Camlipixant is an orally administered antagonist of the ATP-sensing P2X3 homotrimeric receptor ion channel, originated by AstraZeneca AB and assigned to the Canadian NEOMED Institute (now adMare), and developed by BELLUS Health (Canada), for the treatment of chronic cough. Chronic cough remains difficult to treat – the last FDA-approved anti-tussive, dextromethorphan, was first approved in 1958 and has demonstrated limited clinical efficacy.

What is it? GB0139 is a selective, inhaled inhibitor of galectin-3 and galectin-1 in Ph. II for IPF and COVID-19 pneumonitis, and is Galecto’s ($GLTO) lead asset. Galecto was founded in 2011 with Lund University academic galectin research leaders Ulf Nilsson and Hakon Leffler, and has had a research focus on galectin-3 modulators to treat [...]

The Janssen gut-restricted COX-2 inhibitor, compound 10 , is a tool compound used to test the hypothesis that gut-restricted COX-2 inhibition would be beneficial for cancer without the cardiovascular risk of systemic COX-2 inhibition. Unfortunately, IVIVC of several compounds demonstrated that in vivo efficacy was not driven by gut COX-2 [...]

JAK kinases are now well-established targets in immunology, but the class has always had safety concerns hanging over it. The safety issues were exacerbated by a recent FDA decision to expand the black box warnings for the class for major cardiovascular events. Inhaled, lung-restricted JAK inhibitors have been of interest because they could [...]

The Shionogi P2X3 ligand-gated ion channel antagonist, sivopixant ( S-600918 ), is an oral Ph. II candidate for refractory chronic cough, which recently completed a its Ph. IIb study, overcoming the projected high dose requirement of a prior preclinical candidate. The molecule has a very polar core structure with both a dioxotriazine and [...]