Table I.

In Vitro and In Vivo PK Studies

Study	T-DM1 dose producta	Number (n)	T-DM1 administration	Available datab
In vitro plasma stabilityc	T-DM1DAR 3.1	1	100 μg/mL	TT; DAR0–DAR7
Rat PKd	T-DM1DAR 1.5	5	10.0 mg/kg IV	TT; DAR0–DAR7
	T-DM1DAR 3.1	5	10.0 mg/kg IV	TT; DAR0–DAR7
Rat PK	T-DM1DAR 3.1	24	0.3 (n = 7), 3.0 (n = 8), and 20.0 mg/kg IV (n = 9)	TT; T-DM1
Cynomolgus monkey PK	T-DM1DAR 3.1	4	30.0 mg/kg IV	TT; T-DM1; DAR0–DAR7
	T-DM1DAR 3.1	14	Multiple-dose IV infusion: 10.0 mg/kg q3w x4	TT; T-DM1

See “MATERIALS AND METHODS” for details

PK pharmacokinetic, T-DM1 trastuzumab emtansine, DAR drug-to-antibody ratio, IV intravenous, q3w once every 3 weeks, TT total trastuzumab

^aT-DM1_DAR 1.5 and T-DM1_DAR 3.1 dose products have an average of 1.5 and 3.1 DM1/trastuzumab, respectively

^bTotal trastuzumab and T-DM1 were measured by ELISA; DAR₀–DAR₇ were measured by affinity capture LC-MS

^cSeparate experiments for rat and cynomolgus monkey plasma

^dTwo of five animals used for total trastuzumab measurements; three of five animals used for DAR₀–DAR₇ measurements