The limited state of current clinical transplantation science was recently the subject of an opinion piece from an individual that received her first heart transplant at just 25 years of age only to soon succumb at the age of 60 to one of the many risky outcomes expected for anyone taking standard requisite immunosuppression regimens used for any transplantation, in her case terminal cancer. Read More
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. Read More
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. Read More
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. Read More
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. Read More
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). Read More
Lysyl oxidase homologue 2 (LOXL2) inhibitors have been reported in a Yuhan Corp. patent as potentially useful for the treatment of idiopathic pulmonary fibrosis, nonalcoholic steatohepatitis (NASH), chronic kidney disease and cirrhosis. Read More
Nearly everyone with diabetes for >20 years will develop diabetic retinopathy or uveitis, which are collectively among the most common causes of premature blindness. Melanocortin is a short peptide that not only controls pigmentation, but that is most importantly expressed constitutively in the intraocular space where it serves essential functions suppressing inflammation in the retina, ultimately preventing blindness. Read More
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have patented benzodiazepine derivatives acting as GABA(A) receptor subunit α2β2γ1 positive allosteric modulators and reported to be useful for the treatment of neurological disorders. Read More
Research at Beijing Scitech-Mq Pharmaceuticals Ltd. has led to the identification of inhibitors of epidermal growth factor receptor (EGFR; HER1; erbB1) and its mutants which are reported to be useful for the treatment of cancer and autoimmune diseases. Read More
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. Read More
Humanwell Healthcare (Group) Co. Ltd. researchers have prepared and tested AP2-associated protein kinase 1 (AAK1) inhibitors that are reported to be useful for the treatment of bipolar disorder, pain, schizophrenia, Alzheimer’s and Parkinson’s disease. Read More
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. Read More
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. Read More
