MK-1454 (Merck) is an intratumoral stimulator of interferon (IFN) genes (STING) agonist that is being developed for treatment of advanced solid tumors and lymphomas. The molecule follows Aduro’s ADU-S100 , which was terminated after Ph. II due to a lack of substantial activity. Another chemotype of STING agonist, Eisai’s E7766 , has [...]

bradanicline (ATA-101 or TC-5619) is a molecule first disclosed a decade ago by Targacept. It is a selective agonist of the alpha-7 neuronal nicotinic acetylcholine receptor, and was intended as a drug candidate for treatment of cognitive impairment in neurological disorders. It is highly selective for the CNS over peripheral receptor [...]

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 [...]

LEO 134310 is a non-steroidal, selective glucocorticoid receptor (GR) agonist in Ph. I for plaque psoriasis. Glucocorticoid receptor modulators are widely used in tissue-restricted forms (think Flonase) for their acute effects, but prolonged engagement of GR is undesirable. Previously LEO Pharma described the identification of this topical [...]