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M4205 (IDRX-42) is a highly selective type II receptor tyrosine kinase inhibitor of KIT, discovered by Merck KGaA and currently being developed by IDRx. The molecule is a notable example of kinase selectivity achieved with a non-classical hinge binder. M4205 (IDRX-42) has received an Orphan Drug designation and is currently being evaluated in a Ph. I/Ib FIH trial for GIST, one of the most common mesenchymal neoplasms in the GI tract.
SGR-1505, the first in-house clinical compound developed at Schrödinger, is an oral, allosteric MALT1 inhibitor currently in the clinic for the treatment of mature B cell malignancies. The discovery effort, disclosed at the ACS Spring 2024 meeting, was completed in an impressive 10 months, starting from a published scaffold. SGR-1505 demonstrated preclinical single-agent and combination activity as well as inducing resensitization in BTK and BCL-2 inhibitor-resistant tumors. The compound is currently progressing in a Ph. I trial in patients with mature B cell malignancies.
Throughout each month, the Drug Hunter team evaluates hundreds of molecules found in thousands of papers, press releases, conference presentations, and other materials to pick contenders for Molecules of the Month. Here, we curated a roundup of nearly 70 additional molecules that caught our interest from March 2024, including highlights from some of our favorites.
In March 2024, the landscape of patent disclosures continued to reflect the rapid pace of advances against key therapeutic targets. The Drug Hunter team has curated a searchable database encompassing over 200 patents pertinent to the field of drug discovery. This resource is further enriched with insightful spotlight on some of the most promising molecules and targets, including OX2R agonists, TEAD covalent inhibitors, NaV1.8 inhibitors, and selective PI3Kγ inhibitors, among others. This round-up provides a valuable tool for drug hunters to navigate the most recent trends in drug discovery.
Deciphera’s DCC-3116 is an oral ULK1/2 inhibitor targeting the autophagy pathway, a key mechanism of tumor survival and resistance to targeted therapy. Currently in two open-label Ph. I/II trials as a monotherapy and in combination with RTK pathway inhibitors, the structure and discovery of this first-in-class compound were recently presented at the ACS Spring 2024 meeting.