Table 3.
Ongoing clinical trials involving AKT inhibitors as registered on clinicaltrials.gov as of October 2015
| Drug | Company | Alternative names | Targets | Trial phase | Cancer‐specific trials |
|---|---|---|---|---|---|
| GSK2141795 | GlaxoSmithKline | Uprosertib | Pan‐AKT isoforms (competitive) | I/II | Advanced solid tumours with trametinib, dabrafenib |
| II | AML with trametinib | ||||
| II | Multiple myeloma with trametinib | ||||
| II | Triple negative BC with trametinib | ||||
| AZD5363 | AstraZeneca | Pan‐AKT isoforms (competitive) | I | Solid tumours with olaparib | |
| I/II | Castrate resistant prostate Ca with docetaxel | ||||
| I/II | Endometrial and ovarian Ca with mTORC1/2 inhibitor AZD2014 | ||||
| II | Castrate Resistant Prostate Ca with enzalutamide | ||||
| II | ER+ breast cancer | ||||
| II | Triple negative BC with paclitaxel | ||||
| GSK2110183 | GlaxoSmithKline | Afuresertib | Pan‐AKT isoforms (competitive) | Ib | Gastric Ca with paclitaxel |
| I/II | Multiple myeloma with carfilzomib | ||||
| II | Continuation study for responders in solid/haematological malignancies | ||||
| II | CLL with ofatumumab | ||||
| GDC‐0068 | Genentech | Ipatasertib | Pan‐AKT isoforms (competitive) | I/II | Glioblastoma |
| II | Neoadjuvant treatment of triple negative BC with paclitaxel | ||||
| II | Metastatic triple negative BC with paclitaxel (first‐line) | ||||
| MSC‐2363318A | Merck Sorono | Pan‐AKT isoforms and p70S6K inhibitor (competitive) | I | Solid tumours | |
| LY2780301 | Lilly | Pan‐AKT isoforms and p70S6 kinase inhibitor (competitive) | Ib | Solid tumours and NHL with gemcitabine | |
| Ib/II | HER2+ metastatic BC with paclitaxel | ||||
| MK‐2206 | Merck | Pan‐AKT isoforms (allosteric) | I | Pancreatic Ca‐ with dinaciclib | |
| II | HR+ breast cancer with anastrozole/goserelin | ||||
| II | Lung or thymic Ca; only patients with AKT, PTEN, or PIK3CA mutations | ||||
| BAY‐1125976 | Bayer | AKT1/2 isoform inhibitor (allosteric) | I | Solid tumours | |
| ARQ 092 | ArQule | Pan‐AKT isoforms (allosteric) | I | Solid tumours and lymphoma. | |
| Ib | Triple negative BC and gynaecological cancers with carboplatin and paclitaxel | ||||
| KRX‐0401 | Aeterna Zentaris | Perifosine | Pan‐AKT (lipid‐based/PIP3 inhibitor) | II | Gliomas combined with temsirolimus |
| PTX‐200 | Prescient Therapeutics | Triciribine | PH domain (AKT) inhibitor | I/II | Advanced or metastatic HER2‐negative BC with paclitaxel, doxorubicin and cyclophosphamide |
| AG1343 | Roche | Nelfinavir; Viracept | HIV protease inhibitor, AKT | I/II | Multiple myeloma with lenalidomide + dexamethasone |
| ‐‐‐ | Multiple trials in multiple Ca types as radiosensitizing agent | ||||
| ONC‐201 | Oncoceutics | TRAIL pathway inducing compound/indirect AKT inhibitor | I | Solid tumours | |
| I/II | Relapsed/refractory NHL | ||||
| I/II | Relapsed/refractory AML and high‐risk MDS | ||||
| Archexin | Rexahn | AKT1 antisense oligonucleotide | I/II | Renal cell Ca with everolimus | |
AML, acute myeloid leukaemia; BC, breast cancer; Ca, cancer; CLL, chronic lymphocytic leukaemia; DLBCL, diffuse large B‐cell lymphoma; ER, oestrogen receptor; HER2, human epidermal growth factor receptor 2; HIV, human immunodeficiency virus; HR, hormone receptor; MDS, myelodysplastic syndrome; mTOR, mammalian target of rapamycin; NHL, non‐Hodgkin's lymphoma; PH, pleckstrin homology; PIP3, phosphatidylinositol 3,4,5‐trisphosphate; PIK3CA, PIK3 catalytic subunit alpha; PTEN, phosphatase and tensin homologue deleted on chromosome 10; TRAIL, tumour necrosis factor‐related apoptosis‐inducing ligand.