Antibody-Drug Conjugates (ADCs) are targeted drugs composed of a drug linked to an antibody (mAbs) that release their payload at a specific tumor type.
For more information on how different generations of ADCs were developed, please refer to the article ADC Technology Review in 2021. Trodelvy, similarly to Zynlonta, has incorporated monodispersed polyethylene glycol (PEG) chains into its linker.
Sacituzumab govitecan (IMMU-132), an antitrophoblastic cell-surface antigen (anti-Trop-2) humanized antibody-SN-38 conjugate, has been approved for the treatment of adult patients with metastatic triple-negative breast cancer (mTNBC). This ADC works by releasing the anti-cancer drug SN-38 using a cleavable linker which was designed to release at lysosomal pH. Figure 1 shows the site on the linker that is cleaved under the right conditions. Because of the linker design, the ADC showed superior delivery of SN-38 relative to the control, irinotecan.
This linker is comprised of several interesting synthetic features; such as the monodispersed PEG linker, the click chemistry used to form the triazole, and the SMCC group that binds the linker to the antibody.
As a worldwide leader of PEG linker and click chemistry tools, BroadPharm offers a wide array of different ADC Linkers to empower our customer's advanced research. These compounds feature great aqueous solubility, smart choice of PEG length, and a broad selection of functional groups to choose from.