Fmoc-VC-PAB-Eribulin Usage And Synthesis

Uses

Fmoc-VC-PAB-Eribulin is an Antibody-drug Conjugate (ADC) that can specifically recognize and kill target cancer cells without harming the organism, resulting in minimal toxic side effects. It is composed of an antibody, an ADC Cytotoxin (payload), and a Linker that connects these two components. Valine-citrulline (Val-Cit) is an amino acid unit often found in cleavable peptide fragments in the connectome. Eribulin, on the other hand, is a structurally simplified and fully synthetic analog of macrocyclic ketone halichondrin B. In 2010, the FDA approved eribulin for the treatment of metastatic breast cancer (MBC). Eribulin acts as a microtubule dynamics inhibitor and also exhibits tumor microenvironment modulation activities, such as vascular remodeling activity [1-2].

References

[1] Yu Q, et al. Gram-Scale Synthesis of the C14–C23 Fragment of Eribulin. Organic Process Research & Development, 2023; 27: 367–372.
[2] Niwa Y, et al. Liposome-Encapsulated Eribulin Shows Enhanced Antitumor Activity over Eribulin for Combination Therapy with Anti–PD-1 Antibody. Molecular Cancer Therapeutics, 2023; 2: 499–510.