We are happy to continue our series of posts which are inspired by Drug Hunter’s “Molecules of the Month”!
Here are two molecules that were recently highlighted by Drug Hunter!
1. Neflamapimod (VX-745) is an oral, potent, and highly selective BBB penetrating inhibitor of p38α kinase. It reduces the activity of Rab5, the endosome-associated GTPase, which plays an essential role in the pathway leading to the degeneration of basal forebrain cholinergic neurons (BFCN). Inhibiting Rab5 has the potential in treating neurodegenerative disorders associated with loosing of BFCN, including Lewy body dementia (LBD). Neflamapimod displays the reverse of endosomal pathology and restores the numbers and morphology of BFCNs in a mouse model. Now it is in Phase 2a clinical trial in mild-to-moderate dementia with Lewy bodies.
You can find the analogs to this molecule here!
2. Vadadustat (AKB-6548) is an orally active inhibitor of the hypoxia-inducible factor prolyl-4-hydroxylase domain (HIF PHD). Inhibition of PHD enzymes stabilizes HIFs and transcription factors that activate target genes that increase erythropoietin (EPO) synthesis, which leads to the production of new red blood cells (RBCs). Vadadustat interacts with all three human PHD isozymes (PHD1, PHD2, PHD3) and inhibits their activity in low nanomolar concentrations. It showed good results in increased circulating levels of EPO and RBC indices in animal models. Currently, this drug candidate is in Phase 3 for the treatment of anemia in patients with chronic kidney disease (CKD).
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!
