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Review

Comparative clinical pharmacokinetics of antibody-drug conjugates in first-in-human Phase 1 studies

Pages 859-870 | Received 21 Feb 2014, Accepted 22 Apr 2014, Published online: 25 Apr 2014

Figures & data

Table 1. Properties of ADC and dosing regimen in first-in-man studies

Table 2. Comparative PK parameters of ADCs at MTD or nearest dose level, at Cycle 1

Table 3. Incidence of patients with persistent anti-therapeutic antibody response, following ADC administration in Phase 1

Figure 1. ADC dose ranges and maximum tolerated doses in first-in-humans studies. Gray symbol: MTD; open symbol: MTD not reached.

Figure 1. ADC dose ranges and maximum tolerated doses in first-in-humans studies. Gray symbol: MTD; open symbol: MTD not reached.

Figure 2. ADC dose escalation profiles in first-in-human studies.

Figure 2. ADC dose escalation profiles in first-in-human studies.

Figure 3. Dose-exposure relationship for ADC administered every 3 wk.

Figure 3. Dose-exposure relationship for ADC administered every 3 wk.

Figure 4. Effect of dose on ADC clearance, by target antigen type (HT, hematological tumor; ST, solid tumors. (Boxes indicate maximum tolerated dose in mg/kg)

Figure 4. Effect of dose on ADC clearance, by target antigen type (HT, hematological tumor; ST, solid tumors. (Boxes indicate maximum tolerated dose in mg/kg)

Figure 5. Unconjugated drug plasma exposure vs. ADC plasma exposure.

Figure 5. Unconjugated drug plasma exposure vs. ADC plasma exposure.

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