. 2021 Jul 29;88(4):1667–1678. doi: 10.1111/bcp.14980

TABLE 4.

Median cabotegravir tissue‐ and fluid‐to‐plasma ratios after oral dosing and IM injection across all visits vs. 114433 study results

Study	Treatment	Ratio (range)
Study	Treatment	Cervical tissue to plasma (n = 7)	Vaginal tissue to plasma (n = 7)	Cervicovaginal fluid to plasma (n = 7)	Rectal tissue to plasma (n = 13)	Rectal fluid to plasma (n = 12)
201767 (present) ^a	Oral 30 mg	0.18 (0.11–0.25)	0.14 (0.03–0.18)	0.13 (0.02–0.36)	0.10 (0.07–0.17)	0.45 (0.15–10.40)
201767 (present) ^a	IM 600 mg	0.14 (<LLOQ‐0.31)	0.16 (<LLOQ‐0.34)	0.08 (0.01–0.44)	0.09 (<LLOQ‐0.16)	0.32 (<LLOQ‐11.38)
		*Cervical tissue to plasma (n =* 4 each)**	*Vaginal tissue to plasma (n =* 4 each)**		*Rectal tissue to plasma (n =* 4 each)**
114433²⁶ (previous)	IM 400 mg (unsplit) ^b	0.20 (<LLOQ‐0.40)	0.28 (<LLOQ‐0.70)	—	<LLOQ (<LLOQ‐0.10)	—
114433²⁶ (previous)	IM 400 mg (split) ^c	0.16 (<LLOQ‐0.40)	0.19 (<LLOQ‐0.70)	—	0.08 (<LLOQ‐0.20)	—

IM, intramuscular; LLOQ, lower limit of quantification.

^{^a}

LLOQs were 0.025, 0.0000625, and 0.000050 μg/mL, for plasma, tissues, and fluids, respectively.

^{^b}

Administered as a single injection. Samples were collected on Weeks 2 and 8.

^{^c}

Administered as 2 200‐mg injections. Samples were collected on Weeks 4 and 12.