Drug intelligence / Profile preview

zaurategrast

Development stage
Phase 2
Lead developer
UCB
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Zaurategrast is a small-molecule oral prodrug antagonist of the vascular cell adhesion molecule 1 (VCAM‑1), acting by inhibiting α4-integrins (specifically integrin alpha4-beta1, also known as very late antigen 4 or VLA4). It was developed by Celltech (now part of UCB). The drug was investigated for the treatment of multiple sclerosis, aiming to prevent immune cell migration into inflamed tissues such as the brain. This mechanism is similar to that of natalizumab but delivered as an oral agent rather than an antibody. Zaurategrast’s active metabolite is CT7758. Clinical trials included Phase 1 and Phase 2 studies in relapsing multiple sclerosis; however, interim results showed no significant benefit over placebo after six months[1][2][3][5].

Other names
zaurategrast [INN]455264-31-0UNII-06A0IC74I3UNII06A0IC74I3UNII 06A0IC74I3(S)-3-(4-((2,7-Naphthyridin-1-yl)amino)phenyl)-2-((2-bromo-3-oxospiro[3.5]non-1-en-1 yl)amino)propanoic acid
02

Targets

α4β1 (Integrin α4β1)

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