Avstera Therapeutics Corp. has received FDA clearance of its IND application for HDAC6 inhibitor AVS-100. Avstera intends to initiate a phase Ia/b trial in the first half of 2024 to evaluate AVS-100 alone and in combination with pembrolizumab in locally advanced or metastatic solid tumors.
Phosphoinositide 3-kinase (PI3K) is a key cell cycle pathway regulator involved in tumor growth and development. PI3Kα mutations in p110α subunit, H1047R and E542K/E545K are found in patients with several cancer types, including breast cancer and are targeted by approved drugs such as Piqray (alpelisib, Novartis AG).
Researchers from Insilico Medicine Inc. reported on ISM-5043, a novel KAT6A inhibitor aimed to be used for the treatment of refractory ER+ breast cancer.
Shares of Checkpoint Therapeutics Inc. dropped 44.8% Dec. 18 on news that the U.S. FDA issued a complete response letter (CRL), delaying potential approval of PD-L1 antibody cosibelimab in metastatic or locally advanced cutaneous squamous cell carcinoma. The FDA had accepted in March the BLA, seeking use for treating patients who are not candidates for curative surgery or radiation, setting a Jan. 3, 2024, PDUFA date.
Taiwan’s Caliway Biopharmaceuticals Co. Ltd. said it secured more than $100 million in an oversubscribed capital raise to advance CBL-514, its lead asset for subcutaneous fat reduction nearing phase III studies.
Shanghai Meiyue Biotech Development Co. Ltd. has identified serine/threonine-protein kinase SIK2 (QIK) inhibitors reported to be useful for the treatment of fibrosis, cancer, autoimmune diseases, transplant rejection, cardiovascular, dermatological, endocrine, and inflammatory disorders, among others.
Hangzhou Healthytide Biotechnology Co. Ltd. has synthesized peptoids acting as integrin α5β1 (ITGA5; VLA-5) antagonists reported to be useful for the treatment of cancer and macular degeneration.
Neuexcell Therapeutics Inc. has announced that NXL-004, an investigational AAV gene therapy product being developed for the treatment of malignant glioma, has been awarded orphan drug designation by the FDA.
Researchers from Zhejiang University and affiliated organizations have reported the discovery of novel orally bioavailable bromodomain-containing protein 9 (BRD9) proteolysis-targeting chimera (PROTAC) candidates for the treatment of acute myelocytic leukemia (AML). Synthesis and optimization led to the discovery of a novel series of BRD9 PROTACs, with compound [I] selected as the lead candidate with the best degradation and proliferation inhibition activities in vitro.
Isozymes that are overexpressed in cancer and key in some metabolic processes are potential therapeutic targets. Previous studies found that phosphoenolpyruvate carboxykinase 2 (PCK2) is required by cancer cells for maintaining high metabolic activity and proliferation in some cancer types, but no small-molecule PCK2 inhibitors currently exist.
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