Table 1 Pharmacokinetic profiles of BGM0504 in SD rats and cynomolgus monkeys after intravenous (i.v.) or subcutaneous (s.c.) injections.

From: Molecular dynamics-guided optimization of BGM0504 enhances dual-target agonism for combating diabetes and obesity

 

SD rats

Cynomolgus monkey

Dose (mg/kg)

0.2 (i.v.) n = 6

0.3 (s.c.) n = 6

1.5 (s.c.) n = 6

7.5 (s.c.) n = 6

0.1 (i.v.) n = 6

0.2 (s.c.) n = 6

1.0 (s.c.) n = 6

5.0 (s.c.) n = 6

CMAX (ng/mL)

4650 ± 411

814 ± 111

3830 ± 705

15,100 ± 1750

2860 ± 261

1440 ± 109

5970 ± 1090

33,500 ± 3060

TMAX (h)

–

24.0 ± 0.0

24.0 ± 0.0

20.0 ± 6.2

–

16.0 ± 6.2

22.0 ± 14.0

20.0 ± 6.2

T1/2 (h)

13.6 ± 2.3

14.5 ± 1.4

13.4 ± 1.5

14.7 ± 2.4

37.9 ± 2.5

38.7 ± 1.8

41.7 ± 2.9

43.4 ± 5.9

Vdss (L/kg)

0.0648 ± 0.0058

–

–

–

0.0608 ± 0.0050

–

–

–

Cl (mL/min/kg)

0.0680 ± 0.0103

–

–

–

0.0207 ± 0.0022

–

–

–

AUC0–last (ng h/mL)

38,800 ± 5150

14,100 ± 2440

63,900 ± 11,400

269,000 ± 43,000

34,600 ± 2470

26,100 ± 1740

109,000 ± 21,900

603,000 ± 94,200

AUC0–∞ (ng h/mL)

49,800 ± 7470

33,200 ± 6190

153,000 ± 27,700

637,000 ± 88,700

80,400 ± 7880

113,000 ± 7940

488,000 ± 51,200

2,720,000 ± 246,000

Bioavailability

–

44.5%

41.1%

34.3%

–

69.7%

60.5%

67.6%

  1. –: not available.
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