Table II.
Classification and examples of protein kinase C (PKC) inhibitors
PKC class | Example | Isozyme affected | Route of administration | Phase of development | Comments |
---|---|---|---|---|---|
Indocarbazole class | Enzastaurin | PKC β | Oral | Phase I–III | |
Midostaurin (PKC-412) | PKC α, β, γ, δ, ε, η | Oral | Phase I–II | ||
UCN-01 | Conventional > novel PKC isoforms | Intravenous | Phase I–II | ||
Biological agents | Bryostatin | Conventional > novel | Oral | Phase I–II | Behaves as a short-term PKC activator and long-term inhibitor |
Curcumin | PKC isoforms | Intravenous | Phase I–III | ||
Antisense oligonucleotides | Aprinocarsen (ISIS-3521) | Predominantly targets PKC α | Oral | Phase I–III | |
Others | Tamoxifen | PKC α, δ, ε | Oral | Phase II, currently on the market | Positive control studies in bipolar mania; also is an anti-estrogen |