Tubulin inhibitor payloads were the first generation of modern ADC payloads: drugs that jam the cell's scaffolding so it cannot divide. Nerve and eye side effects are typical.
Auristatins (MMAE, MMAF) and maytansinoids (DM1, DM4) bind tubulin and arrest mitosis, so they work best in rapidly dividing tumours. Whether the released form crosses membranes decides the bystander effect: MMAE and DM4 do, MMAF and DM1 do not. Peripheral neuropathy (MMAE), keratopathy (MMAF, DM4) and thrombocytopenia (DM1) are the characteristic toxicities. Most are substrates for P-glycoprotein.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
Showing the molecule this term concerns: Enfortumab vedotin.
Shares MMAE, Tisotumab vedotin, Bystander effect (ADC), Telisotuzumab vedotin.
Shares DM1, Trastuzumab emtansine, Antibody-drug conjugate (ADC).
Shares Mirvetuximab soravtansine, Enfortumab vedotin, Trastuzumab emtansine, Antibody-drug conjugate (ADC).
Shares Mirvetuximab soravtansine, Payload (ADC), Enfortumab vedotin, Antibody-drug conjugate (ADC).
Shares MMAF, Belantamab mafodotin, Antibody-drug conjugate (ADC).
Shares MMAE, Bystander effect (ADC), Drug efflux pumps (ABC transporters), Payload (ADC).
Shares DM4, Mirvetuximab soravtansine, Antibody-drug conjugate (ADC).
Shares Bystander effect (ADC), Drug efflux pumps (ABC transporters), Payload (ADC), Antibody-drug conjugate (ADC).