Evexta Bio News - LARVOL Sigma

|||||||||| rupitasertib (DIACC3010) / Evexta Bio
Journal: p70S6K as a Potential Anti-COVID-19 Target: Insights from Wet Bench and In Silico Studies. (Pubmed Central) - Nov 15, 2024
Meanwhile, our in silico investigations address the known off-target effects associated with M2698 by identifying a close analog called S34. In conclusion, this study presents novel and intriguing findings that could potentially lead to clinical applications with further investigations.

|||||||||| DIACC3010 / Diaccurate
DIACC3010, optimized inhibitor of S6 kinase, combined with endocrine therapy, has potent antitumor activity in treatment-resistant ER-positive HER2-negative metastatic breast cancer (Section 42; Poster Board #2) - Mar 14, 2023 - Abstract #AACR2023AACR_5919;
P1
Exploratory analyses from the phase 1 trial, along with nonclinical efficacy in PDX models, demonstrate that DIACC3010 may have antitumor activity in MBC patients with ET resistance. Experiments are underway to assess nonclinical efficacy of DIACC3010 combination with elacestrant or CDK4/6 inhibitors in various models of ER+ MBC, including ET resistant.

|||||||||| DIACC2010 / Diaccurate
DIACC2010, Sole-in-Class Selective Inhibitor of Kinesin KIF20A, Has Potent Preclinical Efficacy in Acute Myeloid Leukemia (ENMCC - Hall D) - Nov 4, 2022 - Abstract #ASH2022ASH_4863;
In the same experimental conditions, cytarabine (CYTA) had median IC50 of 207 nM (range 4-1580 nM)...Nevertheless, caspase inhibitors ZVAD-fmk and Emricasan partially rescued DIACC2010 cell death, although these inhibitors significantly rescued caspase activation induced by Venetoclax, a BCL-2 inhibitor triggering intrinsic apoptosis commonly used in AML treatment... Altogether, these results confirm the relevance of KIF20A-directed therapeutic approaches and support the development of DIACC2010 for the treatment of AML.

|||||||||| M2698 / EMD Serono
Journal: AKT inhibition in the central nervous system induces signaling defects resulting in psychiatric symptomatology. (Pubmed Central) - May 8, 2022
Altogether, these results confirm the relevance of KIF20A-directed therapeutic approaches and support the development of DIACC2010 for the treatment of AML. Our data elucidate the incidence and mechanisms of psychiatric AEs in patients treated with PI3K/AKT/mTOR inhibitors and emphasize the need for careful monitoring.

|||||||||| M2698 / EMD Serono
Clinical, Journal: Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers. (Pubmed Central) - Feb 16, 2022
Through the screening of in-house proprietary kinase library, 4-benzylamino-quinazoline-8-carboxylic acid amide 1 stood out, with sub-micromolar p70S6k biochemical activity, as the starting point for a structurally enabled p70S6K/Akt dual inhibitor program that led to the discovery of M2698, a dual p70S6k/Akt inhibitor. M2698 is kinase selective, possesses favorable physical, chemical, and DMPK profiles, is orally available and well tolerated, and displayed tumor control in multiple in vivo studies of PAM pathway-driven tumors.

|||||||||| Herceptin (trastuzumab) / Roche, M2698 / EMD Serono
Clinical, P1 data, Clinical Trial,Phase I, Journal: Phase 1 study of M2698, a p70S6K/AKT dual inhibitor, in patients with advanced cancer. (Pubmed Central) - Nov 4, 2021
P1
Trial registration ClinicalTrials.gov, NCT01971515. Registered October 23, 2013.

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
Trial completion, Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Sep 19, 2018
P1, N=101, Completed,  Sponsor: EMD Serono
Registered October 23, 2013. Active, not recruiting --> Completed

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
Enrollment closed, Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Jan 11, 2018
P1, N=101, Active, not recruiting,  Sponsor: EMD Serono
Active, not recruiting --> Completed Recruiting --> Active, not recruiting

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
Trial primary completion date, Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Dec 19, 2017
P1, N=111, Recruiting,  Sponsor: EMD Serono
Recruiting --> Active, not recruiting Trial primary completion date: Jan 2019 --> Aug 2018

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Jun 29, 2017
P1, N=129, Recruiting,  Sponsor: EMD Serono
Trial primary completion date: Jan 2019 --> Aug 2018 Trial primary completion date: Apr 2018 --> Jan 2019

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Oct 11, 2016
P1, N=130, Recruiting,  Sponsor: EMD Serono
Trial primary completion date: Apr 2018 --> Jan 2019 N=100 --> 130 | Trial primary completion date: Dec 2016 --> Apr 2018

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
Enrollment open, Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Dec 19, 2013
P1, N=100, Recruiting,  Sponsor: EMD Serono
N=100 --> 130 | Trial primary completion date: Dec 2016 --> Apr 2018 Not yet recruiting --> Recruiting

||||||||||  rupitasertib (DIACC3010) / Evexta Bio
New P1 trial, Metastases:  EMR100018-001: First-in-Human Dose Escalation Trial in Subjects With Advanced Malignancies (clinicaltrials.gov) -  Oct 27, 2013
P1, N=100, Recruiting,  Sponsor: EMD Serono



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