fbpx

molecules of the month

Pevonedistat

intravenous NEDD8-activating enzyme inhibitor

Ph. III candidate for oncology

from HTS and optimization

Drug Metab. Dispos.

Takeda, Lexington, MA

Pevonedistat Chemical Structure, intravenous NEDD8-activating enzyme inhibitor - Takeda, Lexington, MA
5 mins read

Context. Pevonedistat (Takeda) is a first-in-class intravenous or subcutaneous NEDD8-activating enzyme (NAE) inhibitor being developed for leukemia and advanced solid tumors. NAE is a pivotal regulator of the NEDD8 conjugation pathway which regulates the activity of the Cullin-RING ligases (CRLs), key proteins involved in the ubiquitin-proteasome system (UPS), controlling important physiological processes such as cell-cycle and signal transduction. Neddylation of CRLs is an attractive target pathway as CRLs are often abnormally activated in cancers. Pevonedistat, which was first reported in a 2009 publication, is the most advanced NAE inhibitor in clinical development. The only other NAE inhibitor to ever enter clinical development was Otsuka’s TAS4464, which was put on hold after a Ph. I trial was terminated following observation of…


request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.


already a member? log in: