoided the relapse of the residual tumor in a post-iRFA incomplete-ablation model and appears to be a promising strategy in RFA for eradication of HCC.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 expression
|
eganelisib (IPI-549)
8ms
A Phase II study of intermittent duvelisib dosing in patients with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) (IWCLL 2023)
We report the results of an open-label, phase 2 study utilizing a continuous dosing induction phase followed by an intermittent dosing maintenance phase of the PI3K inhibitor duvelisib in patients with relapsed/refractory CLL/ SLL. Patients who received duvelisib on an intermittent schedule achieved some clinical benefit, however, the desired 12-month PFS goal of 50% was not reached. Adverse events in general were manageable and mainly related to gastrointestinal and liver toxicity, and patient died during treatment from complications from COVID-19 pneumonia.
Clinical • P2 data
|
TP53 (Tumor protein P53) • IGH (Immunoglobulin Heavy Locus) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
Chr del(11q)
|
Copiktra (duvelisib)
8ms
MARIO-3: Evaluation of IPI-549 Combined With Front-line Treatments in Pts. With Triple-Negative Breast Cancer or Renal Cell Carcinoma (clinicaltrials.gov)
P2, N=91, Active, not recruiting, Infinity Pharmaceuticals, Inc. | Trial completion date: Aug 2022 --> Aug 2023 | Trial primary completion date: Aug 2022 --> Aug 2023
Trial completion date • Trial primary completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
PD-L1 expression • HER-2 negative
|
Avastin (bevacizumab) • Tecentriq (atezolizumab) • albumin-bound paclitaxel • eganelisib (IPI-549)
8ms
A Study of Ruxolitinib and Duvelisib in People With Lymphoma (clinicaltrials.gov)
P1, N=52, Recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Aug 2024 --> Aug 2025 | Trial primary completion date: Aug 2024 --> Aug 2025
Trial completion date • Trial primary completion date
|
CD8 (cluster of differentiation 8)
|
CD8 positive
|
Jakafi (ruxolitinib) • Copiktra (duvelisib)
8ms
Duvelisib and Venetoclax in Relapsed or Refractory CLL or SLL or RS (clinicaltrials.gov)
P1/2, N=67, Recruiting, Dana-Farber Cancer Institute | Trial completion date: Jul 2025 --> Jul 2026 | Trial primary completion date: Jul 2023 --> Jul 2024
Trial completion date • Trial primary completion date
|
BCL2 (B-cell CLL/lymphoma 2)
|
Venclexta (venetoclax) • Copiktra (duvelisib)
9ms
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)
9ms
Targeting CCR7-PI3Kγ overcomes resistance to tyrosine kinase inhibitors in ALK-rearranged lymphoma. (PubMed, Sci Transl Med)
The PI3Kγ/δ inhibitor duvelisib potentiated crizotinib activity against ALCL lines and patient-derived xenografts. Furthermore, genetic deletion of CCR7 blocked the central nervous system dissemination and perivascular growth of ALCL in mice treated with crizotinib. Thus, blockade of PI3Kγ or CCR7 signaling together with ALK TKI treatment reduces primary resistance and the survival of persister lymphoma cells in ALCL.
Journal
|
ALK (Anaplastic lymphoma kinase) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CCL19 (C-C Motif Chemokine Ligand 19) • CCR7 (Chemokine (C-C motif) receptor 7) • CCL21 (C-C Motif Chemokine Ligand 21)
|
ALK rearrangement
|
Xalkori (crizotinib) • Copiktra (duvelisib)
9ms
New trial • Real-world evidence • Real-world
|
Copiktra (duvelisib)
9ms
Preclinical • Journal
|
PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C) • PRKDC (Protein Kinase, DNA-Activated, Catalytic Subunit) • IL2RG (Interleukin 2 Receptor Subunit Gamma)
|
PIK3CG expression
|
Copiktra (duvelisib)
9ms
Duvelisib and Nivolumab in Treating Patients With Richter Syndrome or Transformed Follicular Lymphoma (clinicaltrials.gov)
P1, N=7, Active, not recruiting, David Bond, MD | Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: Dec 2022 --> Dec 2023
Trial completion date • Trial primary completion date • Combination therapy
|
Opdivo (nivolumab) • Copiktra (duvelisib) • ETP-47187
10ms
Eganelisib, a First-in-Class PI3K-γ Inhibitor, in Patients with Advanced Solid Tumors: Results of the Phase 1/1b MARIO-1 Trial. (PubMed, Clin Cancer Res)
Based on the observed safety profile, eganelisib doses of 30 mg and 40 mg once daily in combination with PD-1/PD-L1 inhibitors were chosen for phase 2 study.
P1 data • Journal • Metastases
|
PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
Opdivo (nivolumab) • eganelisib (IPI-549)
10ms
A Phase 2 Study Comparing 2 Intermittent Dosing Schedules of Duvelisib in Subjects With Indolent Non-Hodgkin Lymphoma. (TEMPO) (clinicaltrials.gov)
P2, N=102, Active, not recruiting, SecuraBio | Trial completion date: May 2023 --> Aug 2023 | Trial primary completion date: May 2023 --> Aug 2023
Trial completion date • Trial primary completion date
|
Copiktra (duvelisib)
10ms
Dual inhibition of phosphoinositide 3-kinases delta and gamma reduces chronic B cell activation and autoantibody production in a mouse model of lupus. (PubMed, Front Immunol)
Targeting of PI3Kδ using FDA-approved drugs Idelalisib or Umbralisib has shown efficacy in treatment of multiple B cell malignancies. Duvelisib, an inhibitor targeting both PI3Kδ and PI3Kγ (PI3Kδγi) has also been used for treatment of several leukemias and lymphomas and was suggested to offer potential additional benefits in supressing T cell and inflammatory responses...Kidney pathology was also impacted, with reduced IgG deposition and glomerulonephritis. These results indicate that dual inhibition of PI3Kδ and PI3Kγ can target autoreactive B cells and may have therapeutic benefits in autoantibody-mediated disease.
Preclinical • Journal
|
PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CD86 (CD86 Molecule)
|
Zydelig (idelalisib) • Copiktra (duvelisib) • Ukoniq (umbralisib)