Table 3.
Summary of small molecule inhibitor clinical trials in human cancers. Data taken from http://clinicaltrials.gov/.
| Drug | Combination | Sponsor | Tumor type | Sample size | Status | Recruitment Status | Clinical trial ID |
|---|---|---|---|---|---|---|---|
| PI3K inhibitors | |||||||
| BAY80-6946 (Copanlisib) | - | Bayer | Lymphoma, Non-Hodgkin’s | 227 | Phase II | Active | NCT01660451 |
| BKM120 | - | Hospices Civils de Lyon | Thyroid Cancers | 47 | Phase II | Active | NCT01830504 |
| BKM120 | - | SOLTI Breast Cancer Research Group | Triple Negative Metastatic Breast Cancer | 50 | Phase II | Completed | NCT01629615 |
| BKM120 | Centre Leon Berard | Metastatic Head and Neck Cancer Recurrent or Progressive | 70 | Phase II | Recruiting | NCT01737450 | |
| BKM120 | Cetuximab | University of Chicago | Recurrent or Metastatic Head and Neck Cancer | 30 | Phase II | Active | NCT01816984 |
| PQR309 | - | PIQUR Therapeutics AG | Lymphoma, Malignant | 72 | Phase II | Recruiting | NCT02249429 |
| - | Endometrial Clear Cell Adenocarcinoma | ||||||
| - | Endometrial Adenosquamous Carcinoma | ||||||
| BKM120 | Trastuzumab | Novartis Pharmaceuticals | HER2-positive Primary Breast Cancer | 50 | Phase I/II | Completed | NCT01816594 |
| BYL719 | Paclitaxel | Priyanka Sharma | HER-2 Negative Breast Cancer | 44 | Phase I/II | Active | NCT02379247 |
| Taselisib | Enzalutamide | Vanderbilt-Ingram Cancer Center | AR Positive Triple-Negative Metastatic Breast Cancer | 73 | Phase I/II | Recruiting | NCT02457910 |
| Idelalisib | Entospletinib | Hematologic Malignancies | 66 | Phase I/II | Completed | NCT01796470 | |
| GSK2636771 | Pembrolizumab | M.D. Anderson Cancer Center | Metastatic Melanoma and PTEN Loss | 41 | Phase I/II | Recruiting | NCT03131908 |
| Everolimus | Exemestane | Novartis Pharmaceuticals | Metastatic Breast Cancer with ER+ | Phase III | Completed | NCT00863655 | |
| Akt inhibitors | |||||||
| Akt Inhibitor MK2206 | - | National Cancer Institute (NCI) | Endometrial Adenocarcinoma | 37 | Phase II | Completed | NCT01307631 |
| Akt Inhibitor MK2206 | - | National Cancer Institute (NCI) | CRC | 18 | Phase II | Completed | NCT01802320 |
| MK-2206 + AZD6244 | - | National Cancer Institute (NCI) | Colorectal Neoplasms | 21 | Phase II | Completed | NCT01333475 |
| mTOR inhibitors | |||||||
| Everolimus | Vinorebine | AIO-Studien-gGmbH | Advanced Breast Cancer | 139 | Phase II | Completed | NCT01520103 |
| BEZ235 | - | Novartis Pharmaceuticals | Pancreatic Neuroendocrine Tumors (pNET) | 31 | Phase II | Completed | NCT01658436 |
| Rapamycin | - | The University of Texas Health Science Center at San Antonio | Cancer of Breast | 60 | Phase II | Recruiting | NCT02642094 |
| Everolimus | - | M.D. Anderson Cancer Center | Endometrial Cancer | 270 | Phase II | Recruiting | NCT02397083 |
| Everolimus | - | University of Texas Southwestern Medical Center | Children With Recurrent or Progressive Ependymoma | 18 | Phase II | Recruiting | NCT02155920 |
| Everolimus | - | National Cancer Institute (NCI) | Kidney Cancer or Renal Cancer | 18 | Phase II | Recruiting | NCT02504892 |
| TAK-228 | - | Fox Chase Cancer Center | Soft Tissue Sarcomas | 33 | Phase II | Recruiting | NCT02987959 |
| AZD2014 | - | Canadian Cancer Trials Group | Glioblastoma Multiforme | 52 | Phase II | Recruiting | NCT02619864 |
| Everolimus | Cisplatin | Jenny C. Chang, MD | Triple Negative Breast Cancer | 32 | Phase I/II | Recruiting | NCT01931163 |
| Everolimus | Sorafenib Tosylate | Alliance for Clinical Trials in Oncology | Thyroid Cancer | 34 | Phase I/II | Recruiting | NCT02143726 |
| Everolimus | LEE011 | Memorial Sloan Kettering Cancer Center | Neuroendocrine Tumors | 41 | Phase I/II | Recruiting | NCT03070301 |
| Sirolimus+ | Cisplatin | University of Washington | Bladder Cancer | 21 | Phase I/II | Completed | NCT01938573 |
| Enzalutamide | LY3023414 | Eli Lilly and Company | Prostate Cancer | 144 | Phase I/II | Recruiting | NCT02407054 |
| ERK1/2 and MAPK inhibitors | |||||||
| Regorafenib | - | Gerald Batist | Metastatic Colorectal Cancer | 52 | Phase II | Recruiting | NCT01949194 |
| Vandetanib | - | Ronald Weigel | Invasive Breast Cancer | 100 | Phase II | Recruiting | NCT01934335 |
| BVD-523 | - | BioMed Valley Discoveries, Inc | Myelodysplastic Syndrome | 53 | Phase II | Completed | NCT02296242 |
| TDM1 | Abraxane, Lapatinib | Jenny C. Chang, MD | Metastatic HER2 Positive Breast Cancer | 45 | Phase I/II | Recruiting | NCT02073916 |
| LY2228820 | Radiotherapy + TMZ | Centre Jean Perrin | Newly Diagnosed Glioblastoma | 50 | Phase I/II | Recruiting | NCT02364206 |
| Dabrafenib | Pazopanib hydrochloride | Manisha Shah | Unspecified Adult Solid Tumor | 56 | Phase 1 | Active, not recruiting | NCT01713972 |
| GSK2118436 | GSK1120212 | Novartis Pharmaceuticals | Cancer | 430 | Phase 2 | Active, not recruiting | NCT01072175 |
| NFκB inhibitors | |||||||
| Pentoxifylline | - | Ramón Óscar González-Ramella, Ph.D | Pediatric Acute Lymphoblastic Leukemia | 44 | Phase II | Recruiting | NCT02451774 |
| Dexamethasone | - | Emory University | Plasma Cell Myeloma | 90 | Phase II | Recruiting | NCT02765854 |
| Ibrutinib | - | Icahn School of Medicine at Mount Sinai | Multiple Myeloma Patients | 36 | Phase II | Recruiting | NCT02943473 |
| Lansoprazole | - | National Health Research Institutes, Taiwan | Early-stage HP(+) Gastric Pure DLBCL | 30 | Phase II | Recruiting | NCT02388581 |
| Ibrutinib | Rituximab | Samsung Medical Center | EB+ Diffuse Large B-cell Lymphoma | 24 | Phase I/II | Recruiting | NCT02670616 |