Repolarization abbreviation with the antiarrhythmic drug mexiletine has been found to normalize the QTc interval and reduce the rate of events in long QT syndrome type 3 (LQT3), but it is only partially efficacious in other malignant forms, including LQT2 and LQT8. There are compounds that have not been tested, such as hERG channel agonists, which are capable of shortening repolarization. The potent hERG agonist ICA-105574 was thus tested in a clinically relevant porcine model of LQT8.
At the recent European Society of Cardiology meeting, Anacardio AB and Helsinn Healthcare SA presented data on their oral small-molecule ghrelin receptor agonist and first-in-class calcium sensitizing inotrope, AC-01, in preclinical models of heart failure.
Keros Therapeutics Inc. has presented preclinical data on the activin receptor type IIB ligand trap RKER-012 (a research version of KER-012 [cibotercept]) in a preclinical pulmonary arterial hypertension model.
Plexium Inc. has described the efforts that led to the discovery of PLX-4545, an orally bioavailable molecular glue degrader of IKZF2 for the treatment of cancer that is currently undergoing evaluation in a phase I study in healthy volunteers.
Hematopoietic progenitor kinase 1 (HPK1) plays a relevant role in regulating T-cell, B-cell and dendritic cell function. As its inactivation both in vitro and in vivo contributes to tumor growth inhibition, HPK1 is considered a therapeutic target to explore in cancer immunotherapy.
Itheos Therapeutics Inc. recently presented the discovery of a first-in-class, potent and selective ENT1 inhibitor, EOS-984 (EOS-301984), for the treatment of solid tumors. Immune checkpoint inhibitors (ICIs) have become essential in treating solid tumors, but only a limited number of patients currently benefit from approved ICIs.
Aging is part of the life cycle and, although the effects are not manifest until after adulthood, it actually occurs from birth. The concept of senescence has traditionally been associated with aging. However, an embryo has senescent cells. In that case, what is aging, how can it be measured, and from what point in the life cycle?
Since the publication of The Hallmarks of Aging in 2013, aging research has exploded. The field now has more than 300,000 articles on the biological signals of the effect of time on the body. What would Marty McFly, the legendary character from the Back to the Future saga who traveled with his DeLorean time machine from the ‘80s to the ‘50s, think if he visited 2024 and saw laboratories experimenting with techniques to turn back the biological clocks of cells or increase the lifespan of rejuvenated mice?
Arcus Biosciences Inc. recently disclosed the chemical structure of AB-521 (casdatifan), an orally available small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α) in early clinical development for the treatment of advanced solid tumors with a high prevalence of molecular alterations associated with pseudohypoxia, such as clear cell renal cell carcinoma (ccRCC).
Gilead Sciences Inc. recently disclosed details on the work that led to the discovery of elunonavir (GS-1156), an unboosted HIV protease inhibitor currently in phase I studies.
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