Lario Therapeutics Ltd. has synthesized voltage-dependent R-type calcium channel subunit α-1E (Cav2.3) blockers reported to be useful for the treatment of epilepsy, neurodegeneration, neurodevelopmental disorders, Parkinson’s disease, cerebral vasospasm and endocrine disorders.
Overexpression of focal adhesion kinase (FAK) is linked to worse prognosis and greater risk of metastasis in colorectal, cervical, breast and skin cancers. Despite its attractiveness as a therapeutic target, no effective inhibitors of focal adhesion kinase have yet been described.
Receptor-interacting protein kinase 1 (RIPK1) plays a pivotal role in ischemic stroke pathology by mediating necroptosis and promoting neuroinflammation, both of which contribute to secondary brain injury and worsen clinical outcomes.
Trethera Corp. has been awarded a $3 million Small Business Innovation Research (SBIR) grant from the National Institute of Health (NIH) to support evaluation of Trethera’s lead candidate, TRE-515, for the treatment of systemic lupus erythematosus (lupus).
Genfleet Therapeutics Co. Ltd. has presented preclinical data on their KRAS G12C inhibitor fulzerasib, also known as GFH-925, the third approved KRAS G12C inhibitor for treating non-small-cell lung cancer (NSCLC).
DNA-binding drugs have shown potential against the parasitic disease African trypanosomiasis (sleeping sickness), but they have several disadvantages, such as toxic effects or inability to cross the blood-brain barrier, which may prevent them from treating individuals in which the parasites have entered the central nervous system.
Dysregulation of the polycomb repressive complex 2 (PRC2) is associated with epigenetic silencing of tumor suppressor genes, leading to alterations in cell proliferation, differentiation and survival that contribute to cancer progression.
Vasthera Co. Ltd. has received IND clearance from the U.S. FDA, enabling it to initiate a phase I trial for VTB-10 for pulmonary arterial hypertension (PAH). Vasthera identified a deficiency of the enzyme peroxiredoxin (PRX) in PAH lesions and used its Redoxizyme platform to develop VTB-10, a small-molecule enzyme that precisely replicates PRX function.
RAS is the most mutated oncogene in cancer (about 30% rate), where mutations in KRAS are the most prevalent. The approval of covalent KRAS G12C inhibitors has shown allosteric inhibition of KRAS to be a feasible therapeutic strategy, and there is interest in developing new KRAS-directed therapies to target additional KRAS mutants. Amgen has presented data regarding its pan-KRAS inhibitor AMG-410.
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