Petra Pharma Corp. has patented phosphatidylinositol 3-kinase α (PI3Kα, PIK3CA) (H1047R mutant) allosteric inhibitors reported to be useful for the treatment of cancer, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities and PIK3CA-related overgrowth spectrum.
High levels of adenosine known to stimulate tumor immunoevasion are formed by the ecto-5’-nucleotidase enzyme (CD73) conversion of adenosine monophosphate to adenosine. CD73 is a cell surface enzyme that is overexpressed in many cancer types where this overexpression has been correlated with a poor prognosis.
Neuroblastoma is among the deadliest cancers in infants, with frequent relapse and long-term survival being <10%. Recently, it has been found that protein RD3 is constitutively expressed in healthy adult and fetal tissues beyond the retina, and it follows a gradient expression from high to low levels in ganglioneuroma and neuroblastoma.
Triple-negative breast cancer (TNBC) constitutes the most aggressive form of breast cancer and presents a high frequency of relapse. The available treatment options are limited and accompanied by resistance and significant treatment side effects.
Bridge Biotherapeutics Inc. has received FDA clearance to proceed with a first-in-human study of BBT-207, a potential broad-spectrum fourth-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) for the treatment of non-small-cell lung cancer (NSCLC).
Researchers from Jacobio Pharmaceuticals Co. Ltd. have reported preclinical data for JAB-X1800, an immunostimulatory antibody-drug conjugate (iADC) targeting CD73. JAB-X1800 was developed using an anti-CD73 monoclonal antibody (MAb) for targeted delivery of a highly potent noncyclic dinucleotide STING agonist payload, JAB-27670.
The infiltration of regulatory T cells (Tregs) into the tumor microenvironment and a low ratio of effector T cells to Tregs is usually tied to tumor progression and poor prognosis. On the other hand, interleukin-2 receptor subunit α (IL-2-RA) is highly expressed on Tregs.
Researchers from Flare Therapeutics Inc. presented the discovery of a first-in-class covalent peroxisome proliferator-activated receptor γ (PPARγ) inverse agonist, FX-909, being developed for the treatment of urothelial cancer (UC). Synthesis and optimization of covalent lead series of agonists of the PPARγ lineage transcription factor led to the discovery of FX-909 as the lead covalent PPARγ inverse agonist with powerful repressive conformational biasing activity.
Researchers from The Chinese University of Hong Kong and collaborators have discovered a promising target for immunotherapy in non-small-cell lung carcinoma (NSCLC). Their study investigated the regulation of tumor-associated neutrophils (TANs), in particular TGF-β1/Smad3 signaling, and their response to the microenvironment in NSCLC patients.
Caraway Therapeutics Inc. has divulged mucolipin (MCOLN; TRPML) activators reported to be useful for the treatment of metabolic diseases, aging, cancer, ciliopathy, neurodegeneration and muscle disorders.
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