Table 1 Potential inhibitors of the PI3K/AKT/mTOR pathway available for targeting PI3K.
From: Immunometabolism in cancer: basic mechanisms and new targeting strategy
Target | Drug | Phase/status | Tumor type | Treatment | ClinicalTrials. govIdentifier |
|---|---|---|---|---|---|
PI3K/AKT/mTOR inhibitors | |||||
PI3Kα | Alpelisib | FDA approved for marketing | Breast cancer | With Fulvestrant | |
Taselisib | II Ongoing | Advanced lymphoma Advanced malignant Solid neoplasm Hematopoietic and lymphoid cell neoplasm … | Monotherapy | ||
II Completed | Recurrent squamous cell lung carcinoma Stage IV squamous cell lung carcinoma | Monotherapy | |||
I Ongoing | Metastaticbreast cancer Recurrent breast cancer | With Trastuzumab emtansine, Paclitaxel Pertuzumab, Trastuzumab | |||
II Completed | Breast cancer | With Letrozole, | |||
II Ongoing | Advanced malignant Solid neoplasm Bladder carcinoma Breast carcinoma Cervical carcinoma… | With Adavosertib, Afatinib, Afatinib Dimaleate… | |||
Inavolisib | II Ongoing | HER2-positive breast cancer | With PHESGO | ||
III Ongoing | Breast cancer | With Placebo, Palbociclib, Fulvestrant | |||
I Ongoing | Metastatic colorectal cancer | With Bevacizumab, Cetuximab, SY-5609, Atezolizumab, Tiragolumab | |||
II Ongoing | Breast cancer Triple-negative breast cancer | With Capecitabine, Talazoparib, Atezolizumab | |||
II Ongoing | Early-stage breast cancer | With Atezolizumab, Ipatasertib, Olaparib | |||
I/II Ongoing | Inoperable, locally advanced or metastatic, ER-positive breast cancer | With Giredestrant, Abemaciclib, Ipatasertib… | |||
Serabelisib (TAK-117/MLN1117) | I Ongoing | Advanced solid tumor PIK3CA mutation PTEN loss of function mutation | With Nab-paclitaxel | ||
II Completed | Endometrial neoplasms | With Paclitaxel, Sapanisertib | |||
MEN1611 | I/II Ongoing | Metastatic colorectal cancer | With Cetuximab | ||
I Ongoing | Advanced or metastatic breast cancer | With Trastuzumab, Fulvestrant | |||
CYH33 | I Ongoing | Ovarian cancer Breast cancer Solid tumor Prostate cancer Endometrial cancer | Monotherapy | ||
II Ongoing | Ovarian cancer Recurrent cancer | Monotherapy | |||
I Ongoing | Advanced breast cancer | With Fulvestrant, Letrozole, Palbociclib | |||
PI3Kβ | GSK2636771 | II Ongoing | Advanced lymphoma Advanced malignant Solid neoplasm Hematopoietic and lymphoid cell neoplasm Refractory lymphoma Refractory malignant | Monotherapy | |
II Ongoing | Advanced lymphoma Advanced malignant Solid neoplasm Hematopoietic and lymphoid cell neoplasm Refractory lymphoma Refractory malignant | Monotherapy | |||
I/II Ongoing | Melanoma and other malignant neoplasms of skin Metastatic melanoma | With Pembrolizumab | |||
SAR260301 | I/Ib Completed | Neoplasm malignant | With Vemurafenib | ||
AZD8186 | I Ongoing | Advanced breast carcinoma Advanced malignant Solid neoplasm Advanced prostate carcinoma … | With Docetaxel | ||
I/II Ongoing | Solid tumor Stomach cancer | With Paclitaxel | |||
I/II Ongoing | Solid tumor Stomach cancer | With Alpelisib, Paclitaxel | |||
PI3Kγ | IPI549 (Eganelisib) | II Ongoing | Bladder cancer Urothelial carcinoma Solid tumor Advanced cancer | With Nivolumab, Placebos | |
II Ongoing | Head and neck squamous cell carcinoma HPV-related carcinoma HPV-related malignancy HPV-related squamous cell carcinoma | Monotherapy | |||
PI3Kδ | Idelalisib | FDA approved for marketing | Chronic lymphocytic leukemia Follicular lymphoma Small lymphocytic leukemia | With Rituxan, Monotherapy | |
Umbralisib | I/II Ongoing | Mantle cell lymphoma | With Ublituximab | ||
II Ongoing | Lymphoma Follicular lymphoma Marginal zone lymphoma Marginal zone B-cell lymphoma | With Rituximab | |||
II Completed | Waldenstrom macroglobulinemia | Monotherapy | |||
II Ongoing | Chronic lymphocytic leukemia | With Ublituximab | |||
I Completed | Chronic lymphocytic leukemia Richter syndrome | With Ublituximab, TG-1501 | |||
II Ongoing | Chronic lymphocytic leukemia | With Ublituximab, Ibrutinib, Venetoclax, Acalabrutinib Oral Capsule | |||
II/III Ongoing | Chronic lymphocytic leukemia Small lymphocytic lymphoma | With Ublituximab, Venetoclax | |||
II Ongoing | Chronic lymphocytic leukemia Small lymphocytic lymphoma Relapsed chronic lymphocytic leukemia Refractory chronic lymphocytic leukemia | With Acalabrutinib, Ublituximab | |||
I Ongoing | B-cell non-Hodgkin lymphoma Relapsed B-cell non-Hodgkin lymphoma Refractory B-cell non-Hodgkin lymphoma | With Loncastuximab Tesirine, Gemcitabine, Lenalidomide, Polatuzumab Vedotin | |||
I Ongoing | Non-Hodgkin lymphoma Chronic lymphocytic leukemia | With TG1701, Ublituximab | |||
I Ongoing | Chronic lymphocytic leukemia B-cell non-Hodgkin lymphoma | With TGR1202, Pembrolizumab | |||
I/II Ongoing | Chronic lymphocytic leukemia Waldenstrom macroglobulinemia Mantle cell lymphoma Marginal zone lymphoma B-cell lymphoma | With Pirtobrutinib, Venetoclax, Rituximab | |||
Parsaclisib (INCB50465) | II Ongoing | Lymphoma | Monotherapy | ||
I Completed | Advanced malignancies | Monotherapy | |||
II Ongoing | Lymphoma | Monotherapy | |||
II Completed | Lymphoma | Monotherapy | |||
I Ongoing | Lymphoma | Monotherapy | |||
III Ongoing | Myelofibrosis Primary myelofibrosis Post essential thrombocythemia myelofibrosis Post polycythemia vera myelofibrosis | With Ruxolitinib, Placebo | |||
I/II Ongoing | Chronic lymphocytic leukemia Non-Hodgkin lymphoma | With Tafasitamab | |||
II Ongoing | Lymphoma | Monotherapy | |||
I Completed | Advanced malignancies | Monotherapy | |||
I/II Ongoing | Peripheral T-cell lymphoma | With Chidamide | |||
I Completed | B-cell lymphoma | With Rituximab, Bendamustine, Ibrutinib | |||
Zandelisib (ME-401) | II Ongoing | Follicular lymphoma Non-Hodgkin Lymphoma Marginal zone lymphoma | Monotherapy | ||
III Ongoing | Follicular lymphoma Non-Hodgkin lymphoma Marginal zone lymphoma | With Rituximab, Bendamustine, CHOP | |||
II Ongoing | Chronic lymphocytic leukemia | With Rituximab, Venetoclax | |||
Linperlisib (YY-20394) | I Ongoing | Advanced solid tumor | Monotherapy | ||
II Ongoing | Peripheral T/NK cell lymphoma | Monotherapy | |||
I/II Ongoing | Peripheral T-cell lymphoma | With Azacitidine Injection, Dasatinib, Tucidinostat, SHR2554, Apatinib, Camrelizumab | |||
IOA-244 | I Ongoing | Solid tumor, adult Non-Hodgkin lymphoma, adult Non-small-cell lung cancer Myelofibrosis Uveal melanoma | With Avelumab Injection, Cisplatin, Pemetrexed, Ruxolitinib | ||
Pan-PI3K | Copanlisib | FDA approved for marketing | Follicular lymphoma | Monotherapy | |
Buparlisib (BKM120) | III Ongoing | Head and neck cancer | With Paclitaxel | ||
I Ongoing | Mantle cell lymphoma Follicular lymphoma Diffuse large B-cell lymphoma | With Ibrutinib | |||
Pictilisib (GDC-0941) | II Completed | Non-small cell lung cancer | With Placebo, Bevacizumab, Carboplatin, Paclitaxel | ||
I Completed | Breast cancer | With Bevacizumab, Letrozole, Paclitaxel, Trastuzumab | |||
II Completed | Breast cancer | With Placebo, Paclitaxel | |||
SF1126 | I Completed | Advanced or metastatic solid tumors cancer | Monotherapy | ||
Pilaralisib (XL147) | II Completed | Endometrial cancer Endometrial neoplasms | Monotherapy | ||
I/II Completed | Breast cancer Breast neoplasms | With Trastuzumab, Paclitaxel | |||
I Completed | Non-small cell lung cancer | With Erlotinib | |||
PX-866 | II Completed | Prostate cancer | Monotherapy | ||
I Completed | Advanced solid tumors | Monotherapy | |||
II Completed | Glioblastoma | Monotherapy | |||
I/II Completed | Non-small cell lung cancer, squamous cell carcinoma of the head and neck | With Docetaxel | |||
ZSTK474 | I Completed | Neoplasms | Monotherapy | ||
CH5132799 | I Completed | Solid tumors | Monotherapy | ||
Dual PI3Kδ /PI3Kγ | Duvelisib (Copiktra) | FDA approved for marketing | Chronic lymphocytic leukemia Small lymphocytic lymphoma | Monotherapy | |
Tenalisib (RP6530) | I/II Completed | T-cell lymphoma | With Romidepsin | ||
II Completed | Non-Hodgkin lymphoma | Monotherapy | |||
II Ongoing | Locally advanced breast cancer Metastatic breast cancer | Monotherapy | |||
II Ongoing | Peripheral T-cell lymphoma | Monotherapy | |||
Dual PI3Kα/PI3Kδ | TQ-B3525 | I/II Ongoing | Non-small-cell Lung cancer | With Osimertinib Mesylate tablets | |
II Ongoing | Peripheral T-cell lymphoma | Monotherapy | |||
I/II Ongoing | Relapsed/refractory chronic lymphocytic leukemia/small lymphocytic lymphoma | Monotherapy | |||
II Ongoing | Diffuse large B-cell lymphoma | Monotherapy | |||
II Ongoing | Relapsed/refractory follicular lymphoma | Monotherapy | |||
II Ongoing | Advanced endometrial cancer, cervical cancer, and ovarian cancer | Monotherapy | |||
