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Clinical Pharmacology
21 Day PK
Enfortumab vedotin (EV)
1.25 mg/kg Q1W x3
SYS6002 [CRB-701)
1.2 mg/kg Q3W
SYS6002 (CRB-701)
2.7 mg/kg Q3W
Comparison
EV
benchmark
Matched
ADC dose
Matched
MMAE dose
Cmax
100%
79%
177%
% ADC
AUC 21d
100%
106%
183%
Cmax
100%
The half-lives of TAb, ADC, and MMAE were 4-6 days, 4-5 days and 5-10 days, respectively
No obvious accumulation was observed on C3D1
33%
79%
% Free MMAE
AUC 21d
100%
Time-to-peak concentration of MMAE was about 3-7 days
When compared to EV exposures SYS6002 (CRB-701) consistently demonstrates lower free MMAE
29%
After single IV infusion of SYS6002 (CRB-701), the exposure of TAb, ADC and MMAE generally increased in a dose proportional manner
Clearance and volume of distribution were similar across doses
68%View entire presentation