. 2019 Nov 22;59(3):311–326. doi: 10.1007/s40262-019-00842-5

Table 1.

Summary of risankizumab phase I studies

Study	Objective(s)	Study design	Dosage regimen and route of administration	Treatment duration	No. of subjects	Analyses
1	To assess the safety, tolerability, and pharmacokinetics of risankizumab in healthy Caucasian, Chinese, and Japanese male subjects following single rising SC (Stage 1) and IV (Stage 2) doses of risankizumab	Phase I randomized, double-blind, placebo-controlled, two-center study consisting of two stages: Stage 1: SC dosing Stage 2: IV dosing Active: placebo randomization 6:2 in Stages 1 and 2	Risankizumab doses: 18 mg SC: Caucasian (n = 6), Japanese (n = 6), and Chinese (n = 6) 90 mg SC: Japanese (n = 6), Chinese (n = 7) 300 mg SC: Caucasian (n = 6), Japanese (n = 6), Chinese (n = 6) Placebo SC (n = 16) 200 mg IV: Japanese (n = 6) 600 mg IV: Japanese (n = 6) 1200 mg IV: Japanese (n = 6) Placebo IV (n = 6)	Single dose	89 Treated 85 Completed	NCA, PopPK, IIA
2	To assess the safety, tolerability, clinical efficacy, and pharmacokinetics of risankizumab in subjects with moderate-to-severe chronic plaque psoriasis following single IV (Stage 1) and SC doses (Stage 2)	Randomized, double-blind, multicenter, placebo-controlled, ascending dose study consisting of two stages: Stage 1: IV dosing (3:1 active:placebo) Stage 2: SC dosing (6:1 active:placebo)	Risankizumab doses: 0.01 mg/kg IV (n = 3) 0.05 mg/kg IV (n = 3) 0.25 mg/kg IV (n = 3) 1 mg/kg IV (n = 3) 3 mg/kg IV (n = 3) 5 mg/kg IV (n = 3) Placebo IV (n = 6) 0.25 mg/kg SC (n = 7) 1 mg/kg SC (n = 6) Placebo SC (n = 2)	Single dose	39 Treated 38 Completed	NCA, PopPK, IIA
8	To assess the effect of risankizumab on the pharmacokinetics of CYP probe substrates, caffeine (for CYP1A2), warfarin (for CYP2C9), omeprazole (for CYP2C19), metoprolol (for CYP2D6), and midazolam (for CYP3A).	Open-label, one-sequence study in subjects with moderate-to-severe chronic plaque psoriasis with or without concomitant psoriatic arthritis	Caffeine 100 mg, warfarin 10 mg, omeprazole 20 mg, metoprolol 50 mg, midazolam 2 mg as a single dose, as a cocktail, on days 1 and 98 Risankizumab 150 mg SC every 4 weeks on days 8, 36, 64, and 92	Two single doses (CYP cocktail); multiple doses every 4 weeks (risankizumab)	21 Treated 21 Completed	NCA

Study

Objective(s)

Study design

Dosage regimen and route of administration

Treatment duration

No. of subjects

Analyses

To assess the safety, tolerability, and pharmacokinetics of risankizumab in healthy Caucasian, Chinese, and Japanese male subjects following single rising SC (Stage 1) and IV (Stage 2) doses of risankizumab

Phase I randomized, double-blind, placebo-controlled, two-center study consisting of two stages:

Stage 1: SC dosing

Stage 2: IV dosing

Active: placebo randomization 6:2 in Stages 1 and 2

Risankizumab doses:

18 mg SC: Caucasian (n = 6), Japanese (n = 6), and Chinese (n = 6)

90 mg SC: Japanese (n = 6), Chinese (n = 7)

300 mg SC: Caucasian (n = 6), Japanese (n = 6), Chinese (n = 6)

Placebo SC (n = 16)

200 mg IV: Japanese (n = 6)

600 mg IV: Japanese (n = 6)

1200 mg IV: Japanese (n = 6)

Placebo IV (n = 6)

Single dose

89 Treated

85 Completed

NCA, PopPK, IIA

To assess the safety, tolerability, clinical efficacy, and pharmacokinetics of risankizumab in subjects with moderate-to-severe chronic plaque psoriasis following single IV (Stage 1) and SC doses (Stage 2)

Randomized, double-blind, multicenter, placebo-controlled, ascending dose study consisting of two stages:

Stage 1: IV dosing (3:1 active:placebo)

Stage 2: SC dosing (6:1 active:placebo)

Risankizumab doses:

0.01 mg/kg IV (n = 3)

0.05 mg/kg IV (n = 3)

0.25 mg/kg IV (n = 3)

1 mg/kg IV (n = 3)

3 mg/kg IV (n = 3)

5 mg/kg IV (n = 3)

Placebo IV (n = 6)

0.25 mg/kg SC (n = 7)

1 mg/kg SC (n = 6)

Placebo SC (n = 2)

Single dose

39 Treated

38 Completed

NCA, PopPK, IIA

To assess the effect of risankizumab on the pharmacokinetics of CYP probe substrates, caffeine (for CYP1A2), warfarin (for CYP2C9), omeprazole (for CYP2C19), metoprolol (for CYP2D6), and midazolam (for CYP3A).

Open-label, one-sequence study in subjects with moderate-to-severe chronic plaque psoriasis with or without concomitant psoriatic arthritis

Caffeine 100 mg, warfarin 10 mg, omeprazole 20 mg, metoprolol 50 mg, midazolam 2 mg as a single dose, as a cocktail, on days 1 and 98

Risankizumab 150 mg SC every 4 weeks on days 8, 36, 64, and 92

Two single doses (CYP cocktail); multiple doses every 4 weeks (risankizumab)

21 Treated

21 Completed

NCA

IV intravenous, SC subcutaneous, NCA non-compartmental analyses, PopPK population pharmacokinetic analyses, IIA integrated immunogenicity analyses, CYP cytochrome P450