. 2021 Apr 8;60(7):835–853. doi: 10.1007/s40262-021-01005-1

Table 1.

Key pharmacokinetic parameters of cabotegravir and rilpivirine administered either orally or intramuscularly [13, 17, 31, 34, 37, 46, 47].

Cabotegravir	Oral (30 mg QD)	Intramuscular (400 mg Q4W)	Intramuscular (600 mg Q8W)
Time to steady state	7 days	44 weeks	No data available
T_max	3 h^a	7 days^a	7 days (0–57)^b
C_max [µg/mL]	8.0 (5.3, 11.9)^b	4.2 (2.5, 6.5)^b	4.0 (2.3, 6.8)^b
AUC [µg × h/mL]	145 (93.5, 224)^b	2415 (1494, 3645)^b	3764 (2431, 5857)^b
C_trough [µg/mL]	4.6 (2.8, 7.5)^b	2.8 (1.7, 4.6)^b	1.6 (0.8, 3.0)^b
Elimination half-life	41 h^a	5.6–11.5 weeks^a
Drug metabolism	UGT1A1 > UGT1A9 No inhibitory/inducing effects on CYPs or UGTs
Drug transporters	Substrate of P-gp, BCRP, OAT3 No clinically significant inhibitory effects on drug transporters
Rilpivirine	Oral (25 mg QD)	Intramuscular (600 mg Q4W)	Intramuscular (900 mg Q8W)
Time to steady state	< 7 days	Approximately 80% of steady-state is reached at 48 weeks
T_max	4 h^b	3–4 days^a	No data available
C_max [ng/mL]	116 (48.6, 244)^b	120 (68.2, 208)^b	133 (77.8, 223)^b
AUC [ng × h/mL]	2083 (1125, 3748)^b	67,703 (39,029, 117,472)^b	127,031 (74,845, 211,644)^b
C_trough [ng/mL]	79.4 (31.8, 177)^b	84.9 (49.4, 146)^b	65.6 (36.9, 113)^b
Elimination half-life	45 h^a	13–28 weeks^a
Drug metabolism	CYP3A4 No inhibitory effect on CYPs or UGTs
Drug transporters	No clinically significant inhibitory effects on drug transporters

Pharmacokinetic parameters are expressed as geometric mean (5th, 95th percentile), except T_max, which is expressed as median (range)

AUC area under the curve, BCRP breast cancer resistance protein, C_max maximum concentration, C_trough trough concentration, CYPs cytochrome P450s, OAT organic anion transporter, P-gp P-glycoprotein, Q4W once every 4 weeks, Q8W once every 8 weeks, QD once daily, T_max time to maximum concentration, UGT UDP-glucuronosyltransferases

^aSingle dose

^bSteady state