We are happy to continue our series of posts which are inspired by Drug Hunter’s “Molecules of the Month”!
Below are two molecules that were recently highlighted by Drug Hunter!
1. Baxdrostat (CIN-107) is an oral, potent, and highly selective inhibitor of the aldosterone synthase (CYP11B2) enzyme, that is responsible for the synthesis of aldosterone in the adrenal gland. Dysregulation in the aldosterone synthesis can be the cause of hypertension, primary aldosteronism (PA), or chronic kidney disease (CKD). Baxdrostat (CIN-107) effectively decreases aldosterone levels by targeting aldosterone synthase without blocking the activity of 11ß-hydroxylase, which is responsible for the synthesis of cortisol. Phase II clinical trial in patients with treatment-resistant hypertension was well-tolerated and displayed a significant reduction in systolic blood pressure. Two other Phase II trials in hypertensive patients with PA and in CKD are currently underway.
You can find the analogs to this molecule here!
2. PF-6870961 is a newly discovered major hydroxy metabolite of PF-5190457, an inverse agonist of the ghrelin receptor (growth hormone secretagogue receptor 1a, GHSR1a). It was identified during clinical trials of PF-5190457 as a potential treatment for alcohol use disorder. In vitro and in vivo studies have shown, that PF-6870961 has a binding affinity and inverse agonist activity at GHSR1a, and a greater inhibitory potency at GHSR1a-induced β-arrestin recruitment compared to its parent compound. Additional in vivo studies have shown that PF-6870961 leads to suppressing food intake in rodent models, and its effects were mediated by the GHSR receptor. These findings suggest that PF-6870961 may contribute to the overall activity of PF-5190457 through its inhibiting of GHSR1a and increasing the impact in alcohol use disorder treatment.
You can find the analogs to this molecule here!
Use chem-space.com/search to find off-the-shelf and Make-on-Demand molecules of your interest!
