When used as monotherapy against tumors, small molecules that mimic the SMAC protein and thereby inhibit apoptosis are ineffective. The same is true for inhibitors of BET family proteins. If each therapy on its own does not work, what about the two therapies together?
Four Chinese biopharmaceuticals unveiled early data on respective cancer therapies at the American Society of Hematology (ASH) 2024 meet in San Diego, including Cstone Pharmaceuticals Co. Ltd.’s receptor tyrosine kinase-like orphan receptor 1 (ROR1)-inhibiting antibody-drug conjugate (ADC) in phase I study for lymphomas.
Vyne Therapeutics Inc. has received IND clearance from the FDA allowing it to initiate a first-in-human phase Ia study of VYN-202, an oral small-molecule BD2-selective BET inhibitor for autoimmune diseases.
Because selective BET inhibitors present better efficacy and safety than pan-BET inhibitors, current research is focused on the development of BD1- or BD2-selective inhibitors.
The bromodomain and extraterminal domain (BET) family of proteins are involved in cell cycle regulation and for this reason are considered therapeutic targets in cancer therapeutics.
More than 30 years after entering the scene as a first-generation monoclonal antibody pioneer, Morphosys AG is to be acquired by Novartis AG for €2.7 billion (US$2.9 billion). The all-cash deal, announced after Nasdaq closed on Feb. 5, will see Novartis paying €68 per share, a premium of 94% to the average daily price in the month leading up to Jan. 25, when rumors of a takeover started swirling.
Morphosys AG’s rare blood cancer treatment hit its phase III primary endpoint but missed statistical significance on a secondary endpoint, sinking the stock for the day. Top-line data from the study treating JAK inhibitor-naïve patients who have the rare blood cancer myelofibrosis showed the combination of pelabresib, a BET inhibitor, and the JAK inhibitor ruxolitinib produced a statistically significant improvement in spleen volume reduction, which was the primary endpoint.
Vyne Therapeutics Inc. has released promising new preclinical data on its oral small-molecule BD2-selective BET inhibitor, VYN-202, in preclinical models of psoriasis and rheumatoid arthritis. In a well-established model, a psoriasis phenotype was induced in BALB-C mice, and treatment was administered intraperitoneally with either VYN-202, the allosteric TYK2 inhibitor Sotykto (deucravacitinib, Bristol Myers Squibb Co.) or placebo.
Researchers from China Pharmaceutical University and affiliated organizations have reported the discovery and preclinical evaluation of a novel bromodomain and extra-terminal (BET) inhibitor, DDO-8926, being developed for the management of neuropathic pain.
By the end of this year, it will become apparent whether Morphosys AG has executed one of the biotechnology industry’s boldest pivots in recent years or has instead blown $1.7 billion of investor cash on a dud. The day of reckoning is coming a little sooner than expected for the Planegg, Germany-based firm, as it has completed recruitment in a phase III trial of pelabresib in first-line myelofibrosis ahead of schedule. Top-line data from the study are now expected before year-end, instead of early 2024.
