Proapoptotic Sulindac Analog CP-461

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable second-generation selective apoptotic antineoplastic drug (SAAND) and analog of the nonsteroidal anti-inflammatory drug (NSAID) sulindac, with potential pro-apoptotic and antineoplastic activities. Upon administration, CP-461 specifically binds to and blocks the activity of cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway. Inhibition of cGMP-PDE permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death. cGMP-PDE is overexpressed in a variety of cancer cell types; therefore, CP-461 selectively induces apoptosis in cancer cells, with minimal or no effect in healthy cells.

**Synonyms:** - 1H-Indene-3-acetamide, 5-Fluoro-2-methyl-N-(phenylmethyl)-1-(4-pyridinylmethylene)-, Monohydrochloride, (1Z)- - CEL 031 - CP 461 - CP-461 - CP-461 - CP461 - OSI 461