Table 3.
A summary of major AKT inhibitors.
| Inhibitor | Compound | Inventor | IC50 (nmol/L) | Phase | Clinical |
|---|---|---|---|---|---|
| Allosteric inhibitor | MK-2206 | Merck | Akt1/2/3: 8/12/65 | II | NCT01277757 |
| BAY 1125976 | Bayer | Akt1/Akt2: 5.2/18 | Terminated | ||
| TAS-117 | Takeda | Akt1/Akt2/Akt3: 4.8/1.6/44 |
II | NCT03017521 | |
| Miransertib(ARQ-092) | ArQule | Akt1/Akt2/Akt3: 2.7/14/8.1 |
II | NCT03094832 | |
| ALM301 | Almac Discovery Ltd | Akt1/2: 125/95 | Preclinical | ||
| Competitive inhibitor | Capivasertib(AZD5363) | AstraZeneca | Akt1/Akt2/3: 3/8/8 |
III-Ongoing | NCT03997123 |
| Afuresertib(GSK2110183) | GlaxoSmithKlie | Akt1/Akt2/Akt3: 0.08/ 2/ 2.6 (Ki) |
II | NCT01532700 | |
| Uprosertib(GSK2141795) | GlaxoSmithKlie | Akt 1/2/3: 180/328/38 |
II | NCT01907815 | |
| Ipatasertib(GDC0068) | Roche | Akt1/2/3: 5/18/8 | III-Ongoing | NCT03072238 | |
| NTQ1062 | Zhengda Tianqing | Akt1/Akt2/Akt3: 0.4 /6.3/0.1 |
I | CTR20211999 |