Table 2.

The FDA-approved and clinically developed PI3K-AKT-mTOR inhibitors

Type	Target	Drug	Highest Phase	Indications	Company/Identifier	Status
PI3K	Pan-PI3K	Copanlisib (BAY80-6946)	Approved	Relapsed follicular lymphoma	Bayer	/
		Buparlisib (BKM120)	III	Head and neck cancer	NCT04338399	Recruiting
			III	Metastatic breast cancer	NCT01633060	Terminated
			III	Breast cancer	NCT01610284	Completed
			III	Breast cancer	NCT01572727	Completed
		SF1126 (prodrug of LY294002)	I	Neuroblastoma	NCT02337309	Terminated
	p110α	Alpelisib (BYL719)	Approved	ER + /HER2-advanced metastatic breast cancer	Novartis Pharmaceuticals	/
		Inavolisib	III	Breast cancer	NCT05646862	Recruiting
			III	Breast cancer	NCT04191499	Recruiting
			III	Metastatic breast cancer	NCT05894239	Recruiting
	p110β	AZD8186	I	Advanced castrate-resistant prostate cancer, squamous non-small cell lung cancer, triple-negative breast cancer	NCT01884285	Completed
		GSK2636771	II	Melanoma and other malignant neoplasms of skin, metastatic melanoma	NCT03131908	Active, not recruiting
			II	Advanced lymphoma, advanced malignant solid neoplasm, hematopoietic and lymphoid cell neoplasm, refractory lymphoma, refractory malignant solid neoplasm, refractory multiple myeloma	NCT04439188	Active, not recruiting
			II	Advanced lymphoma, advanced malignant solid neoplasm, hematopoietic and lymphoid cell neoplasm, refractory lymphoma, refractory malignant solid neoplasm, refractory multiple myeloma	NCT04439149	Active, not recruiting
			I/II	Advanced gastric adenocarcinoma	NCT02615730	Completed
	p110γ	IPI-549	II	Head and neck squamous cell carcinoma, head and neck cancer, head and neck carcinoma, head and neck cancer stage IV, head and neck cancer stage III, HPV-Related carcinoma, HPV-Related malignancy, HPV-Related squamous cell carcinoma	NCT03795610	Recruiting
			II	Bladder cancer, urothelial carcinoma, solid tumor, advanced cancer	NCT03980041	Completed
			II	Breast cancer, renal cell carcinoma	NCT03961698	Active, not recruiting
	p110δ	Idelalisib	Approved	Relapsed chronic lymphocytic leukemia	Gilead Sciences	/
		Duvelisib	Approved	Relapsed or refractory chronic lymphocytic leukemia, small lymphocytic lymphoma	Verastem	/
		Umbralisib	Approved	Relapsed or refractory marginal zone lymphoma	TG Therapeutics	/
Dual PI3K/mTOR		Omipalisib (GSK2126458)	I	Solid tumors	NCT00972686	Completed
AKT		Capivasertib (AZD5363)	Approved	HR + , HER2- locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN-alterations	AstraZeneca	/
		Ipatasertib (GDC0068)	III	Breast cancer	NCT04060862	Active, not recruiting
		GSK2141795	II	Cervical cancer	NCT01958112	Terminated
			II	Melanoma	NCT01941927	Completed
			II	Recurrent adult acute myeloid leukemia, untreated adult acute myeloid leukemia	NCT01907815	Terminated
			II	Estrogen receptor negative, HER2/Neu negative, invasive breast carcinoma, progesterone receptor negative, recurrent breast carcinoma, stage IV breast cancer, triple-negative breast carcinoma	NCT01964924	Completed
		MK-2206	II	Colorectal neoplasms	NCT01333475	Completed
			II	Ovarian sarcoma, recurrent fallopian tube carcinoma, recurrent ovarian carcinoma, recurrent primary peritoneal carcinoma	NCT01283035	Completed
			II	Recurrent nasopharyngeal carcinoma	NCT01370070	Completed
mTOR	mTORC1	Everolimus	Approved	Advanced renal cell carcinoma following one prior antiangiogenic therapy	Novartis	/
			Approved	HR+ and HER2- breast cancer	Novartis	/
		Temsirolimus	Approved	Advanced renal cell carcinoma	Wyeth Pharmaceuticals	/
	mTORC1/ mTORC2	AZD2014	II	Meningioma	NCT03071874	Active, not recruiting
			II	Neurofibromatosis 2 meningioma	NCT02831257	Completed
			II	Diffuse large B-cell lymphoma	NCT02752204	Completed
			I/II	Endometrial carcinoma, metastatic carcinoma, HR+ tumor	NCT02730923	Active, not recruiting
			II	Metastatic breast cancer	NCT02299999	Active, not recruiting
			II	Non-small cell lung cancer metastatic	NCT02117167	Active, not recruiting
			II	Hepatocellular carcinoma	NCT03591965	Terminated
		INK128	II	Metastatic castration-resistant prostate cancer	NCT02091531	Completed
			II	merkel cell carcinoma	NCT02514824	Completed
			II	anaplastic thyroid cancer, thyroid cancer	NCT02244463	Active, not recruiting
		OSI-027	I	Any solid tumor or lymphoma	NCT00698243	Completed

Source: All the information is derived from ClinicalTrials.gov (https://www.clinicaltrials.gov) and the United States Food and Drug Administration.gov (https://www.fda.gov/)