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. 2011 Dec 15;12(12):1032–1049. doi: 10.4161/cbt.12.12.18442

Table 1.

Pharmacological agents that are under clinical evaluation for inhibiting PI3K/Akt3 pathway in melanomas

Agent Target Assay to measure the efficacy Drawbacks/reasons for failure in clinic Ref.
Perifosine Western blotting and Immunohistochemistry Lack of objective response, gastrointestinal and hematological toxicity 9496, 154165
17-AAG HSP90, MAPK and Akt Western blot and immunohistochemistry Lack of objective response, Lack of target inhibition 167170
CCI-779 mTOR Immunohistochemistry Lack of sufficient antitumor activity, mild to moderate toxic side effects 128, 171, 172
RAD001 mTOR Immunohistochemistry No objective clinical response, grade-2 toxicity 128, 173
API-2 Akt Western blotting Toxic side effects including hepatotoxicity, hyperglycemia, thrombocytopenia 110113
Riluzole GRM1 Immunohistochemistry Mild toxicities including dryness in mouth, dizziness, and neurologic toxicity 176180