We are happy to continue our series of posts, which are inspired by Drug Hunter’s “Small Molecules of the Month”!
Here are two molecules that were recently highlighted by Drug Hunter:
1. Belvarafenib is a potent and selective RAF dimer (type II) inhibitor that exhibits clinical activity in patients with BRAF V600E- and NRAS-mutant melanomas. It inhibits 7 other kinases (CSF1R, DDR1, DDR2, EPHA2, EPHA7, EPHA8, and EPHB2) out of 187 kinases analyzed with more than 90% inhibition at 1 μM. Now it is in human trials (Phase I) for treating BRAF V600E- and RAS-mutated advanced solid tumors.
You can find the analogs to this molecule here!
2. Icenticaftor (QBW251) is an oral drug candidate for the treatment of chronic obstructive pulmonary disease (COPD) and cystic fibrosis (CF). Icenticaftor functions by acting as a stimulator of the protein cystic fibrosis transmembrane conductance regulator (CFTR). Now it in Phase II in COPD patients with chronic bronchitis and a history of exacerbations.
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!