Gilead Sciences Inc. has identified new GTPase KRAS G12D mutant inhibitors and proteolysis targeting chimeras (PROTACS) comprising an E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS G12D mutant-targeting moiety potentially useful for the treatment of cancer.
Bristol Myers Squibb Co. (BMS) has disclosed new Ikaros family zinc finger protein 1 (IKZF1, Ikaros), IKZF2 (Helios), IKZF3 (Aiolos) and/or IKZF4 (Eos) degradation inducers potentially useful for the treatment of cancer.
Researchers from Hangzhou DAC Biotechnology Co. Ltd. reported preclinical efficacy data for DXC-016, a next-generation, subcutaneously administered, dual-payload c-Met-targeting antibody-drug conjugate (ADC) derived from the DXA-016 anti-c-Met nanobody.
Tumor-associated calcium signal transducer 2 (TROP2) is a transmembrane glycoprotein involved in different signaling pathways that promote proliferation, migration and invasion of tumoral cells, and its overexpression is associated with poor prognosis in multiple cancer types. Astellas Pharma Inc. has developed a TROP2-targeting antibody-drug conjugate (ADC), ASP-2998, and recently presented preclinical data on the candidate.
Taiho Oncology Inc., Taiho Pharmaceutical Co. Ltd. and Araris Biotech AG have announced completion by the FDA of the IND review period for ARC-02, enabling initiation of a phase I trial by Taiho Oncology.
Researchers from Genfleet Therapeutics (Shanghai) Co. Ltd. reported the preclinical profile of GFH-276, a molecular glue designed to function as a pan-RAS(ON) inhibitor.
A recent Ensem Therapeutics Inc. patent details the discovery of tricyclic derivatives acting as GTPase KRAS (mutant) inhibitors for use in the treatment of cancer.
Codeable Therapeutics Inc. has developed new antibody-drug conjugates comprising an antibody covalently linked to a cytotoxic drug for potential use in the treatment of cancer.
CDKs are central regulators of cell-cycle progression in cancer, with resistance to CDK4/6 inhibitors frequently converging on CDK2 activation through cyclin E upregulation or CCNE1 amplification, supporting CDK2 inhibition as a strategy to restore cell-cycle control. Researchers from Novartis AG have revealed the preclinical profile of ECI-830, an oral bioavailable, highly selective ATP-competitive CDK2 inhibitor.
Insilico Medicine Cayman Topco has nominated ISM-0387, an MTA-cooperative protein arginine methyltransferase 5 (PRMT5) inhibitor, as a preclinical developmental candidate for glioblastoma. The discovery and optimization process for ISM-0387 was powered by Chemistry42, Insilico’s generative chemistry platform integrated with over 40 generative AI models.
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