Table 3.

Simulated blood concentrations and brain V1a receptor occupancies over 5 days following three 60-min IV infusions of balovaptan 50, 25, and 15 mg on days 1, 2, and 3

	Day 1		Day 2		Day 3		Day 5
	1 h	24 h	25 h	48 h	49 h	72 h	96 h
Blood concentration (ng/mL), median and 5th to 95th percentile range
Ref 76 kg	352 (215–566)	74 (23–147)	261 (176–392)	59 (17–149)	166 (107–268)	42 (12–117)	15 (3–57)
Ref 82.2 ± 20.3 kg	332 (175–624)	74 (22–144)	254 (161–406)	61 (16–145)	167 (1–2–270)	43 (12–118)	15 (3–63)
Brain receptor occupancy (%), median and 5th to 95th percentile range
Ref 76 kg	99 (98–99)	96 (88–98)	99 (98–99)	95 (83–98)	98 (97–99)	93 (79–97)	82 (48–95)
Ref 82.2 ± 20.3 kg	99 (98–99)	96 (87–98)	99 (98–99)	95 (83–98)	98 (97–99)	93 (78–97)	82 (46–95)

Data at 24 h and 48 h above are pre-infusion; data at 1, 25 and 49 h are immediately post-infusion