Tesmilifene

Description

Tesmilifene is a small molecule chemopotentiator under development by YM BioSciences, a Candian pharmaceutical company that specialises in the development of cancer treatments. It is indicated for use in combination with standard cytotoxic drugs, such as taxanes and anthracyclines, which are widely used in the treatment of metastatic disease – when cancers spread to distant sites in the body.

Characteristics

Tesmilifene is a diphenylmethane derivative that is structurally related to the triphenylethylene derivative tamoxifen but lacks the stilbene bridge and third phenyl ring necessary for binding to the estrogen receptor (ER), and as such, it is not a selective estrogen receptor modulator (SERM). In addition to tamoxifen, tesmilifene is structurally related to diphenylmethane antihistamines like diphenhydramine and hydroxyzine, but is much weaker than these agents in assays of anti-H1 receptor activity, and hence, neither acts as an antihistamine.

Definition

ChEBI: N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine is a diarylmethane.