Table 2 Important ongoing clinical trials with PI3K-targeted therapies
From: Targeting PI3K in cancer: mechanisms and advances in clinical trials
Conditions | Sample size | Design | Phase | Status | Trial number |
|---|---|---|---|---|---|
NVP-BEZ235 (BEZ235, Dactolisib) Dual PI3K/mTOR inhibitor | |||||
 Acute Lymphoblastic Leukemia; Acute Chronic Myelogenous Leukemia With Crisis of Blast Cells | 23 | BEZ235 | I | Active not recruiting | NCT01756118 |
GDC-0084 (RG7666) Dual PI3K/mTOR inhibitor | |||||
 Glioblastoma, Adult | 66 | GDC-0084 | II | Recruiting | NCT03522298 |
 Brain and Central Nervous System Tumors | 41 | Radiation therapy+ GDC-0084 | I | Not yet recruiting | NCT03696355 |
GDC-0980 (Apitolisib, RG7422) Dual PI3K/mTOR inhibitor | |||||
 Prostate Cancer | 273 | Abiraterone Acetate +/− (GDC-0980/Ipatasertib) | I/II | Active not recruiting | NCT01485861 |
LY3023414 Dual PI3K/mTOR inhibitor | |||||
 Endometrial Cancer; Recurrent Endometrial Cancer | 25 | LY3023414 | II | Recruiting | NCT02549989 |
 Advanced Malignant Solid Neoplasm; Ann Arbor Stage III/IV Childhood Non-Hodgkin Lymphoma | – | LY3023414 | II | Recruiting | NCT03155620 |
 Metastatic Colorectal Neoplasm; Metastatic Breast Cancer | 205 | Prexasertib+Cisplatin/Cetuximab/Pemetrexed/5-FU/LY3023414 | I | Recruiting | NCT02124148 |
 Advanced or Metastatic Solid Tumors | 163 | LY3039478 + LY3023414/Taladegib/Abemaciclib/Cisplatin/Gemcitabine/Carboplatin | I | Recruiting | NCT02784795 |
 NSCLC | 150 | Abemaciclib+LY3023414/Pemetrexed/Gemcitabine/Ramucirumab/Pembrolizumab | I | Active not recruiting | NCT02079636 |
 Prostate Cancer Metastatic | 144 | Enzalutamide +/− LY3023414 | II | Recruiting | NCT02407054 |
 Advanced Non-Hodgkin Lymphoma; Metastatic Breast Cancer; Advanced Mesothelioma; Advanced NSCLC | 130 | LY3023414 + Midazolam/Fulvestrant OR LY3023414 + Pemetrexed/Cisplatin OR LY3023414 +/− (Abemaciclib+ Letrozole) | I | Recruiting | NCT01655225 |
 Pancreatic Ductal Adenocarcinoma | 231 | Abemaciclib+/− LY3023414 VS Gemcitabine/Capecitabine | II | Active not recruiting | NCT02981342 |
 Breast Neoplasms | 198 | LY3023414 + LY2835219 + Fulvestrant | I | Recruiting | NCT02057133 |
 Advanced Malignant Solid Neoplasm; Ann Arbor Stage III/ IV Non-Hodgkin Lymphoma | 144 | LY3023414 | II | Recruiting | NCT03213678 |
 Endometrial Cancer | 62 | (LY3023414 + Abemaciclib) +/− Letrozole | II | Not yet recruiting | NCT03675893 |
PF-05212384 (Gedatolisib, PKI-587) Dual PI3K/mTOR inhibitor | |||||
 Therapy-related Acute Myeloid Leukemia and Myelodysplastic Syndrome; Relapsed Acute Myeloid Leukemia; de Novo Acute Myeloid Leukemia at Diagnostic | 10 | PF-05212384 | II | Active not recruiting | NCT02438761 |
 Neoplasm | 124 | PF-05212384 + Docetaxel/Cisplatin/Dacomitinib | I | Recruiting | NCT01920061 |
 Lung Cancer Squamous Cell; Solid Tumors; Head & Neck Cancer; Pancreatic Cancer | 96 | PF-05212384 + Palbociclib | I | Recruiting | NCT03065062 |
 NSCLC | 51 | PF-05212384/Paclitaxel/Carboplatin | I/II | Recruiting | NCT02920450 |
 Breast Cancer; NSCLC; Ovary Cancer; Endometrial Cancer; SCLC | 40 | PF-05212384 + Paclitaxel+Carboplatin | I | Recruiting | NCT02069158 |
 ER+/HER2- Breast Cancer | 18 | PF-05212384 + Fulvestrant+ Palbociclib | I | Recruiting | NCT02626507 |
 Breast Cancer | 80 | Hydrpxychloroquine+/− PF-05212384 | I/II | Not yet recruiting | NCT03400254 |
 Breast Cancer | 120 | PF-05212384 + Palbociclib+/−Letrozole/Fulvestrant | I | Recruiting | NCT02684032 |
 Triple Negative Breast Cancer; Metastatic Breast Cancer | 18 | PF-05212384 + PTK7-ADC | I | Recruiting | NCT03243331 |
PQR309 (Bimiralisib) Dual PI3K/mTOR inhibitor | |||||
 Lymphoma | 72 | PQR309 | I/II | Recruiting | NCT02249429 |
 Lymphoma; Non-Hodgkin Lymphoma | 72 | PQR309 | II | Recruiting | NCT03127020 |
 Primary Central Nervous System Lymphoma | 21 | PQR309 | II | Not yet recruiting | NCT03120000 |
 Metastatic Breast Cancer | 60 | PQR309 + Eribulin | I/II | Recruiting | NCT02723877 |
P7170 Dual PI3K/mTOR inhibitor | |||||
 Advanced Refractory Solid Tumors | 60 | P7170 | I | Suspended | NCT01762410 |
SF-1126 Dual PI3K/mTOR inhibitor | |||||
 Advanced Hepatocellular Carcinoma | 14 | SF-1126 | I | Recruiting | NCT03059147 |
 Advanced Castrate-resistant Prostate Cancer; Squamous NSCLC; Triple Negative Breast Cancer | 180 | AZD8186+/−Abiraterone Acetate/AZD2014 | I | Recruiting | NCT01884285 |
Copanlisib (BAY 80–6946) PI3Kδ/α inhibitor | |||||
 Recurrent Endometrial, Ovarian, Primary Peritoneal, or Fallopian Tube Cancer | 44 | Copanlisib+Niraparib | I | Not yet recruiting | NCT03586661 |
 Head and Neck Squamous Cell Carcinomas | 32 | Copanlisib+Cetuximab | I/II | Recruiting | NCT02822482 |
 Endometrial cancer | 84 | Copanlisib | II | Suspended | NCT02728258 |
 HR+, HER2-, Stage I-IV Breast Cancer | 102 | Copanlisib+Letrozole+/-Palbociclib | I/II | Recruiting | NCT03128619 |
 HER2+ Breast Cancer | 19 | Copanlisib +Trastuzumab | I | Recruiting | NCT02705859 |
 Non-Hodgkin Lymphoma | 25 | Copanlisib | I/II | Active not recruiting | NCT02342665 |
 Mature T-Cell and NK-Cell Neoplasm | 36 | Copanlisib+Gemcitabine | I/II | Recruiting | NCT03052933 |
 Advanced or Metastatic Solid Tumor | 65 | Copanlisib+Rogaratinib | I | Recruiting | NCT03517956 |
 Medical Oncology | 51 | Copanlisib+/-Itraconazole/ Rifampin | I | Active not recruiting | NCT02253420 |
 Mixed Tumor, Malignant | 130 | Copanlisib | I/II | Recruiting | NCT03458728 |
 Biliary Carcinoma; Gall Bladder Carcinoma; Cholangiocarcinoma; Gastrointestinal Tumor | 25 | Copanlisib+Gemcitabine+Cisplatin | II | Recruiting | NCT02631590 |
 Refractory/Recurrent Primary Central Nervous System Lymphoma | 45 | Copanlisib+Ibrutinib | I/II | Not yet recruiting | NCT03581942 |
 Marginal Zone Lymphoma | 56 | Copanlisib+Rituximab | II | Not yet recruiting | NCT03474744 |
 Large B-Cell Lymphoma | 99 | Copanlisib+Nivolumab | II | Not yet recruiting | NCT03484819 |
 Ann Arbor Stage III/IV Lymphoma; Metastatic Malignant; Solid Neoplasm | 50 | Copanlisib+Nivolumab | I | Recruiting | NCT03502733 |
 Non-Hodgkin Lymphoma | 450 | Rituximab+Copanlisib/Placebo | III | Recruiting | NCT02367040 |
 Non-Hodgkin Lymphoma | 227 | Copanlisib | II | Active not recruiting | NCT01660451 |
 Non-Hodgkin Lymphoma | 25 | Copanlisib | III | Active not recruiting | NCT02369016 |
 Non-Hodgkin Lymphoma | 12 | Copanlisib | I | Recruiting | NCT03498430 |
 Non-Hodgkin Lymphoma | 546 | Standard Immunochemotherapy+/− Copanlisib | III | Recruiting | NCT02626455 |
Buparlisib (BKM120 NVP-BKM120) Class I PI3K inhibitor | |||||
 Metastatic Transitional Cell Carcinoma of the Urothelium | 35 | Buparlisib | II | Active not recruiting | NCT01551030 |
 Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma; | 30 | Buparlisib+Cetuximab | I/II | Active not recruiting | NCT01816984 |
 Head and Neck Cancer | 170 | Buparlisib | II | Recruiting | NCT01737450 |
 NSCLC | 37 | Buparlisib+Erlotinib | II | Active not recruiting | NCT01487265 |
 NSCLC | 38 | Buparlisib+Gefitinib |  | Active not recruiting | NCT01570296 |
 Advanced Squamous Cell Cancer of Head and Neck | 23 | Radiotherapy+Buparlisib+ Cisplatin | I | Active not recruiting | NCT02113878 |
 Breast Cancer | 106 | Buparlisib+lapatinib | I/II | Suspended (Data analysis) | NCT01589861 |
 Breast Cancer | 1149 | Buparlisib/Placebo+Fulvestrant | III | Active not recruiting | NCT01610284 |
 Breast Cancer | 110 | Buparlisib | II | Active not recruiting | NCT01790932 |
 Metastatic Breast Cancer | 47 | Buparlisib+Capecitabine+/− (Trastuzumab/Lapatinib) OR BYL719+ Capecitabine | I | Active not recruiting | NCT01300962 |
 Breast Cancer Patients With Brain Metastases | 10 | Buparlisib/Capecitabine | II | Active not recruiting | NCT02000882 |
 Pre-menopausal Breast Cancer | 40 | Buparlisib/BYL719 + Tamoxifen+Goserelin Acetate | I | Active not recruiting | NCT02058381 |
 Ovarian Cancer; Breast Cancer | 118 | Buparlisib/BYL719+ Olaparib | I | Active not recruiting | NCT01623349 |
 Glioblastoma Multiforme | 88 | Buparlisib+Bevacizumab | I/II | Active not recruiting | NCT01349660 |
 Glioblastoma | 65 | Buparlisib+/-Surgery | II | Active not recruiting | NCT01339052 |
 Thyroid Cancers | 47 | Buparlisib | II | Active not recruiting | NCT01830504 |
 Thymoma | 14 | Buparlisib | II | Active not recruiting | NCT02220855 |
 Malignant Melanoma; Metastases | 22 | Buparlisib | II | Recruiting | NCT02452294 |
 Melanoma | 140 | LGX818 + MEK162+/−(Buparlisib/LEE011/ BGJ398/ INC280) | II | Active not recruiting | NCT02159066 |
 Metastatic Colorectal Cancer | 22 | Buparlisib+Panitumumab | I/II | Active not recruiting | NCT01591421 |
 Relapsed or Refractory Indolent B-Cell Lymphoma | 18 | Buparlisib+Rituximab | I | Active not recruiting | NCT02049541 |
 Chronic Lymphocytic Leukemia | 14 | Buparlisib | II | Active not recruiting | NCT02340780 |
 Recurrent/ Refractory Chronic Lymphocytic Leukemia; Recurrent/ Refractory Small Lymphocytic Lymphoma | 1 | Buparlisib+Ofatumumab/Ibrutinib | I | Active not recruiting | NCT02614508 |
 Mantle Cell Lymphoma; Follicular Lymphoma; Diffuse Large B Cell Lymphoma | 37 | Buparlisib+Ibrutinib | I | Active not recruiting | NCT02756247 |
Duvelisib (IPI-145) PI3Kδ/γ inhibitor | |||||
 Indolent Non-Hodgkin Lymphoma | 129 | Duvelisib | II | Active not recruiting | NCT01882803 |
 Relapsed/Refractory T-cell Lymphomas | 88 | Duvelisib+Romidepsin/ Bortezomib | I | Recruiting | NCT02783625 |
 Peripheral T-cell Lymphoma | 120 | Duvelisib | II | Recruiting | NCT03372057 |
 Chronic Lymphocytic Leukemia | 47 | Duvelisib+Venetoclax | I/II | Recruiting | NCT03534323 |
 Hematologic Malignancy | 500 | Duvelisib | II | Active not recruiting | NCT02711852 |
 Chronic Lymphocytic Leukemia; Small Lymphocytic Lymphoma | 150 | Duvelisib VS Ofatumumab | III | • Enrolling by invitation | NCT02049515 |
 Chronic Lymphocytic Leukemia; Small Lymphocytic Lymphoma | 300 | Duvelisib VS Ofatumumab | III | Active not recruiting | NCT02004522 |
 Chronic Lymphocytic | 50 | Duvelisib | II | Recruiting | NCT03370185 |
Leukemia; Small Lymphocytic Lymphoma | |||||
 Chronic Lymphocytic Leukemia | 32 | Duvelisib+Fludarabine+Cyclophosphamide+Rituximab | I/II | Active not recruiting | NCT02158091 |
RP6530 (Tenalisib) PI3Kδ/γ inhibitor | |||||
 Peripheral T-Cell Lymphoma; Cutaneous T-Cell Lymphoma | 58 | RP6530 | I | Active not recruiting | NCT02567656 |
 Classical Hodgkin Lymphoma | 57 | RP6530 + Pembrolizumab | I | Recruiting | NCT03471351 |
Taselisib (GDC-0032) PI3Kα/β/γ inhibitor | |||||
 Recurrent/ Stage IV Squamous Cell Lung Carcinoma | 59 | Taselisib | II | Active not recruiting | NCT02785913 |
 Metastatic Breast Cancer; Recurrent Breast Cancer | 76 | Taselisib+Trastuzumab emtansine +/− Pertuzumab OR Pertuzumab+Trastuzumab+/− Paclitaxel | I | Recruiting | NCT02390427 |
 Androgen Receptor Positive Triple Negative Metastatic Breast Cancer | 73 | Taselisib+Enzalutamide | I/II | Active not recruiting | NCT02457910 |
 Breast Cancer | 290 | Tamoxifen+ Taselisib/Placebo | I/II | Recruiting | NCT02285179 |
 Breast Cancer | 631 | Fulvestrant+ Taselisib/Placebo | III | Active not recruiting | NCT02340221 |
 PIK3CA-Related Overgrowth | 30 | Taselisib | I/II | Recruiting | NCT03290092 |
 Solid Cancers; Non-Hodgkin Lymphoma | 724 | Taselisib+/-Fulvestrant/Letrozole/Midazolam/ Fulvestrant | I | Active not recruiting | NCT01296555 |
 Advanced Refractory Solid Tumors; Lymphomas; Multiple Myeloma | 6452 | Molecular Analysis for Therapy Choice Screening Trial | II | Recruiting | NCT02465060 |
KA2237 PI3Kβ/γ inhibitor | |||||
 B Cell Lymphoma | 53 | KA2237 | I | Recruiting | NCT02679196 |
BYL719 (Alpelisib) PI3Kα inhibitor | |||||
 PIK3CA Mutated Advanced Breast Cancer | 90 | BYL719 VS Chemotherapy | II | Recruiting | NCT03386162 |
 Breast Cancer | 23 | BYL719 + LJM716+ Trastuzumab | I | Active not recruiting | NCT02167854 |
 Breast Cancer | 44 | BYL719 + Nab-Paclitaxel | I/II | Active not recruiting | NCT02379247 |
 HER2+ Metastatic Breast Cancer | 17 | BYL719 + Ado-Trastuzumab Emtansine | I | Active not recruiting | NCT02038010 |
 Metastatic Breast Cancer | 34 | BYL719 | II | Recruiting | NCT02506556 |
 Malignant Neoplasm of Breast | 28 | BYL719 + Enzalutamide | I | Not yet recruiting | NCT03207529 |
 Pancreatic Cancer | 15 | BYL719 + Gemcitabine+(Nab)-Paclitaxel | I | Active not recruiting | NCT02155088 |
 Breast Cancer | 572 | Fulvestrant+ BYL719/Placebo | III | Active not recruiting | NCT02437318 |
 Premenopausal Patients With HR+, HER2- Locally Advanced or Metastatic Breast Cancer | 40 | BYL719/BKM120 + Tamoxifen+Goserelin Acetate | I | Active not recruiting | NCT02058381 |
 Advanced or Metastatic ER+ Breast Cancer | 312 | LSZ102+/− LEE011/BYL719 | I | Recruiting | NCT02734615 |
 Metastatic or Locally-advanced Unresectable Breast Cancer | 52 | BYL719 + Letrozole/Exemestane | I | Active not recruiting | NCT01870505 |
 Breast Cancer | 160 | BYL-719 + Fulvestrant/Letrozole | II | Recruiting | NCT03056755 |
 ER+ Breast Cancer; HER2-negative Breast Cancer; Invasive Ductal Breast Carcinoma | 46 | BYL719 + Letrozole | I | Active not recruiting | NCT01791478 |
 Breast Cancer | 253 | Letrozole+BYL719/LEE011/ Both | I | Recruiting | NCT01872260 |
 Metastatic Breast Cancer | 47 | BMK120 + Capecitabine+/− Trastuzumab/Lapatinib OR BYL719+ Capecitabine | I | Active not recruiting | NCT01300962 |
 Head and Neck Cancer and Esophageal Cancer Patient | 259 | BYL719/Poziotinib/Nintedanib/Abemaciclib/(Durvalumab+Tremelimumab) | II | Recruiting | NCT03292250 |
 Head and Neck Squamous Cell Cancer | 30 | BYL719 | N/A | Recruiting | NCT03138070 |
 Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck | 43 | BYL719 | II | Recruiting | NCT02145312 |
 Head and Neck Squamous Cell Cancer | 16 | BYL719 + Cetuximab+IMRT (Intensity-Modulated Radiation Therapy) | I | Active not recruiting | NCT02282371 |
 Locoregionally Advanced Squamous Cell Carcinoma of Head and Neck | 36 | BYL719 + Cisplatin+Radiation (Intensity modulated radiation therapy) | I | Recruiting | NCT02537223 |
 Uveal Melanoma | 30 | BYL719 + AEB071 | I | Active not recruiting | NCT02273219 |
 Rectal Cancer | 24 | BYL719 + Capecitabine+Radiation | I | Recruiting | NCT02550743 |
 Colorectal Cancer | 150 | LGX818 + Cetuximab+/− BYL719 | I/II | Active not recruiting | NCT01719380 |
 Patients With Gastrointestinal Stromal Tumor | 56 | BYL719 + ST571 | I | Active not recruiting | NCT01735968 |
 Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma | 67 | BYL719/AUY922/INC280/LDK378/MEK162 | II | Active not recruiting | NCT02276027 |
 CDKN2A-p16+; Human Papillomavirus+ Oropharyngeal Squamous Cell Carcinoma | 14 | BYL719 + Surgery | II | Not yet recruiting | NCT03601507 |
 Breast Neoplasms; Kidney Neoplasms; Pancreatic  Neuroendocine Neoplasms | 79 | BYL719 + Everolimus/Exemestane/Both | I | Active not recruiting | NCT02077933 |
Advanced Solid Tumors With an Alteration of the PIK3CA Gene; ER+ Breast Cancer | 221 | BYL719+/-Fulvestrant | I | Active not recruiting | NCT01219699 |
 Solid Tumors | 41 | BYL719 + Cisplatin | I | Recruiting | NCT02620839 |
 Ovarian Cancer; Breast Cancer | 118 | Olaparib+BYL719/BKM120 | I | Active not recruiting | NCT01623349 |
 Meningioma | 25 | BYL719 + Trametinib | I | Not yet recruiting | NCT03631953 |
CAL-101 (GS-1101, Idelalisib) PI3Kδ inhibitor | |||||
 Metastasis/Recurrence NSCLC | 40 | CAL-101 + Pembrolizumab | I/II | Recruiting | NCT03257722 |
 Waldenstrom Macroglobulinemia | 50 | Obinutuzumab | II | Active not recruiting | NCT02962401 |
 Chronic Lymphocytic Leucemia | 62 | CAL-101 + Bendamustine+GA101 | II | Recruiting | NCT02445131 |
 Chronic Lymphocytic LeukemiaSmall Lymphocytic Lymphoma | 50 | CAL-101 + Ofatumumab | II | Suspended | NCT02135133 |
 Follicular Non-Hodgkin Lymphoma Refractory | 260 | CAL-101 | N/A | Recruiting | NCT03568929 |
 Chronic Lymphocytic Leukemia | 42 | CAL-101 + Rituximab+Venetoclax | I | Not yet recruiting | NCT03639324 |
 Chronic Lymphocytic Leukemia | 104 | CAL-101 + Rituximab | N/A | Not yet recruiting | NCT03545035 |
 Diffuse Large B-Cell | 36 | CAL-101 + (Rituximab+Ifosfa | I | Recruiting | NCT03349346 |
 Lymphoma; Mediastinal B-cell Lymphoma |  | mide+Carboplatin+Etoposide) (RICE) |  |  |  |
 Chronic Lymphocytic Leukemia | 35 | CAL-101 + Tirabrutinib+/− Obinutuzumab | II | Recruiting | NCT02968563 |
 Chronic Lymphocytic Leukemia; Small Lymphocytic Lymphoma | 24 | MOR00208 + CAL-101/ Venetoclax | II | Recruiting | NCT02639910 |
 Chronic Lymphocytic Leukemia | 308 | Acalabrutinib VS Rituximab + CAL-101/Bendamustine | III | Recruiting | NCT02970318 |
 Recurrent Chronic Lymphocytic Leukemia; Extranodal Marginal Zone Lymphoma; Follicular Lymphoma | 68 | Pembrolizumab+/-CAL-101/Ibrutinib | II | Recruiting | NCT02332980 |
 B-cell Malignancies | 197 | Tirabrutinib+/-CAL-101/Entospletinib+/− Obinutuzumab | I | Active not recruiting | NCT02457598 |
 Chronic Lymphocytic Leukemia; Peripheral T-cell Lymphoma | 123 | TRU-016 + Rituximab/ Obinutuzumab/Ibrutinib/ Bendamustine OR TRU-016 + Rituximab+CAL-101 | I | Recruiting | NCT01644253 |
 Acute Lymphoblastic Leukemia; Acute Myeloid Leukemia | 24 | Personalized Kinase Inhibitor Therapy Combined With Chemotherapy | I | Recruiting | NCT02779283 |
 Non-Hodgkin Lymphoma | 30 | CAL-101 | N/A | Recruiting | NCT02928510 |
 Hematological Malignancies | 150 | CAL-101 VS Ibrutinib (Side Effects) | N/A | Recruiting | NCT02824159 |
 Recurrent Chronic Lymphoid Leukemia | 3 | ACY-1215+ CAL-101/Ibrutinib | I | Active not recruiting | NCT02787369 |
 Chronic Lymphocytic Leukemia | 416 | Rituximab+Bendamustine+ Placebo/ CAL-101 | III | Active not recruiting | NCT01569295 |
 Follicular Lymphoma | 240 | CAL-101 | III | Recruiting | NCT02536300 |
 B Cells-Tumors; B Cell Chronic Lymphocytic Leukemia; Follicular Lymphoma; Mantle Cell Lymphoma; Large B-Cell Diffuse Lymphoma | 60 | CAL-101 VS Placebo | I | Recruiting | NCT03151057 |
 Chronic Lymphocytic Leukemia; Small Lymphocytic Lymphoma | 24 | MOR00208 + CAL-101/ Venetoclax | II | Active not recruiting | NCT02639910 |
 Diffuse Large B Cell Lymphoma | 72 | CAL-101 | II | Recruiting | NCT03576443 |
 B-Cell Non-Hodgkin Lymphoma | 34 | CAL-101 | II | Recruiting | NCT03133221 |
 Chronic Lymphocytic Leukemia | 20 | CAL-101 + Rituximab | N/A | Recruiting | NCT02993536 |
 Chronic Lymphocytic Leukaemia | 150 | CAL-101 + Rituximab | N/A | Not yet recruiting | NCT03582098 |
GSK2636771 PI3Kβ inhibitor | |||||
 Gastric Cancer | 400 | Biomarker Screening | N/A | Recruiting | NCT02951091 |
 Advanced Gastric Adenocarcinoma | 66 | GSK2636771+ Paclitaxel | I/II | Recruiting | NCT02615730 |
 Metastatic Castration-Resistant Prostate Cancer | 64 | GSK2636771+ Enzalutamide | I | Recruiting | NCT02215096 |
 Melanoma and Other Malignant Neoplasms of Skin; Metastatic Melanoma | 41 | GSK2636771 + Pembrolizumab | I/II | Recruiting | NCT03131908 |
 Advanced Malignant Solid Neoplasm | – | Patients with PTEN mutation, deletion, expression or loss were given GSK2636771 | II | Recruiting | NCT02465060 |
INCB050465 (Parsaclisib) PI3Kδ inhibitor | |||||
 MPN (Myeloproliferative Neoplasms) | 78 | INCB050465 + Ruxolitinib | II | Recruiting | NCT02718300 |
 Advanced Solid Tumors | 237 | Pembrolizumab+Itacitinib/ INCB050465 | I | Recruiting | NCT02646748 |
 Advanced Solid Tumors | 159 | Itacitinib+Epacadostat/ INCB050465 | I | Active, not recruiting | NCT02559492 |
 Solid Tumors; Advanced Malignancies; Metastatic Cancer | 80 | Ia:INCB052793 Ib:INCB052793 + (Gemcitabine+Nab-Paclitaxel+Dexamethasone+Carfilzomib/+Bortezomib+Lenalidomide+Azacitidine+INCB052793 + Pomalidomide+INCB050465) II:INCB052793 + Azacitidine+ INCB039110 | I/II | Active not recruiting | NCT02265510 |
 Unresectable or Metastatic Solid Tumors | 100 | INCMGA00012 + Epacadostat / INCB050465 | I | Recruiting | NCT03589651 |
 Primary Sjögren’s Syndrome | 12 | INCB050465 | II | Not yet recruiting | NCT03627065 |
 Lymphoma | 120 | INCB050465 | II | Recruiting | NCT03235544 |
 Lymphoma | 120 | INCB050465+/-CITADEL-204 | II | Recruiting | NCT03144674 |
 Lymphoma | 60 | INCB050465 | II | Active not recruiting | NCT02998476 |
 Lymphoma | 18 | INCB050465 | I | Recruiting | NCT03314922 |
 Lymphoma | 45 | INCB050465 + Bendamustine +Obinutuzumab | I | Recruiting | NCT03039114 |
 Lymphoma | 100 | INCB050465 | II | Recruiting | NCT03126019 |
 B-Cell Malignancies | 88 | INCB050465+/-Itacitinib OR INCB050465 + Rituximab+Ifosfamide+Carboplatin+Etoposide | I/II | Active not recruiting | NCT02018861 |
 Relapsed/ Refractory Diffuse Large B-Cell Lymphoma | 25 | INCB050465 + INCB053914 | I | Not yet recruiting | NCT03688152 |
 B-cell Lymphoma | 81 | INCB050465 + Rituximab+/− Bendamustine OR INCB050465+ Ibrutinib | I | Recruiting | NCT03424122 |
Serabelisib (INK-1117,MLN-1117,TAK-117) PI3Kα inhibitor | |||||
 Advanced Solid Tumor | 30 | Serabelisib+TAK-228+ Paclitaxel | I | Not yet recruiting | NCT03154294 |
 Clear-cell Metastatic Renal Cell Carcinoma | 96 | MLN0128+/-Serabelisib VS Everolimus | II | Active not recruiting | NCT02724020 |
 Endometrial Neoplasms | 242 | Paclitaxel+/− MLN0128 OR MLN0128+/− Serabelisib | II | Recruiting | NCT02725268 |
 Triple Negative Breast Cancer | 20 | TAK-228 + Serabelisib+ Cisplatin+Nab Paclitaxel | II | Recruiting | NCT03193853 |
ME401 (PWT-143) PI3Kδ inhibitor | |||||
 Chronic Lymphocytic Leukemia (CLL) Small Lymphocytic Lymphoma (SLL), B-cell Non-Hodgkin Lymphoma | 133 | ME401+/−Rituximab | I | Recruiting | NCT02914938 |
Umbralisib (RP5264, TGR-1202) PI3Kδ inhibitor | |||||
 Marginal Zone Lymphoma; Waldenstrom Macroglobulinemia | 30 | Umbralisib | II | Recruiting | NCT03364231 |
 Chronic Lymphocytic Leukemia | 30 | Ublituximab +Umbralisib + Venetoclax | I/II | Recruiting | NCT03379051 |
 Follicular Lymphoma | 150 | Obinutuzumab+ Umbralisib / lenalidomide/Chemotherapy | II | Recruiting | NCT03269669 |
 Non-Hodgkin Lymphoma; Chronic Lymphocytic Leukemia | 50 | TG-1701 +/− (Ublituximab + Umbralisib) | I | Recruiting | NCT03671590 |
 Chronic Lymphocytic Leukemia; B-cell Non-Hodgkin Lymphoma | 36 | Umbralisib +Pembrolizumab | I | Recruiting | NCT03283137 |
 Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma; Mantle Cell Lymphoma | 45 | Umbralisib+Ibrutinib | I | Active not recruiting | NCT02268851 |
CUDC-907 (Fimepinostat) PI3Kα/β/δ and HDAC1/2/3/10 inhibitor | |||||
 Advanced/Relapsed Solid Tumors | 60 | CUDC-907 | I | Recruiting | NCT02307240 |
 Lymphoma; Neuroblastoma; Brain Tumor; Solid Tumor | 44 | CUDC-907 | I | Recruiting | NCT02909777 |
 Multiple Myeloma; Lymphoma | 88 | CUDC-907 | I | Active not recruiting | NCT01742988 |
 Relapsed and/or Refractory Diffuse Large B-cell Lymphoma Including With Myc Alterations | 200 | CUDC-907 | II | Recruiting | NCT02674750 |
Rigosertib (ON-01910) PI3K and PIk-1 inhibitor | |||||
 Leukemia; Myelofibrosis; Anemia; Splenomegaly | 35 | Rigosertib | II | Recruiting | NCT02730884 |
 Myelodysplastic Syndromes | 36 | Rigosertib | I | Suspended | NCT02075034 |
 Myelodysplastic Syndromes | 45 | Rigosertib | II | Active not recruiting | NCT01904682 |
 Myelodysplastic Syndromes; MDS; RAEB; Chronic Myelomonocytic Leukemia | 299 | Rigosertib | III | Active not recruiting | NCT01241500 |
 Myelodysplastic Syndromes; Refractory Anemia With Excess Blasts; Chronic Myelomonocytic Leukemia; Cytopenia | 67 | Rigosertib | III | Active not recruiting | NCT01928537 |
 Myelodysplastic Syndromes | 12 | Rigosertib | I | Recruiting | NCT03495167 |
 Myelodysplastic Syndrome; Acute Myeloid Leukemia; Chronic Myelomonocytic Leukemia | 45 | Rigosertib+Azacitidine | I/II | Active not recruiting | NCT01926587 |
 Myelodysplastic Syndrome; MDS; Refractory Anemia With Excess Blasts; RAEB | 360 | Rigosertib VS. Any approved or standard-of-care therapy | III | Recruiting | NCT02562443 |