termsTerm
Tubulin inhibitor payloads
aka auristatins, maytansinoids, microtubule payloads
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.
Category
ADC chemistry
technologies
1drugs
10ApprovedADC
Belantamab mafodotin · Blenrep
ApprovedADC
Brentuximab vedotin · Adcetris
Not filedADC
Disitamab vedotin
ApprovedADC
Enfortumab vedotin · Padcev
ApprovedADC
Mirvetuximab soravtansine · Elahere
Phase 3ADC
Sonesitatug vedotin
ApprovedADC
Telisotuzumab vedotin · Emrelis
ApprovedADC
Tisotumab vedotin · Tivdak
ApprovedADC
Trastuzumab emtansine · Kadcyla
Phase 3ADC
Zilovertamab vedotin