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Process Chemistry Development for the EZH2 Inhibitor PF-06821497 (Room 1B (San Diego Convention Center)) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_9287; Trial completion date: Dec 2024 --> May 2024 | Trial primary completion date: Dec 2024 --> May 2024 Development of new synthetic routes to the Zeste Homolog 2 (EZH2) Inhibitor PF-06821497 will be described.
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Bidirectional synthetic enablement of the EZH2 candidate PF-06821497 (Room 6C) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_2129; Thus, acetate performed better than carbonate and acetonitrile performed better than methanol. This new process installed the secondary alcohol early in the synthesis and oxidation followed by asymmetric reduction using a keto-reductase, provided a more efficient process for isolating the secondary alcohol with a high yield and >99% ee.
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Trial completion date, Trial primary completion date: PF-06821497 Treatment Of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma (clinicaltrials.gov) - Oct 30, 2020 P1, N=172, Recruiting, Our study results unravel potent synergy between ONC201 and EZH2i, highlight the role of ISR in the synergy, and provide further insights into the role of H3K27me3 in ONC201 drug sensitivity. Trial completion date: Apr 2023 --> Nov 2022 | Trial primary completion date: Apr 2023 --> Nov 2022
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Inhibition of EZH2 enhances tumor immunogenicity through diversification of tumor antigen presentation (Prince George's Exhibition Halls AB) - Oct 2, 2019 - Abstract #SITC2019SITC_1043; Our data illustrate the potential for targeting EZH2 to increase the immunogenicity of tumors through relieving epigenetic suppression of tumor antigen presentation machinery and silenced neoantigens. As EZH2 inhibitors are currently under clinical investigation, targeting EZH2 represents a promising combination approach with checkpoint inhibitors to elicit responses in poorly immunogenic tumors.
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Trial completion date, Trial primary completion date: PF-06821497 Treatment Of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma (clinicaltrials.gov) - Jul 2, 2019 P1, N=172, Recruiting, As EZH2 inhibitors are currently under clinical investigation, targeting EZH2 represents a promising combination approach with checkpoint inhibitors to elicit responses in poorly immunogenic tumors. Trial completion date: Jun 2023 --> Sep 2023 | Trial primary completion date: Jun 2023 --> Sep 2023
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