Table 3.

Emibetuzumab PK for cycle 1 day 1 by dose

Emibetuzumab monotherapy
Dose20 mg70 mg210 mg700 mg1,400 mg2,000 mg
N633533
tmaxa (h)3.52 (1.50–3.62)1.58 (1.55–3.50)5.33 (5.25–5.47)3.60 (3.25–5.25)6.25 (4.50–6.50)4.53 (2.58–6.25)
Cmax (ng/mL)7,280 (83)20,700 (30)65,000 (18)185,000 (28)283,000 (42)892,000 (10)
AUC(0–tlast) (μgEmbedded Imageh/mL)146 (25)1,250 (37)8,020 (15)29,400 (35)44,200 (50)113,000 (21)
AUC(0–∞) (μgEmbedded Imageh/mL)162 (16)1,320 (32)9,380 (17)46,400 (42)74,400 (53)223,000 (9)
t1/2 (h)18.0 (17)45.4 (9)122 (11)246 (36)255 (16)342 (49)
CL (L/hr)0.123 (16)0.0529 (32)0.0224 (17)0.0151 (42)0.0188 (53)0.00895 (9)
Vss (L)3.31 (16)3.72 (25)3.80 (16)5.24 (36)6.86 (48)4.23 (39)
Emibetuzumab in combination with erlotinib 150-mg QD
Dose700 mg1,400 mg2,000 mg
N536
tmaxa (h)5.5 (1.53–7.50)7.93 (2.50–8.50)2.57 (2.50–4.75)
Cmax (ng/mL)205,000 (17)621,000 (27)646,000 (14)
AUC(0–tlast) (μgEmbedded Imageh/mL)28,900 (29)87,800 (13)103,000 (19)
AUC(0–∞) (μgEmbedded Imageh/mL)48,900 (21)120,000 (12)157,000 (20)
t1/2 (h)224 (19)173 (16)226 (27)
CL (L/hr)0.0143 (21)0.0117 (12)0.0128 (20)
Vss (L)4.62 (14)2.92 (19)4.09 (28)
  • NOTE: Values are reported as geometric mean (%CV).

  • Abbreviations: AUC(0–∞), area under the concentration–time curve from time of dose to infinity; AUC(0–tlast), area under the concentration–time curve from time of dose to the last quantifiable concentration measurement; CL, systemic clearance; Cmax, maximum observed serum concentration; CV, coefficient of variation; min, minimum; max, maximum; t1/2, half-life; tmax, time to Cmax; Vss, volume of distribution at steady state.

  • aMedian (Min - Max).