Table 1. Pharmacological properties of clinical PI3K inhibitors.

PI3K inhibitors that have reached late phases of clinical development and/or have been approved by the FDA for the treatment of cancer are listed.

			In vitro IC50 (nM)
PI3K inhibitor	Company	Structure	PI3Kα	PI3Kβ	PI3K	PI3Kγ	Clinical	Dose	t1/2 (h)	Registration trial	Ref
Alpelisib	Novartis		4.6	1156	290	250	Approved for HR+/Her2- mBC in combination with Fulvestrant	Oral; 300 mg daily	8	NCT02437318	71–73
Buparlisib	Novartis		52	166	116	262	Discontinued during Phase III	Oral; 100 mg daily	40	NCT01633060	58,121
Copanlisib	Bayer		0.5	3.7	0.7	6.4	Approved for relapsed follicular lymphoma	IV; 60 mg three times a month	39.1	NCT01660451	68,69
Duvelisib	Verastem		1602	85	2.5	27	Approved for relapsed follicular lymphoma, Chronic lymphocytic leukemia; small lymphocytic leukemia	Oral; 25 mg twice daily	4.7	NCT02004522	81
Idelalisib	Gilead		8600	4000	19	110	Approved for relapsed follicular lymphoma, Chronic lymphocytic leukemia; small lymphocytic leukemia	Oral; 150 mg twice daily	8.2	NCT01282424	122,123
Inavolisib	Genentech		0.038	N/A	N/A	N/A	Ongoing Phase III in combination with Fulvestrant and palbociclib for HR+/Her2- mBC	Oral; 9 mg daily	18	NCT04191499	124,125
Taselisib	Genentech		0.029	8	0.12	0.97	Discontinued during Phase III	Oral; 4 mg daily	39.3	NCT02340221	76,77,94
Umbrasilib	TG Therapeutics		>10000	>10000	6.2	1400	Approved for relapsed follicular lymphoma and marginal zone lymphoma	Oral; 800 mg daily	91	NCT02793583	82