TABLE 2.

Treatment-related adverse events

Preferred term	Single ascending dose										Multiple ascending dose
	10 mg	30 mg	60 mg	100 mg fasted	100 mg fed	150 mg	200 mg	250 mg	300 mg	Placebo	30 mg BID	60 mg BID	100 mg BID	Placebo
	(N = 8)	(N = 8)	(N = 8)	(N = 16)	(N = 16)	(N = 8)	(N = 8)	(N = 8)	(N = 8)	(N = 16)	(N = 10)	(N = 10)	(N = 10)	(N = 6)
	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)	n (%)
All AEsa	2 (25.0%)	3 (37.5%)	2 (25.0%)	5 (31.3%)	3 (18.8%)	1 (12.5%)	4 (50.0%)	2 (25.0%)	5 (62.5%)	5 (31.3%)	5 (50.0%)	4 (40.0%)	10 (100%)	2 (33.3%)
Drug related AEs	2 (25.0%)	2 (25.0%)	1 (12.5%)	4 (25.0%)	2 (12.5%)	1 (12.5%)	4 (50.0%)	2 (25.0%)	4 (50.0%)	5 (31.3%)	4 (40.0%)	2 (20.0%)	10 (100%)	2 (33.3%)
Serum creatinine increased	0	2 (25.0%)	0	0	0	0	2 (25.0%)	0	1 (12.5%)	0	2 (20.0%)	0	3 (30.0%)	1 (16.7%)
Neutrophil count decreased	0	0	0	0	0	0	0	0	2 (25.0%)	0	0	0	0	1 (16.7%)
WBC count decreased	0	0	0	0	0	0	0	0	2 (25.0%)	0	0	0	0	0
Blood bilirubin increased	0	0	0	1 (6.3%)	0	0	1 (12.5%)	0	0	1 (6.3%)	0	1 (10.0%)	0	0
Neutrophil count increased	0	0	0	0	0	0	0	0	1 (12.5%)	0	0	0	1 (10.0%)	0
Positive antinuclear antibodies	0	0	1 (12.5%)	0	0	0	0	0	0	0	0	0	0	0
WBC count increased	0	0	0	0	0	0	0	0	1 (12.5%)	0	0	0	1 (10.0%)	0
Reduced sperm forward movement	1 (12.5%)	0	0	0	0	0	0	0	0	1 (6.3%)	0	0	0	0
Blood creatine phosphokinase increased	0	0	0	0	0	0	0	0	1 (12.5%)	0	0	0	0	0
Alanine aminotransferase increased	0	0	0	0	0	0	0	0	0	1 (6.3%)	0	0	0	0
Aspartate aminotransferase increased	0	0	0	0	0	0	0	0	0	1 (6.3%)	0	0	0	0
Sperm count decreased	0	0	0	0	0	0	0	0	0	1 (6.3%)	0	0	0	0
Cacospermia	0	0	0	0	0	0	0	0	0	0	3 (30.0%)	1 (10.0%)	0	1 (16.7%)
Abnormal sperm morphology	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0	0	0
Lipase increased	0	0	0	0	0	0	0	0	0	1 (6.3%)	0	0	0	0
Hyperuricemia	0	0	0	1 (6.3%)	0	0	0	1 (12.5%)	0	1 (6.3%)	0	0	0	0
Hypoalbuminemia	0	0	0	0	1 (6.3%)	0	0	0	0	0	0	0	0	0
Hypoglycemia	0	0	0	1 (6.3%)	0	0	0	0	0	0	0	0	0	0
Hyponatremia	0	0	0	0	0	0	1 (12.5%)	0	0	0	0	0	3 (30.0%)	0
Hypokalemia	0	0	0	1 (6.3%)	0	0	0	0	0	0	0	0	0	0
Hyperglycemia	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0	1 (10.0%)	0
Hypophosphatemia	0	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0
Hypocalcemia	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0	0
Hypertriglyceridemia	0	0	0	0	0	0	0	0	1 (12.5%)	0	0	1 (10.0%)	0	1 (16.7%)
Urinary tract infection	0	0	0	2 (12.5%)	1 (6.3%)	1 (12.5%)	0	0	1 (12.5%)	1 (6.3%)	1 (10.0%)	0	0	0
Upper respiratory infection	0	1 (12.5%)	0	0	0	0	0	0	0	0	0	0	0	0
Anemia	0	0	0	1 (6.3%)	1 (6.3%)	0	0	1 (12.5%)	0	0	0	0	0	0
Headache	1 (12.5%)	0	0	0	0	0	0	0	0	0	0	0	0	0
Dizziness	0	0	0	0	0	0	0	0	0	0	0	0	9 (90.0%)	0
Asthenospermia	0	0	1 (12.5%)	0	0	0	0	0	0	0	2 (20.0%)	0	0	0
Haematuria	0	1 (12.5%)	0	0	0	0	0	0	0	0	0	0	0	0
Supraventricular extrasystole	0	0	0	0	0	0	0	0	0	1 (6.3%)	0	0	0	0
Nausea	0	0	0	0	0	0	0	0	0	0	0	0	9 (90.0%)	0
Vomit	0	0	0	0	0	0	0	0	0	0	0	0	6 (60.0%)	0
Gastroesophageal reflux disease	0	0	0	0	0	0	0	0	0	0	0	0	3 (30.0%)	0
Abdominal discomfort	0	0	0	0	0	0	0	0	0	0	0	0	2 (20.0%)	0
Upper abdominal pain	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0	0
Retching	0	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0
Cheat discomfort	0	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0
Pharyngeal erythema	0	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0
Tonsil hypertrophy	0	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0
Tinnitus	0	0	0	0	0	0	0	0	0	0	0	0	1 (10.0%)	0

^aAE, adverse event; data are n (%).