Features and properties of sacituzumab govitecan

Alternative names	hRS7-SN38 antibody drug conjugate; IMMU-132; Isactuzumab govitecan; Sacituzumab govitecan-hziy; TRODELVY; TROP-2-SN-38
Class	Antineoplastics; Camptothecins; Drug conjugates; Immunoconjugates; Immunotherapies; Indolizines; Monoclonal antibodies; Pyrans; Quinolines
Mechanism of Action	Trop-2 directed antibody conjugated to a DNA topoisomerase I inhibitor
Route of Administration	Intravenous
Pharmacodynamics	Antibody–drug conjugate; delivers more SN-38 (irinotecan active metabolite) than irinotecan; delivers SN-38 in its most active nonglucuronidated form; potent in vitro and/or in vivo cytotoxicity against diverse solid tumours, including carcinomas
Pharmacokinetics	Volume of distribution 0.045 L/kg, half-life 16 h and clearance 0.002 L/h/kg for whole product; half-life 18 h for free SN-38
Most frequent adverse events	Nausea, neutropenia, diarrhoea, fatigue, anaemia, vomiting, alopecia, constipation, rash, decreased appetite, and abdominal pain in patients with mTNBC
ATC codes
WHO ATC code	L01 (Antineoplastic Agents)
EphMRA ATC code	L1 (Antineoplastics)
Chemical Name	(2R)-2-amino-3-[1-[[4-[[1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[2-[2-[[(2S)-6-amino-1-[4-[[(19S)-10,19-diethyl-7-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-19-yl]oxycarbonyloxymethyl]anilino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]acetyl]amino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoyl]cyclohexyl]methyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoic acid