Glutamic acid–valine–citrulline linkers (EVCit Linker) ensure stability and efficacy of antibody–drug conjugates in vivo.
Valine–citrulline linkers are widely used as enzymatically cleavable linkers for antibody–drug conjugates. Although they are stable in human plasma, these linkers are unstable in mouse plasma. The potential premature release of drugs in mouse circulation poses challenges in ADC drug design.
Yasuaki Anami, etc in “Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice“, reported that an antibody–drug conjugate with glutamic acid–valine–citrulline linkers preserve the enzymatic drug release while avoiding the premature cleavage in mice. The study also shows their ADC with EVCit-PAB linker exhibits greater treatment efficacy in mouse tumor models than does a valine–citrulline-based variant.
AxisPharm maintain Fmoc-EVCit-PAB linker in stock and can custom synthesize corresponding pegylated EVCit-PAB linker with competitve price.