BEA-17 / Beactica - LARVOL DELTA

Leveraging non-enzymatic functions of LSD1 for novel therapeutics. (PubMed, Trends Pharmacol Sci) - "Only one allosteric inhibitor (SP-2577) and two nonproteolysis-targeting chimera (PROTAC) LSD1 degraders (BEA-17 and UM171), which target its enzyme-independent functions, have entered clinical assessment. Given the limited exploration of therapeutic strategies targeting the non-enzymatic functions of LSD1, in this opinion, we summarize current insights into its biological roles and structural characteristics. We also highlight potential therapeutic interventions targeting the non-enzymatic functions of LSD1, including allosteric inhibitors, protein-protein interaction (PPI) inhibitors, and small-molecule degraders, and discuss challenges and future directions in drug discovery targeting these functions."

Journal • Review • Targeted Protein Degradation

Mining the Dynamical Properties of Substrate and FAD Binding Pockets of LSD1: Hints for New Inhibitor Design Direction. (PubMed, J Chem Inf Model) - "After 20 years of research, only one small-molecule drug, BEA-17, targeting the degradation of LSD1 and CoREST has been approved by the U.S. Food and Drug Administration...Additionally, we identified pockets that positively or negatively correlate with the substrate and FAD binding pockets, which can be exploited for the design of allosteric or concurrent inhibitors. Our results reveal the intricate dynamical properties of LSD1 as well as multiple novel conformational states, which deepen our understanding of its sophisticated functions and aid in the rational design of new inhibitors."

Journal

Strategies that regulate LSD1 for novel therapeutics. (PubMed, Acta Pharm Sin B) - "Several LSD1 inhibitors and two small-molecule degraders (UM171 and BEA-17) have entered the clinical stage...Moreover, some post-transcriptional modifications and cellular metabolites can also regulate LSD1 expression or its demethylase activity. Therefore, in this review, we will systematically summarize how proteins involved in the transcriptional corepressor complex, various post-translational modifications, and metabolites act as regulatory factors for LSD1 activity."

Journal • Review • CNS Disorders • Infectious Disease • Oncology • KDM1A

Beactica Therapeutics strengthens its preclinical development team (PRNewswire) - "Beactica Therapeutics AB...announced two appointments to its preclinical development team. Dr Anneli Hällgren will lead the preclinical development and Dr Carl Magnus Andersson will lead the CMC activities. The appointments are made in preparation for IND-enabling studies of preclinical candidate BEA-17, a novel small molecule cancer immunotherapeutic agent under development by Beactica."

Preclinical • Oncology • Solid Tumor

Beactica Therapeutics announces the selection of BEA-17 as a preclinical candidate (PRNewswire) - "Beactica Therapeutics AB...announced the selection of BEA-17 as a preclinical candidate for its LSD1 programme aimed at finding new therapies for aggressive brain tumours and other life-threatening cancers....With the selection of this first preclinical candidate, IND-enabling toxicology studies will be initiated in preparation for clinical trials."

Preclinical • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Oncology • Solid Tumor

Potentiation of immunotherapy by LSD1 modulation (AACR 2023) - "LSD1 has emerged as a potential therapeutic target to increase the effectiveness of cancer immunotherapy. In a CT26 syngeneic animal model of colon cancer, BEA-17 potentiates the activity of anti-PD1 inhibitors. Finally, in a syngeneic GL261 animal model of glioblastoma, BEA-17 increases the effectiveness of standard-of-care temozolomide + radiation."

IO biomarker • Brain Cancer • CNS Tumor • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Glioblastoma • Oncology • Solid Tumor

Beactica Therapeutics and Oscotec mutually agree to conclude oncology collaboration (PRNewswire) - "Beactica Therapeutics AB...and Oscotec Inc...announced that they have mutually agreed to terminate their collaboration and licensing agreement. The collaboration focused on research and development of novel anti-cancer drug candidates arising out of Beactica's LSD1 programme. The LSD1 programme includes BEA-17...As part of the agreement, Beactica Therapeutics will retain full exclusive global rights for further development and commercialization of the LSD1 programme, and gain ownership of all results from the collaboration."

Licensing / partnership • CNS Tumor • Glioblastoma • Glioma • Oncology • Solid Tumor

Beactica Therapeutics to present update on LSD1 programme at the AACR Annual Meeting 2023 (PRNewswire) - "Beactica Therapeutics AB, the Swedish precision oncology company, today announced that its LSD1 programme has been selected for a poster presentation at the American Association for Cancer Research's Annual Meeting 2023....Beactica Therapeutics' poster presentation will include new positive results with BEA-17 from in vitro and in vivo studies, including potentiation of anti-PD1 checkpoint inhibitors in a syngeneic animal model of colon cancer (CT26) and potentiation of standard of care (radiation + temozolomide) in a syngeneic animal model of glioblastoma (GL261)."

Preclinical • Brain Cancer • CNS Tumor • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Glioblastoma • Glioma • Oncology • Solid Tumor

Beactica Therapeutics receives FDA Orphan Drug Designation for BEA-17 for the treatment of glioblastoma (PRNewswire) - "Beactica Therapeutics AB...announced that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation to BEA-17 for the treatment of glioblastoma (GBM). Incentives that come with the designation include eligibility for federal grants, tax credits for qualified clinical trials, prescription drug user fee exemptions, and a seven-year marketing exclusivity period upon FDA approval."

Orphan drug • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor