TABLE 2.
Summary of lenacapavir pharmacokinetic parameters in moderate hepatic impairment, severe renal impairment, and healthy matched control groups
| Pharmacokinetic parametera |
Cmax (ng/mL) |
Tmax (h) |
AUClast (h*ng/mL) |
AUCinf (h*ng/mL) |
CL/Fb (L/h) |
Vz/Fb (L) |
t1/2b (days) |
|---|---|---|---|---|---|---|---|
| Hepatic impairment | |||||||
| Moderate hepatic impairment (n = 10) | 61.1 (21.0, 229) |
6.00 (2.00, 48.0) |
11,900 (4940, 29,200) |
12,000 (4,990, 29,600) |
25.0 (10.1, 60.2) |
10,800 (4,060, 23,000) |
12.6 (9.74, 17.1) |
| Normal hepatic function (n = 10) | 23.4 (9.70, 55.2) |
4.00 (4.00, 12.0) |
7,590 (3,050, 20,500) |
8,180 (3,150, 20,700) |
36.6 (14.5, 95.3) |
17,000 (6,970, 49,800) |
13.1 (10.7, 17.0) |
| Moderate hepatic impairment/normal hepatic function; GMR (90% CI) | 2.61 (1.51, 4.52) |
NC | 1.57 (1.01, 2.43) |
1.47 (0.947, 2.27) |
NC | NC | NC |
| Renal impairment | |||||||
| Severe renal impairment (n = 10) | 51.5 (6.80, 427) |
8.00 (4.00, 48.0) |
11,500 (1,310, 62,400) |
12,100 (1,430, 63,000) |
24.8 (4.76, 210) |
8,560 (1,690, 46,000) |
9.73 (5.69, 16.6) |
| Normal renal function (n = 10) | 19.7 (5.90, 34.4) |
6.00 (4.00, 48.0) |
6,050 (2,420, 12,300) |
6,590 (2,660, 13,200) |
45.5 (22.6, 113) |
20,900 (10,000, 52,300) |
13.3 (11.0, 17.0) |
| Severe renal impairment/normal renal function; GMR (90% CI) | 2.62 (1.12, 6.14) |
NC | 1.89 (0.952, 3.77) |
1.84 (0.936, 3.60) |
NC | NC | NC |
Pharmacokinetic parameters presented to three significant figures. AUCinf, AUClast, Cmax, CL/F, and Vz/F presented as geometric mean (minimum, maximum); Tmax (time to maximal concentration) and t1/2 (half-life) presented as median (minimum, maximum). AUCinf, area under the plasma concentration–time curve from time 0 to infinity; AUClast, area under the plasma concentration–time curve from time 0 to the last quantifiable plasma concentration; CI, confidence interval; CL/F, apparent oral clearance; Vz/F, apparent volume of distribution; Cmax, maximum concentration; GMR, geometric least-squares means ratio; NC, not calculated; t1/2, half-life; Tmax, time to maximum concentration.
Nonparametric comparisons of PK parameters between hepatic and renal function groups are presented in (Table S5).