Table 2. Class I PI3K/mTOR inhibitors in clinical trials.
| Compound | Target | Indication | Clinical trial identifier |
|---|---|---|---|
| BYL-719 | p110α | Recurrent or Metastatic Squamous Cell Carcinoma |
NCT02145312, Phase 1/2 |
| MLN1117 (INK-1117) | p110α | Advanced Nonhaematologic Malignancies |
NCT01899053, Phase 1b |
| AZD6482 | p110β | Antiplatelet Effect | NCT00853450, Phase 1 |
| AMG 319 | p110δ | Haematologic Malignancies | NCT01300026, Phase 1 |
| GSK2269557 | p110δ | COPD | NCT02294734, Phase 2 |
| Idelalisib (CAL-101) | p110δ | Chronic Lymphocytic Leukaemia (CLL) Non-Hodgkin Lymphoma |
FDA and EMA approved, 2014 |
| INCB040093 | p110δ | B cell malignancies | NCT01905813, Phase 1 |
| TGR-1202 | p110δ | Cancer (CLL and B-cell lymphoma) | NCT01767766, Phase 1 |
| UCB-5857 | p110δ | Psoriasis | NCT02303509, Phase 1 |
| AZD8835 | p110α/p110δ | Advanced Solid Malignancies | NCT02260661, Phase 1 |
| BAY80-6946 (Copanlisib) | p110α/p110δ | Non-Hodgkin’s Lymphoma | NCT01660451, Phase 2 |
| GDC-0941 (Pictilisib) | p110α/p110δ | Breast Cancer | NCT01437566, Phase 2 |
| AZD8186 | p110β/p110δ | Prostate, Lung and Breast Cancer | NCT01884285, Phase 1 |
| GS-9820 (Acalisib) | p110β/p110δ | Lymphoid Malignancies | NCT01705847 Phase 1b |
| IPI-145 (Duvelisib) | p110δ/p110γ | Non-Hodgkin Lymphoma Small lymphocytic lymphoma; CLL |
NCT01882803, Phase 2 NCT02004522, Phase 3 |
| RP-6530 | p110δ/p110γ | Haematologic malignancies | NCT02017613, Phase 1 |
| RV-1729 | p110δ/p110γ | Asthma/COPD | NCT01813084, Phase 1 |
| BKM120 | pan-class I | Metastatic Breast Cancer | NCT01633060, Phase 3 |
| XL-147 (SAR245408) | pan-class I | Malignant neoplasm | NCT01587040, Phase 1 |
| ZSTK474 | pan-class I | Advanced Solid Malignancies | NCT01682473, Phase 1 |
| BEZ235 | pan-class I/mTOR | Renal Cancer | NCT01453595, Phase 1/2 |
| BGT226 | pan-class I/mTOR | Solid Tumours, Breast Cancer | NCT00600275, Phase 1/2 |
| GSK2126458 | pan-class I/mTOR | Solid Tumours Pulmonary Fibrosis |
NCT00972686, Phase 1 NCT01725139, Phase 1 |
| VS-5584 | pan-class I/mTOR | Non-haematologic metastatic cancer Lymphoma |
NCT01991938, Phase 1 |
| XL-765 (SAR245409) | pan-class I/mTOR (p110γ) | Malignant neoplasm | NCT01587040, Phase 2 |
| PX866 | pan PI3K | Metastatic prostate cancer | NCT01331083, Phase 2 |
| SF1126 | pan PI3K | Neuroblastoma | NCT02337309, Phase 1 |
| AQX-1125 | SHIP1 activator | COPD Atopic Dermatitis Interstitial Cystitis |
NCT01954628, Phase 2 NCT02324972, Phase 2 NCT01882543, Phase 2 |