Table 1.

PI3K/AKT inhibitors in clinical development.

Drug Name	Phase	Treatment Composition	Disease Studied
Pan-PI3K inhibitors
Buparlisib	I/II	Buparlisib monotherapy [148,149] Buparlisib + mFOLFOX6 [150] Buparlisib + abiraterone acetate [151] Buparlisib + enzalutamide [152]	Advanced solid tumors [148,150] Patients with solid or hematologic malignancies with PI3K pathway activation [149] Castration-resistant prostate cancer [151] Metastatic castration-resistant prostate cancer [152]
Dual PI3K/mTOR inhibitors
Gedatolisib	I/II	Gedatolisib monotherapy [157,158]	Advanced solid tumors [157] Advanced solid tumors treated with palliative chemotherapy [158]
Isoform-selective PI3K inhibitors
Idelalisib	III/FDA approved (for treating SLL)	Idelalisib monotherapy [161,162] Idelalisib + rituximab [163]	Relapsed indolent lymphoma [161,162] Relapsed chronic lymphocytic leukemia [163]
ATP-competitive AKT inhibitors
Capivasertib	I/II	Capivasertib + fulvestrant [168,169] Capivasertib + paclitaxel [170]	PTEN-mutant ER + metastatic breast cancer [168] Estrogen receptor + HER2- metastatic/advanced breast cancer with aromatase inhibitor resistance [169] Metastatic triple-negative breast cancer [170]
Ipatasertib	II/III	Ipatasertib + mFOLFOX6 [171] Ipatasertib + abiraterone [172] Ipatasertib + abiraterone and prednisolone [173]	Locally advanced/metastatic gastric and gastroesophageal junction cancer [171] PTEN metastatic prostate cancer [172] Metastatic castration-resistant prostate cancer [173]
Allosteric AKT Inhibitors
BAY 1125976	I	BAY 1125976 monotherapy [176]	Advanced solid cancer [176]
MK-2206	II	MK-2206 + anastrozole [177] MK-2206 + standard neoadjuvant therapy [178]	Stage II/III ER+/HER2- breast cancer with PIK3CA mutation [177] HR-/HER2+ breast cancer [178]