Table 3.

PK parameters in plasma following administration of a single oral dose of tepotinib (500 mg) and an IV tracer dose of [¹⁴C]-tepotinib (11.7 μg/mL, equivalent to 53–54 kBq [1.4 μCi])

PK parametera	Units	[14C]-tepotinib (IV tracer)	Tepotinib (oral)
Cmax	ng/mL	8580.3 (36.4),b 5816.0–15,946.5	555.7 (13.6), 469.0–675.0
tmax	Hours	–	10.0 (3.0–10.0)
tlag	Hours	–	0.52 (0.25–2.0)
AUC0–t	ng/mL × hours	35,137.8 (7.8),b 33,203.1–40,996.4	25,000.9 (16.9), 20,319–32,217
AUC0–∞	ng/mL × hours	35,316.9 (7.8),b 33,370.6–41,206.0	25,300.2 (16.7), 20,615–32,559
t½	Hours	31.2 (13.3), 24.2–35.2	28.3 (16.5), 20.5–32.3
CL or CL/f	L/hours	12.8 (7.8), 10.9–13.5	17.8 (16.7), 13.8–21.8
Vc	L	34.6 (44.3), 16.4–54.5	–
Vz or Vz/f	L	573.6 (14.4), 463.7–659.0	726.0 (24.8), 550.0–969.4

^aValues are geometric mean (geometric CV%), followed by min–max, except for t_max and t_lag, for which median values, followed by min–max, are provided

^bTo allow comparisons in this table, exposure parameters C_max, AUC_0–t, and AUC_0–∞ estimated after IV tracer administration were individually adjusted to the 500 mg oral dose, including a factor to normalize for salt:free base concentration

AUC_0–∞, area under the concentration–time curve from time 0 to infinity; AUC_0–t, area under the curve from 0 to t (last measurable concentration) hours; CL, total body clearance; CL/f, apparent body clearance; C_max, maximum plasma concentration; CV, coefficient of variation; IV, intravenous; PK, pharmacokinetic; t_½, elimination half-life; t_lag, lag time prior to the first measurable (non-zero) concentration; t_max, time to reach maximum concentration; V_c, volume of distribution of the central compartment; V_z, total volume of distribution; V_z/f, apparent volume of distribution