molecules of the month


FR-targeted DNA crosslinking agent conjugate

activity in xenograft w/ once weekly dosing

from conjugation of FR-ligand and PBD dimer

Sci. Rep., Jul. 29, 2020

Endocyte, West Lafayette, IN / Novartis

Structure of EC2629, a folate receptor (FR)-targeted small molecule drug conjugate
1 min read

EC2629 is a folate receptor (FR)-targeted small molecule drug conjugate with a folate receptor-targeting moiety, a pyrrolobenzodiazepine (PBD) DNA-crosslinking warhead, and a linker. Similar to antibody-drug conjugates, this small molecule conjugate is intended to maintain the activity of the potent PBD warhead while minimizing systemic toxicity by targeting tumor cells expressing the folate receptor. I think the small molecule drug conjugate concept is an interesting one, though previous clinically tested molecules like vintafolide haven’t shown much promise yet. There’s probably a strong use case for this modality somewhere to be discovered!

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