eprenetapopt

01/01/2023 - "APR-246 has been reported to exert such effects in malignant cells and is currently undergoing clinical trials in several cancer types. "
01/01/2022 - "Recent studies in solid cancers have found that APR-246 can also induce p53-independent cell death. "
01/01/2024 - "Here, we demonstrate that APR-246 and its active moiety, methylene quinuclidinone (MQ) can enhance the immunogenicity of tumor cells directly. "
01/01/2024 - "APR-246 increases tumor antigenicity independent of p53."
10/09/2023 - "Treatment with APR-246 reversed the effects of TP53 mutations in vitro and inhibited 22Rv1 TP53 R175H tumor growth in vivo in a dosage-dependent manner. "

11/08/2022 - "Thus, APR-246 treatment in combination with xCT immunetargeting may open new perspectives in the management of breast cancer."
11/08/2022 - "We demonstrate that combining the inhibition of xCT with the APR-246 drug significantly decreased breast cancer cell viability in vitro and induced apoptosis and affected cancer stem cells' self-renewal compared to the single treatments. "
11/08/2022 - "Here, we propose a combinatorial treatment based on xCT immunetargeting and APR-246 treatment as a strategy for tackling breast cancer. "
12/01/2018 - "The Mutant p53-Targeting Compound APR-246 Induces ROS-Modulating Genes in Breast Cancer Cells."
01/01/2018 - "However, APR-246 did not reduce cell viability in MCF-7 breast cancer cells, which express wild-type p53. "

05/28/2021 - "CX-5461 Enhances the Efficacy of APR-246 via Induction of DNA Damage and Replication Stress in Triple-Negative Breast Cancer."
01/01/2019 - "APR-246 alone and in combination with a phosphatidylserine-targeting antibody inhibits lung metastasis of human triple-negative breast cancer cells in nude mice."
01/01/2016 - "Combining the mutant p53-inactivating agent APR-246 (PRIMA-1MET) with the proteasome inhibitor carfilzomib is effective in overcoming chemoresistance in triple-negative breast cancer cells, creating a therapeutic opportunity for treatment of solid tumours and metastasis with mutant p53."

01/01/2016 - "An open-label phase I dose-finding study of APR-246 in hematological malignancies."
10/10/2012 - "Targeting p53 in vivo: a first-in-human study with p53-targeting compound APR-246 in refractory hematologic malignancies and prostate cancer."
01/01/2023 - "Results: APR-246 and COTI-2 activity favored hematologic neoplasms, but solid tumor activity varied by diagnosis. "
10/10/2012 - "APR-246 was administered as a 2-hour intravenous infusion once per day for 4 consecutive days in 22 patients with hematologic malignancies and prostate cancer. "
01/01/2021 - "The mutant p53-reactivating compound APR-246 (Eprenetapopt/PRIMA-1Met) is currently being tested in phase II and III clinical trials in several hematological malignancies with mutant TP53. "

01/01/2016 - "APR-246 is currently tested in a phase Ib/II trial in patients with high-grade serous ovarian cancer. "
01/01/2022 - "Accordingly, combination of APR-246 and NF-κB inhibitor compounds strongly synergized in killing of CIP2A-positive ovarian cancer cells. "
01/01/2022 - "Mechanistically, the lack of CIP2A expression hypersensitizes the ovarian cancer cells to APR-246 by inhibition of NF-κB activity. "
12/01/2018 - "APR-246 is currently being tested in a phase II clinical trial in high-grade serous ovarian cancer. "
01/01/2022 - "Results also reveal CIP2A as a candidate APR-246 combination therapy target for ovarian cancer."