SLX 3030 / Biolexis Therap - LARVOL DELTA

Development of a selective, oral ATP-competitive CDK9 inhibitor, BLX-3030, for treatment of pancreatic cancer (AACR 2024) - "The combination effects between BLX-3030 and standard of care regimen, gemcitabine (GEM) and nab-paclitaxel (NP), was assessed using the SRB assay. Overall, the novel CDK9 inhibitor, BLX-3030, demonstrated potent activity in pancreatic cancer cell line models and presents a promising preclinical lead for pancreatic cancer. (This work was supported in part by Biolexis Therapeutics and the Seena Magowitz Foundation)."

Endocrine Cancer • Gastrointestinal Cancer • Neuroendocrine Tumor • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • MYC

BLX-3030, a potent, selective, orally available small molecule CDK9 inhibitor for aggressive variant prostate cancers (AACR 2024) - "BLX-3030 is currently being investigated in non-clinical toxicology, toxicokinetic, and core battery of safety pharmacology studies including the assessment of effects on cardiovascular, central nervous, and respiratory systems."

Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Neuroendocrine Tumor • Oncology • Prostate Cancer • Solid Tumor • MCL1 • MYC • MYCN

Discovery of an oral, potent, and selective CDK9 molecular glue degrader SLX-3065 active in aggressive variant prostate cancers (AVPC) (AACR 2024) - "Kinase selectivity, Nano BRET, ADME-Tox, in vitro safety, secondary pharmacological assays, Cell engraftment mouse tumor mode, and PK studies were performed. We designed and synthesized a series of novel small molecule CDK9 Molecular Glue degraders based on our initial CDK9 inhibitor lead SLX-3030 and SLX-3039. In summary, both SLX-3064 and SLX-3065 molecular glues display complete degradation of CDK9 and its downstream markers, and these degraders possess ideal developable criteria as oral agents. With these characteristics, SLX-3065 was selected as a candidate that had the appropriate developable properties and our plans for conducting additional IND-enabling studies and future clinical trial plans will also be discussed."

Late-breaking abstract • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Neuroendocrine Tumor • Oncology • Prostate Cancer • Solid Tumor • CDK9 • MCL1 • MYC • MYCN

Biolexis Therapeutics to Present Five Posters at the American Association for Cancer Research (AACR) Annual Meeting 2024 (PRNewswire) - "Biolexis Therapeutics, Inc...today announced it will present five posters at the 2024 American Association for Cancer Research (AACR), taking place April 5-10, 2024, in San Diego, CA."

Preclinical • Genito-urinary Cancer • Hematological Malignancies • Multiple Myeloma • Oncology • Prostate Cancer • Solid Tumor

Development of BLX-3030, a Potent, Selective, Orally Available CDK9i shows promise in Pancreatic Ductal Adenocarcinoma (PDAC) Models (AACR-NCI-EORTC 2023) - No abstract available

Late-breaking abstract • Gastrointestinal Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma

Development of BLX-3030, a Potent and Selective Inhibitor of CDK9 for the Treatment of N-MYC Driven NeuroEndocrine Prostate Cancers (NEPC). (AACR-NCI-EORTC 2023) - No abstract available

Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • CDK9 • MYCN

Development of BLX-3030, a potent and selective inhibitor of CDK9 for the treatment of NMYC-driven NEPCS. (ASCO 2023) - "In summary, a series of BLX-3030 and its analogs display a potency in MYC-driven PCa, with ideal PK properties in rodent, canine species ranging 28-82 % F, with low clearance, and > 3.0 hr half-life. Within this profile, BLX-3030 was selected as a candidate that had the appropriate developable properties. Our plans for IND enabling studies and future clinical trials will also be discussed."

Genito-urinary Cancer • Neuroendocrine Tumor • Oncology • Prostate Cancer • Solid Tumor • CDK9 • MCL1 • MYC • MYCN