ATUX-1215 / Atux Iskay Group - LARVOL DELTA

Evaluating PP2a Activators As an Adjunct to Doxorubicin Treatment in Neuroblastoma (Quick-Shot) (ACS-CLINCON 2025) - "Pharmacologic PP2A activation in combination with doxorubicin increases intracellular accumulation of doxorubicin resulting in a synergistic therapeutic effect. These findings are likely secondary to decreased expression of drug efflux pumps seen with PP2A activation."

Breast Cancer • Neuroblastoma • Oncology • Solid Tumor • ABCB1 • ABCG2

Pharmacologic PP2A activation as an adjunct to doxorubicin treatment in neuroblastoma (AAP-NCE 2025) - "Because of the effects of PP2A activation on drug efflux pumps in other cancer cell types, we hypothesized that pharmacologic reactivation of PP2A in neuroblastoma would enhance doxorubicin cytotoxicity through modulation of drug efflux pumps. SK-N-BE(2) human neuroblastoma cells were treated with doxorubicin in combination with a novel PP2A activating compound, ATUX-1215, supplied by our collaborator. Pharmacologic PP2A activation in human neuroblastoma cells increases intracellular accumulation of doxorubicin resulting in a synergistic effect on cell viability. These findings are likely secondary to decreased expression of drug efflux pumps seen with PP2A activation. Further exploration of PP2A activators as a chemotherapeutic adjunct in neuroblastoma is warranted."

Breast Cancer • Genito-urinary Cancer • Hepatocellular Cancer • Neuroblastoma • Prostate Cancer • Solid Tumor • ABCB1 • ABCG2

PP2a Activating Compound Sensitizes Group 3 Medulloblastoma Cells to Irradiation (Quick-Shot) (ACS-CLINCON 2024) - "PP2A activation downregulates DNA damage repair responses, leading us to hypothesize that pretreatment of human medulloblastoma patient-derived xenograft (PDX) cells with the novel PP2A activating compound, ATUX-1215, would sensitize the cells the effects of irradiation... Our findings illustrate that pretreatment with a PP2A activator, prior to XRT, sensitized the cells to irradiation. These results underscore the need for additional exploration of PP2A activators as a potential therapeutic adjunct for medulloblastoma."

Brain Cancer • Endocrine Disorders • Medulloblastoma • Oncology • Pediatrics • Solid Tumor

PP2A activation overcomes leptomeningeal dissemination in Group 3 medulloblastoma. (PubMed, J Biol Chem) - "The PP2A activators employed in this study are ATUX-6156 and ATUX-6954 (diarylmethylcycloamine sulfonylureas), and ATUX-1215 and ATUX-5800 (diarylmethyl-4-aminotetrahydropyran-sulfonamides)...The present investigation offers proof-of-principle data for PP2A-based reactivation therapy for Group 3 MB and provides the first indications that PP2A reactivation may challenge the current paradigm in targeting the 3-stage process of MB LMD. Further investigations of PP2A activators are warranted as these compounds may prove beneficial as therapeutics for MB."

Journal • Brain Cancer • Medulloblastoma • Oncology • Solid Tumor • CASP9 • CCL2 • CCR2 • CIP2A

PP2A activation as a new therapeutic strategy in neuroblastoma: Making sense out of senescence. (ASCO 2024) - "Topotecan, a common NBL chemotherapeutic, known to induce senescence, and ATUX-1215, a small molecule PP2A activator, were utilized. Activation of PP2A with a novel small molecule ameliorates topotecan-induced TIS in NBL cells irrespective of MYCN status. These results are promising, providing a potential novel therapeutic adjunct to children who are most in need of innovative interventions."

CNS Tumor • Neuroblastoma • Oncology • Pediatrics • Solid Tumor • CCL2 • MYC • MYCN