The apparent volume of distribution of toremifene ranged from 457 to 958 L.

Metabolism
Toremifene is metabolized in the liver primarily by CYP3A4 and then undergoes secondary hydroxylation. The metabolites of toremifene include N-desmethyltoremifene, 4-hydroxytoremifene, and 4-hydroxy-N-desmethyltoremifene, among others. Ospemifene (deaminohydroxytoremifene) is also a major metabolite of toremifene. Elimination
The elimination half-life of toremifene is 3 to 7 days in healthy individuals. In people with impaired liver function, the half-life is 11 days. The elimination half-lives of the metabolites of toremifene are 5 to 21 days for N-desmethyltoremifene, 5 days for 4-hydroxytoremifene, and 4 days for ospemifene. The long elimination half-lives of toremifene and its metabolites are thought to be due to enterohepatic recirculation and high plasma protein binding. Toremifene is eliminated 70% in the feces, as metabolites. Chemistry
Toremifene, also known as 4-chlorotamoxifen, is a derivative of triphenylethylene and a close analogue of tamoxifen. It is also closely related to afimoxifene (4-hydroxytamoxifen) and ospemifene (deaminohydroxytoremifene). History
Toremifene was introduced in the United States in 1997. It was the first antiestrogen to be introduced in this country since tamoxifen in 1978. Society and culture
Generic names
Toremifene is the generic name of the drug and its INN and BAN, while toremifene citrate is its USAN and JAN and torémifène is its DCF. Brand names
Toremifene is marketed almost exclusively under the brand name Fareston. Availability
Toremifene is marketed widely throughout the world and is available in the United States, the United Kingdom, Ireland, many other European countries, South Africa, Australia, New Zealand, and elsewhere throughout the world.
However, clinical studies have found no significant differences between toremifene and tamoxifen, including in terms of effectiveness, tolerability, and safety, and hence the clinical use of toremifene has been somewhat limited. Toremifene is thought to have about one-third of the potency of tamoxifen; i.e., 60 mg toremifene is roughly equivalent to 20 mg tamoxifen in the treatment of breast cancer.Toremifene has been found to have antigonadotropic effects in postmenopausal women, progonadotropic effects in men, to increase sex hormone-binding globulin levels, and to decrease insulin-like growth factor 1 levels by about 20% in postmenopausal women and men.In addition to its activity as a SERM, 4-hydroxytoremifene is an antagonist of the estrogen-related receptor γ (ERRγ). Pharmacokinetics
Absorption
The bioavailability of toremifene has not been precisely determined but is known to be good and has been estimated to be approximately 100%. Levels of toremifene at steady state with a dosage of 60 mg/day are 800 to 879 ng/mL. Levels of N-desmethyltoremifene at steady state with toremifene were 3,058 ng/mL at 60 mg/day, 5,942 ng/mL at 200 mg/day, and 11,913 ng/mL at 400 mg/day. Levels of 4-hydroxytoremifene at steady state with toremifene were 438 ng/mL at 200 mg/day and 889 ng/mL at 400 mg/day. Concentrations of toremifene increase linearly across a dose range of 10 to 680 mg.

Distribution
Toremifene is 99.7% bound to plasma proteins, with 92% bound specifically to albumin, about 6% to β1 globulin fraction, and about 2% to a fraction between albumin and α1 globulins.