Michael Lahn
YOU?
Author Swipe
View article: Novel PI3kδ inhibitor roginolisib synergizes with venetoclax in hematologic malignancies
Novel PI3kδ inhibitor roginolisib synergizes with venetoclax in hematologic malignancies Open
The phosphoinositide 3-kinase (PI3K) pathway remains a potent drug target in hematological malignancies despite the challenges that have affected clinical drug development, particularly unpredictable toxicity, and inherent/acquired drug re…
View article: 41P Total tumor burden and radiomics to evaluate response in dose escalation studies: Roginolisib (IOA-244), a highly selective PI3Kδ inhibitor in metastatic uveal melanoma patients
41P Total tumor burden and radiomics to evaluate response in dose escalation studies: Roginolisib (IOA-244), a highly selective PI3Kδ inhibitor in metastatic uveal melanoma patients Open
View article: 164P Roginolisib (IOA-244), the first highly selective oral allosteric modulator of phosphoinositide 3-kinase inhibitor delta (PI3Kδ), has immuno-modulatory effects associated with clinical benefits in patients with metastatic uveal melanoma
164P Roginolisib (IOA-244), the first highly selective oral allosteric modulator of phosphoinositide 3-kinase inhibitor delta (PI3Kδ), has immuno-modulatory effects associated with clinical benefits in patients with metastatic uveal melanoma Open
View article: The highly selective and oral phosphoinositide 3-kinase delta (PI3K-δ) inhibitor roginolisib induces apoptosis in mesothelioma cells and increases immune effector cell composition
The highly selective and oral phosphoinositide 3-kinase delta (PI3K-δ) inhibitor roginolisib induces apoptosis in mesothelioma cells and increases immune effector cell composition Open
Targeting aberrantly expressed kinases in malignant pleural mesothelioma (MPM) is a promising therapeutic strategy. We here investigated the effect of the novel and highly selective Phosphoinositide 3-kinase delta (PI3K-δ) inhibitor rogino…
View article: Targeting T regulatory (T<sub>reg</sub>) cells in immunotherapy-resistant cancers
Targeting T regulatory (T<sub>reg</sub>) cells in immunotherapy-resistant cancers Open
Primary or secondary (i.e., acquired) resistance is a common occurrence in cancer patients and is often associated with high numbers of T regulatory (Treg) cells (CD4+CD25+FOXP3+). The approval of ipilimumab and the development of similar …
View article: Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma
Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma Open
The TGFβ receptor inhibitor galunisertib demonstrated efficacy in patients with pancreatic ductal adenocarcinoma (PDAC) in the randomized phase II H9H-MC-JBAJ study, which compared galunisertib plus the chemotherapeutic agent gemcitabine w…
View article: Supplementary Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma
Supplementary Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma Open
Figures S1-5, Tables S1-3
View article: Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma
Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma Open
The TGFβ receptor inhibitor galunisertib demonstrated efficacy in patients with pancreatic ductal adenocarcinoma (PDAC) in the randomized phase II H9H-MC-JBAJ study, which compared galunisertib plus the chemotherapeutic agent gemcitabine w…
View article: Supplementary Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma
Supplementary Data from Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma Open
Figures S1-5, Tables S1-3
View article: The future of targeting cytotoxic T-lymphocyte-associated protein-4: Is there a role?
The future of targeting cytotoxic T-lymphocyte-associated protein-4: Is there a role? Open
View article: 131P Safety and clinical efficacy of roginolisib (IOA-244): The first oral allosteric modulator of phosphoinositide 3-kinase inhibitor delta (PI3Kδ)
131P Safety and clinical efficacy of roginolisib (IOA-244): The first oral allosteric modulator of phosphoinositide 3-kinase inhibitor delta (PI3Kδ) Open
View article: 469 Combining a safe PI3Kd inhibitor with chemotherapy and anti-PD1 in immunotherapy-refractory NSCLC: a proof-of-concept study to allow clinical trial design
469 Combining a safe PI3Kd inhibitor with chemotherapy and anti-PD1 in immunotherapy-refractory NSCLC: a proof-of-concept study to allow clinical trial design Open
Background Roginolisib (IOA-244) is a first in class allosteric modulator and non-ATP competitive PI3Kd inhibitor currently in a Phase 1 clinical study. In preclinical studies, roginolisib inhibits suppressive immune cells, such as Tregs a…
View article: Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma
Autotaxin Secretion Is a Stromal Mechanism of Adaptive Resistance to TGFβ Inhibition in Pancreatic Ductal Adenocarcinoma Open
The TGFβ receptor inhibitor galunisertib demonstrated efficacy in patients with pancreatic ductal adenocarcinoma (PDAC) in the randomized phase II H9H-MC-JBAJ study, which compared galunisertib plus the chemotherapeutic agent gemcitabine w…
View article: Non-Clinical Toxicology Evaluation of the Novel Non-ATP Competitive Oral PI3 Kinase Delta Inhibitor Roginolisib
Non-Clinical Toxicology Evaluation of the Novel Non-ATP Competitive Oral PI3 Kinase Delta Inhibitor Roginolisib Open
Roginolisib (IOA-244) is a novel, non-ATP competitive phosphoinositide-3-kinase (PI3K) delta inhibitor that regulates Akt/mTOR signaling. Roginolisib was administered once daily to rats and dogs in dose-range finding (DRF) and 4-week GLP t…
View article: Correction: Autotaxin inhibitor IOA-289 reduces gastrointestinal cancer progression in preclinical models
Correction: Autotaxin inhibitor IOA-289 reduces gastrointestinal cancer progression in preclinical models Open
View article: Autotaxin inhibitor IOA-289 reduces gastrointestinal cancer progression in preclinical models
Autotaxin inhibitor IOA-289 reduces gastrointestinal cancer progression in preclinical models Open
Background Autotaxin (ATX) is a secreted enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA). LPA stimulates cell proliferation and migration and promotes wound repair following tissue damage. ATX levels are directl…
View article: P1114: HIGHLY SELECTIVE ALLOSTERIC MODULATOR OF THE PHOSPHOINOSITIDE 3-KINASE DELTA (PI3KΔ) ROGINOLISIB (IOA-244) IN A DOSE ESCALATION STUDY OF PATIENTS WITH REFRACTORY/RELAPSED FOLLICULAR LYMPHOMA (FL)
P1114: HIGHLY SELECTIVE ALLOSTERIC MODULATOR OF THE PHOSPHOINOSITIDE 3-KINASE DELTA (PI3KΔ) ROGINOLISIB (IOA-244) IN A DOSE ESCALATION STUDY OF PATIENTS WITH REFRACTORY/RELAPSED FOLLICULAR LYMPHOMA (FL) Open
Topic: 18. Indolent and mantle-cell non-Hodgkin lymphoma - Clinical Background: Roginolisib has shown a favourable toxicity and ADME profile in over 30 patients (pts) with solid tumours. Using the recommended phase 2 dose (RP2D) establishe…
View article: Highly Selective Allosteric Modulator of the Phosphoinositide 3‐Kinase Delta (PI3Kδ) Roginolisib In Patients With Refractory/Relapsed Follicular Lymphoma
Highly Selective Allosteric Modulator of the Phosphoinositide 3‐Kinase Delta (PI3Kδ) Roginolisib In Patients With Refractory/Relapsed Follicular Lymphoma Open
Introduction: PI3Kδ inhibitors are very active in patients with lymphomas, but their clinical development has been hampered by toxicity (Brown et al, Lancet Oncol 2022). Roginolisib (IOA-244) exerts an allosteric modulation of the PI3Kδ C …
View article: Figure S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Correlation analysis of PI3Kd levels and the response to IOA-244 and Idelalisib
View article: Figure S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Correlation analysis of PI3Kd levels and the response to IOA-244 and Idelalisib
View article: Figure S1 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S1 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
IC50 curve of the ATP competitive assay and pie chart of the Kinativ assay
View article: Figure S2 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S2 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Target engagement kinase tree
View article: Table S2 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Table S2 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Table showing values of microsomal stability of IOA-244
View article: Figure S1 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S1 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
IC50 curve of the ATP competitive assay and pie chart of the Kinativ assay
View article: Data from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Data from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
PI3K delta (PI3Kδ) inhibitors are used to treat lymphomas but safety concerns and limited target selectivity curbed their clinical usefulness. PI3Kδ inhibition in solid tumors has recently emerged as a potential novel anticancer therapy th…
View article: Table S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Table S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Table showing the raw data of the AUC value of figure 2A
View article: Figure S2 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S2 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Target engagement kinase tree
View article: Figure S4 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S4 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Tumor experiments showing monotherapy testing of IOA-244
View article: Table S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Table S3 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Table showing the raw data of the AUC value of figure 2A
View article: Figure S4 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance
Figure S4 from IOA-244 is a Non–ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance Open
Tumor experiments showing monotherapy testing of IOA-244