Table 4 PK assessment with all LY3127804 doses at different administration times.

From: First-in-human, dose-escalation, phase 1 study of anti-angiopoietin-2 LY3127804 as monotherapy and in combination with ramucirumab in patients with advanced solid tumours

LY dose (mg/kg)

Day

N

Cmax (ng/mL)

AUC(0-336) (µg·h/mL)

AUC(0-∞) (µg·h/mL)

CL (mL/h)

t1/2 (h)

4

1

3

96,867 (57)

11,631 (30)

16,737 (34)

16.5 (28)

199 (16)

15

3

100,120 (22)

16,647 (33)

16.8 (25)

202 (21)

29

3/2a

109,960 (27)

16,136 (27)a

15.3 (31)a

211 (27)a

43

2

96,380 (26)

8

1

9/6a

187,210 (20)

29,817 (25)a

44,854 (31)

15.3 (13)a

202 (21)a

15

9

225,140 (28)

42,486 (22)

14.4 (22)

240 (36)

29

6/5a

310,580 (36)

53,889 (41)a

12.2 (40)a

211 (55)a

43

9

303,320 (21)

12

1

9

231,190 (29)

33,036 (31)

50,661 (40)

18.5 (43)

220 (33)

15

8/6a

294,290 (32)

47,084 (35)

20.3 (42)

199 (25)a

29

9/8a

342,140 (24)

62,327 (26)

15.5 (35)

209 (24)a

43

8

390,170 (13)

16

1

9

313,230 (22)

43,636 (25)

73,477 (46)

15.5 (38)

255 (41)

15

10

347,080 (39)

65,837 (39)

16.8 (24)

270 (26)

29

8/5a

480,120 (23)

93,032 (25)

13.0 (26)

248 (7.1)a

43

9

439,330 (22)

20

1

17

423,120 (35)

57,917 (23)

91,311 (32)

15.8 (33)

228 (50)

15

13

531,190 (17)

85,529 (22)

16.9 (25)

227 (25)

29

14/10a

631,940 (27)

106,655 (28)

13.4 (25)

238 (38)a

43

10

620,870 (16)

27

1

12

551,370 (36)

81,931 (28)

122,518 (34)

16.6 (38)

211 (39)

15

9

608,330 (38)

108,015 (24)

18.2 (21)

202 (42)

29

10/8a

721,420 (30)

120,607 (29)a

15.9 (23)a

185 (19)a

43

8

797,710 (19)

  1. All data reported as geometric mean (coefficient of variation %), unless specified.
  2. As CL of LY3127804 monotherapy and LY3127804 combination is similar, combined PK data are reported for parts A, B, and C.
  3. aN as (X1/X2*): Cmax was determined in X1 patients and t1/2 (hence AUC(0-∞) and CL) could only be determined in X2 patients.