Loading
The GGFG tetrapeptide (glycine-glycine-phenylalanine-glycine) is the tether between antibody and payload in Enhertu and Dato-DXd. Lysosomal cathepsins cut it inside the cancer cell, and it holds in circulation well enough to allow eight payloads per antibody, a load earlier linkers could not carry safely.
The glycine-glycine-phenylalanine-glycine tetrapeptide is cleaved by lysosomal cathepsins, releasing DXd through a self-immolative aminomethylene spacer. Its stability in circulation allows a drug-to-antibody ratio of eight with acceptable off-target exposure, a combination that earlier linkers could not deliver.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
Showing the molecule this term concerns: Trastuzumab deruxtecan.
Shares DXd, Raludotatug deruxtecan, Patritumab deruxtecan, Ifinatamab deruxtecan.
Shares Datopotamab deruxtecan, Trastuzumab deruxtecan, Antibody-drug conjugate (ADC).
Shares Patritumab deruxtecan, Trastuzumab deruxtecan, Antibody-drug conjugate (ADC).
Shares Raludotatug deruxtecan, Antibody-drug conjugate (ADC).
Shares Raludotatug deruxtecan, Antibody-drug conjugate (ADC).
Shares Raludotatug deruxtecan, Antibody-drug conjugate (ADC).