Toremifene citrate improves HDL in men on testosterone therapy

Nelson Vergel

Founder, ExcelMale.com
The Journal of Urology
Volume 199, Issue 4, Supplement, April 2018, Page e1171

Sexual Function/Dysfunction: Medical, Hormonal & Non-surgical Therapy II

MP85-06 TOREMIFENE CITRATE IMPROVES HIGH-DENSITY LIPOPROTEIN LEVELS IN MEN ON TESTOSTERONE REPLACEMENT THERAPY


INTRODUCTION AND OBJECTIVES
Decreases in high-density lipoprotein (HDL) levels have been observed in men on testosterone therapy (TTh). Niacin is commonly used as a therapy for low HDL, although its side effect (SE) profile often leads to frequent discontinuation. Toremifine citrate is an oral selective estrogen modulator (SERM) that is well tolerated and can improve lipid profiles by raising HDL levels in both breast and prostate cancer patients. Here we assess the role of toremifene in the management of HDL abnormalities in men on TTh.

METHODS
Men on TTh with low HDL levels (<39 mg/dL) at a single andrology clinic treated between October 2015 and August 2017 with either toremifine (60 mg daily), niacin (titrated to 1,000 mg daily over 2 months) plus krill oil (1,000 mg daily) (NKO), or no treatment (patient refusal) were reviewed in a retrospective intent-to-treat analysis. Patient age, type of TTh, length of follow-up, and baseline and subsequent non-fasting lipid panels, total testosterone (TT) levels, and estrogen (E) levels were determined. Analysis of variance (ANOVA) was used to determine differences between groups.

RESULTS
A total of 75 men with low HDL levels on injectable TTh were included (34 treated with toremifine, 17 treated with NKO, and 24 untreated). No differences in the mean (SD) age between the cohorts (39.2 (10.2) years for whole cohort), baseline laboratory values, or the mean duration of follow-up (6.4 (4.1) months, for whole cohort). Changes in laboratory values are listed in Table 1. Only the change in HDL was significant between the groups during follow-up, with both toremifine and NKO resulting in significant improvements in HDL when compared with untreated men (p = 0.02 and 0.01, respectively). No significant difference in the change in HDL between toremifine vs NKO was observed. 3 men (17.6%) stopped niacin prior to follow up secondary to intolerable SEs (flushing), whereas no men stopped toremifine due to SEs.

CONCLUSIONS
Toremifine results in improvement in HDL in men with low HDL on TTh similar to that observed with niacin + krill oil. However, toremifine is better tolerated than niacin and could serve as an reasonable alternative treatment for low HDL in men on TTh. Prospective studies are needed to validate these results.
 

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Estradiol (E2)

A form of estrogen produced from testosterone. Important for bone health, mood, and libido. Too high can cause side effects; too low can affect well-being.

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Dihydrotestosterone is a potent androgen derived from testosterone. Affects hair growth, prostate health, and masculinization effects.

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The biologically active form of testosterone not bound to proteins. Directly available for cellular uptake and biological effects.

Scientific Reference

Lakshman KM, Kaplan B, Travison TG, Basaria S, Knapp PE, Singh AB, LaValley MP, Mazer NA, Bhasin S. The effects of injected testosterone dose and age on the conversion of testosterone to estradiol and dihydrotestosterone in young and older men. J Clin Endocrinol Metab. 2010 Aug;95(8):3955-64.

DOI: 10.1210/jc.2010-0102 | PMID: 20534765 | PMCID: PMC2913038

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