Foghorn Therapeutics Inc. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding agent coupled to a histone acetyltransferase p300 (EP300)-targeting moiety. As such, they are described as EP300 degradation inducers potentially useful for the treatment of cancer.
Just as investors were looking ahead to news by year-end on Prelude Therapeutics Inc.’s SMARCA2-targeted degraders, the firm said work in the space will be halted, with efforts shifting toward the mutant selective JAK2V617F JH2 inhibitor program by way of a new deal with Incyte Corp.
Foghorn Therapeutics Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising ubiquitin ligase binding moieties covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety reported to be useful for the treatment of cancer and viral infection.
Work at Foghorn Therapeutics Inc. has led to the design of proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding agent coupled to CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker acting as CBP degradation inducers.
Wall Street apparently wanted more from Prelude Therapeutics Inc.’s phase I data with SMARCA2 enzyme degrader PRT-3789 in cancer, which rolled out Sept. 13 during the recent European Society of Medical Oncology Congress in Barcelona, but hopes are still high for other prospects in the class pushed forward by various developers.
Researchers from Foghorn Therapeutics Inc. recently presented preclinical data for FHD-609, a heterobifunctional degrader of BRD9 designed for the treatment of sarcoma. Synthesis and optimization of a series of first-generation compounds led to the identification of FHD-609 as a rapid, selective and highly potent BRD9 degrader, with high plasma stability and acceptable solubility.
Eli Lilly & Co. has selected FHD-909, a first-in-class oral BRM-selective inhibitor, for clinical development from its 2021 collaboration with Foghorn Therapeutics Inc. Lilly plans to file an IND for FHD-909 in the second quarter of this year. The primary target patient population is BRG1-mutated non-small-cell lung cancer.
Foghorn Therapeutics Inc. has described probable global transcription activator SNF2L2 (SMARCA2; BRM) and transcription activator BRG1 (SMARCA4) degradation inducers acting as BRG1- or BRM-associated factor (BAF) complex modulators reported to be useful for the treatment of cancer and viral infection.
Additional deaths believed to be associated with one of Foghorn Therapeutics Inc.'s lead candidates led the U.S. FDA to put a full clinical hold on its phase I study in relapsed and/or refractory acute myelogenous leukemia and myelodysplastic syndrome.
