Merck KGaA has announced it is advancing M-3554, a potential first-in-class anti-GD2 antibody-drug conjugate (ADC), toward the clinic. M-3554 links an exatecan payload with an anti-GD2 antibody.
Researchers from National Health Research Institutes reported the discovery and preclinical characterization of a novel long half-life Aurora A (AURKA) inhibitor being developed for the treatment of MYC-amplified solid tumors. Lead optimization of a previously reported series of small-molecule Aurora kinase inhibitors led to the discovery of AURKA kinase inhibitor 6K465, which was then developed into the acyl-based prodrug DBPR-728.
Xuanzhu Pharma Co. Ltd. has divulged poly (ADP-ribose) polymerase 1 (PARP-1; ARTD1) inhibitors reported to be useful for the treatment of atherosclerosis, cancer, epilepsy, hyperlipidemia, ischemia, osteoarthritis, pain and Alzheimer’s disease.
Sitryx Therapeutics Ltd. has identified compounds acting as pyruvate kinase M2 (PKM2) and/or PKLR activators reported to be useful for the treatment of cancer, obesity, inflammation, diabetes and hematologic disorders.
Petra Pharma Corp. has synthesized phosphatidylinositol 3-kinase α (PI3Kα) inhibitors, particularly H1047R and/or E545K mutant allosteric inhibitors. They are described as potentially useful for the treatment of cancer, PIK3CA-related overgrowth spectrum, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities.
Tumor-associated macrophages (TAMs), located within the tumor microenvironment (TME), are involved in immunosuppression, metastasis, chemoresistance and angiogenesis. Reprogramming TAMs intratumorally by targeting glutamine metabolism may provide a robust antitumor effect.
Researchers from Australis Pharmaceuticals Pty Ltd. have presented preclinical data for the microtubule-destabilizing agent AUS-001, which is being evaluated in models of glioblastoma (GBM).
It is known that an abnormal activation of the mitogen-activated protein kinase (MAPK) pathway is involved in tumor formation and progression, where MEK1 and MEK2 are the key proteins involved in this pathway. At the ongoing ASCO meeting in Chicago, Pasithea Therapeutics Corp. presented data on PAS-004, a macrocyclic MEK inhibitor for the potential treatment of cancer.
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