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.
Erasca Inc. has received FDA clearance of its IND application for ERAS-3490, an orally available small-molecule KRAS G12C inhibitor designed to have high central nervous system (CNS) penetration for the treatment of KRAS G12C-mutated solid tumors, including non-small-cell lung cancer (NSCLC).
Researchers from the University of Zaragoza and Promontory Therapeutics Inc. have discovered that PT-112, which has a multimodal mechanism of action, could have different clinical applications in cancer treatment due to its effects on mitochondria in castration-resistant prostate cancer (CRPC). PT-112 is an immunogenic small molecule currently in phase II development in metastatic castration-resistant prostate cancer (mCRPC). The researchers designed PT-112 to target advanced solid tumors, such as thymus, small-cell, non-small-cell lung or CRPC.
Recent efforts have unveiled UCB-0022 (UCB Pharma Inc.) as an oral, brain-penetrant small molecule acting as a selective D1 positive allosteric modulator.
Prism Biolab Co. Ltd. has added Genentech Inc., a unit of Roche Holding AG, to the list of users for its peptide mimetic small-molecules library after signing a multitarget research collaboration and licensing agreement.
Prism Biolab Co. Ltd. has added Genentech Inc., a unit of Roche Holding AG, to the list of users for its peptide mimetic small-molecules library after signing a multitarget research collaboration and licensing agreement. Under the agreement, Tokyo-based Prism Biolab will open its Pepmetics Library, a library of peptide mimetic small molecules, to screen against targets selected by Roche and Genentech.
In June, Morphosys AG acquired Constellation Pharmaceuticals Inc. in a deal worth $1.7 billion in which the German biotech monetizes a royalty from a big-selling antibody, spending the lump sum on research into small-molecule BET inhibitors. It’s a bold move and one that perhaps demonstrates a renewed interest in small-molecule drugs after a period when antibody-based molecules have been the dominant force in the market for branded drugs.
Boston-based Nirogy Therapeutics Inc.’s $16.5 million series A round is meant to enable a pipeline of small-molecule drugs targeting the solute carrier family of transporter proteins (SLCTs) embedded in the cell membrane, and let the firm bring its front oncology runner to the clinic in 2022.
Pointing to his company’s work on “the next frontier in small molecules,” Ribometrix Inc. CEO Mike Solomon said the potential $1 billion-plus deal with Roche Holding AG offers evidence of big pharma’s mounting interest. Expertise in RNA folds helped Ribometrix nail down an agreement with Basel, Switzerland-based Roche’s Genentech arm that brings $25 million up front and potential milestone payments beyond $1 billion, as the pair discovers and develops RNA-targeted small-molecule therapeutics. Genentech gains exclusive rights to several predefined targets, including an exclusive global license for the development and commercialization of molecules.
Skyhawk Therapeutics Inc., one of the early leaders in developing small-molecule drugs that target RNA, closed out the year with yet another big pharma partnering deal, an alliance with Vertex Pharmaceuticals Inc., in which it is getting $40 million up front plus up to $2.2 billion more in milestones and royalties on product sales.
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