Table 2.

Treatment-Related Adverse Events Occurring in at Least 5% of Patients or Grade 3 in Severity

	Dose Escalation								Dose Expansion		All Patients
	80 mg ORIC-101 + 160 mg enzalutamide (N=4)		160 mg ORIC-101 + 160 mg enzalutamide (N=3)		240 mg ORIC-101 + 160 mg enzalutamide (N=3)		Total (N=10)		240 mg ORIC-101 + 160 mg enzalutamide (N=31)		Total (N=41)
Patients with at least one TRAE n (%)	All Grades	Grade 3	All Grades	Grade 3	All Grades	Grade 3	All Grades	Grade 3	All Grades	Grade 3	All Grades	Grade 3
Fatigue	-	-	2 (66.7)	-	3 (100)	-	5 (50)	-	12 (38.7)	-	17 (41.5)
Nausea	-	-	1 (33.3)	-	2 (66.7)	-	3 (30)	-	9 (29.0)	1 (3.2)	12 (29.3)	1 (2.4)
Decreased appetite	1 (25)	-	-	-	1 (33.3)	-	2 (20)	-	6 (19.4)	-	8 (19.5)
Constipation	1 (25)	-	-	-	1 (33.3)	-	2 (20)	-	4 (12.9)	-	6 (14.6)
Headache	-	-	1 (33.3)	-	1 (33.3)	-	2 (20)	-	3 (9.7)	-	5 (12.2)
AST increased	-	-	2 (66.7)	-	-	-	2 (20)	-	2 (6.5)	-	4 (9.8)
ALT increased	-	-	1 (33.3)	-	-	-	1 (10)	-	2 (6.5)	1 (3.2)	3 (7.3)	1 (2.4)
Alk Phos increased	-	-	2 (66.7)	-	-	-	2 (20)	-	1 (3.2)	-	3 (7.3)
TSH increased	-	-	-	-	-	-	-	-	3 (9.7)	-	3 (7.3)
Dyspepsia	-	-	-	-	-	-	-	-	3 (9.7)	-	3 (7.3)
Hot flush	-	-	-	-	1 (33.3)	-	1 (10)	-	2 (6.5)	-	3 (7.3)
Vomiting	-	-	-	-	-	-	-	-	3 (9.7)	-	3 (7.3)
Syncope	-	-	-	-		1 (33.3)	-	1 (10)	-	1 (3.2)	2 (4.9)	2 (4.9)
Hypokalemia	1 (25)	-	-	-	-	-	1 (1)	-	-	1 (3.2)	2 (4.9)	1 (2.4)

TRAE: treatment-related adverse events (related to ORIC-101 or enzalutamide); AEs coded using MedDRA v22.0; AST: aspartate aminotransferase; ALT: alanine aminotransferase; Alk Phos: blood alkaline phosphatase; TSH: thyroid stimulating hormone