▾ Testosterone undecanoate – oral therapy for male hypogonadism

1985 ◽  
Vol 23 (2) ◽  
pp. 7-8
Keyword(s):  
Systemic Circulation ◽  
Plasma Testosterone ◽  
Testosterone Replacement Therapy ◽  
Sublingual Administration ◽  
Male Hypogonadism ◽  
Testosterone Undecanoate ◽  
Natural Hormone ◽  
Oral Preparation ◽  
Loss Of Libido ◽  
The Uk

In men with sexual dysfunction due to hypogonadism, plasma testosterone is by definition low; testosterone replacement therapy may help to overcome impotence and loss of libido, but not infertility. Oral administration of the natural hormone is inefficient because testosterone, like some other natural steroids, is rapidly inactivated in the gut wall and liver. Sublingual administration allows direct absorption into the systemic circulation, but frequent dosing is needed. Testosterone is therefore usually given in the UK as an ester by intramuscular injection every 2 – 4 weeks, or by surgical insertion of an implant every 3 – 6 months with risk of extrusion1, infection or haematoma formation.2 An oral preparation which raised plasma testosterone predictably when given by mouth would therefore represent a significant therapeutic advance. This is what Restandol (Organon) - testosterone undecanoate dissolved in oleic acid - is claimed to offer.

scholarly journals Spotlight on a New Heme Oxygenase Pathway: Testosterone-Induced Shifts in Cardiac Oxidant/Antioxidant Status

Antioxidants ◽  
2019 ◽  
Vol 8 (8) ◽  
pp. 288 ◽  
Author(s):  
Renáta Szabó ◽  
Denise Börzsei ◽  
Krisztina Kupai ◽  
Alexandra Hoffmann ◽  
Rudolf Gesztelyi ◽  
...  
Keyword(s):  
Replacement Therapy ◽  
Heme Oxygenase ◽  
Testosterone Level ◽  
Antioxidant Status ◽  
Hormone Replacement ◽  
Plasma Testosterone ◽  
Testosterone Replacement Therapy ◽  
Testosterone Undecanoate ◽  
Inflammatory Status ◽  
Tnf Α

A low testosterone level contributes to the development of oxidative damages; however, the cardiovascular effects of exogenous hormone therapy are not well elucidated. The aim of our work is to study the association of the testosterone level, antioxidant/oxidant system, and anti-inflammatory status related to the heme oxygenase (HO) system. To determine the effects of testosterone, 10-week-old, and 24-month-old sham-operated and castrated male Wistar rats were used. One part of the castrated animals was daily treated with 2.5 mg/kg cyproterone acetate, while the hormone replacement therapy was performed via an i.m. injection of a dose of 8.0 mg testosterone undecanoate/kg/once a week. The plasma testosterone level, the activity of HO and myeloperoxidase (MPO) enzymes; the concentrations of the HO-1, tumor necrosis alpha (TNF-α), and cyclic guanosine monophosphate (cGMP), as well as the total level of glutathione (GSH + GSSG) were determined from the cardiac left ventricle. In accordance with the testosterone values, the aging process and castration resulted in a decrease in antioxidant HO activity, HO-1 and cGMP concentrations and in the level of GSH + GSSG, whereas the inflammatory TNF-α and MPO activity significantly increased. Testosterone therapy was able to restore the physiological values. Our results clearly show that testosterone replacement therapy increases the antioxidant status and mitigates the inflammatory parameters via the modulation of the HO system.

scholarly journals Efficacy and Safety of TLANDO, A Novel Oral Easy to Prescribe and Use TRT Option

2021 ◽  
Vol 5 (Supplement_1) ◽  
pp. A486-A486
Author(s):  
Kongnara Papangkorn ◽  
Kiran Vangara ◽  
Benjamin J Bruno ◽  
Kilyoung Kim ◽  
Nachiappan Chidambaram ◽  
...  
Keyword(s):  
Dose Adjustment ◽  
Dose Titration ◽  
Testosterone Replacement Therapy ◽  
Male Hypogonadism ◽  
Open Label ◽  
Testosterone Undecanoate ◽  
Pivotal Study ◽  
Require Dose ◽  
Gradual Dose ◽  
Selection Of

Abstract Most widely used testosterone replacement therapy (TRT) products can be inconvenient and cumbersome topical and invasive injectable requiring dose adjustments to attain efficacy. In a pivotal study, a recently approved oral TRT only 26% of patients did not require any dose adjustment. Typically, patients start on a sub-therapeutic dose with gradual dose increases to attain efficacy resulting in additional visit(s) to clinic and pharmacy. Physician research data (N=402) suggested it typically takes 3-6 months of titrations to reach an efficacious dose for majority of patients, a significant barrier in effecting a switch without a period of “efficacy gap”. The requirement of additional visit(s) presents significant challenges for new and current patients desiring to start and to switch to a convenient TRT option, especially in the current COVID-19 pandemic. Recent reports suggest increase of disease severity/mortality in men with low testosterone is possibly due to underlying co-morbidities commonly associated with male hypogonadism. There remains a need for an effective, safe, and easy to use and prescribe product that does not require dose titration. TLANDO is a “triglyceride-free” oral single strength TRT with single dose designed to lymphatically deliver effective and safe levels of testosterone regardless of meal fat content. Moreover, dose titration is prone to some inherent titration decision errors and requires understanding of often complex titration rules. The objective is to assess whether TLANDO, an oral TRT without requiring dose titration, safely restores effective testosterone (T) levels in hypogonadal men. An open-label, single-arm, multicenter study (NCT03242590) was performed with TLANDO in hypogonadal males (N=95). Subjects received orally 225 mg twice a day testosterone undecanoate (TU) for 24 days without dose adjustment. Efficacy was evaluated by % of subjects who achieved daily T Cavg within the eugonadal range. Using 450mg daily dose without dose adjustment, 80% of subjects (95% CI of 72% to 88%) achieved a T Cavg in the normal range and safely restored with mean T Cavg of 476±184 ng/dL post steady state. T restoration was comparable to other non-oral TRT products. TLANDO was well tolerated with no deaths, no drug-related severe AEs, and no hepatic AEs. In conclusion, effective T restoration using TLANDO, an easy to use and prescribe oral TRT option, was confirmed. Minimal AEs were reported with no hepatic AEs. Upon approval, TLANDO will be the first convenient TRT option without requiring dose adjustments; therefore, enabling selection of an efficacious dose from the start of therapy. TLANDO is well suited for new or existing TRT patients desiring a convenient oral option.

scholarly journals TLANDO, a Novel Oral TRT, Improves Sexual and Mental Domain Outcomes in Hypogonadal Men

2021 ◽  
Vol 5 (Supplement_1) ◽  
pp. A495-A496
Author(s):  
Benjamin J Bruno ◽  
Kiran Vangara ◽  
Kilyoung Kim ◽  
Kongnara Papangkorn ◽  
Nachiappan Chidambaram ◽  
...  
Keyword(s):  
Active Control ◽  
Dose Adjustment ◽  
Short Form ◽  
Fixed Dose ◽  
Dose Titration ◽  
Testosterone Replacement Therapy ◽  
Male Hypogonadism ◽  
Dosing Regimen ◽  
Testosterone Undecanoate ◽  
Patient Reported

Abstract Male hypogonadism is characterized by symptoms and deficiency (<300 ng/dL) in levels of in total testosterone (TT), a critical hormone for sexual, cognitive, and body function and development. TLANDO, a testosterone undecanoate (TU) comprising lymphatically delivered oral testosterone replacement therapy (TRT) option not requiring dose titration, treatment has demonstrated effective restoration in hypogonadal men of TT levels to the eugonadal range in multiple clinical studies. TLANDO therapy resulted in decreased sex hormone binding globulin with increased free testosterone (FT). TLANDO’s unique delivery system enables consistent restoration of TT regardless of meal fat content. Moreover, TLANDO has shown potential to improve liver health through resolution of fatty liver disease in hypogonadal men and is not known to have any adverse liver effects. However, it is unclear if fixed dose TLANDO therapy without dose adjustment improves symptoms of psychosexual functions. The objective is to assess key sexual and mental domain Patient Reported Outcomes (PRO) post 52 weeks of treatment using TLANDO on the to-be-marketed dosing regimen in comparison with a widely used topical TRT, Androgel 1.62%. Data analysis was performed in in hypogonadal males post TLANDO treatment without dose adjustment, and in patients on the active control from a randomized, multi-center, open label, active controlled 52-week trial (SOAR, NCT02081300). Sexual and mental domain function PROs were measured at baseline (BL) and end of study (EOS) using Psychosexual Daily Questionnaire (PDQ) and Short Form (SF)-36 surveys and compared between TLANDO and active control. Post treatment with TLANDO dosing regimen not requiring dose titration, key sexual domain function PROs at week 52 were significantly (p<0.05) improved from BL: positive mood (BL:4.5 vs EOS:5.1, p<0.001), negative mood (1.8 vs 1.4, p<0.01), overall sexual desire (2.5 vs 3.7, p<0.001), sexual activity (2.5 vs 4.0, p<0.001), highest pleasure with partner (2.0 vs 2.8, p=0.06), highest pleasure without partner (1.8 vs 2.4, p<0.05), weekly maintained erection (3.3 vs 4.5, p<0.001), and weekly full erection % (50.5% vs 68.9%, p<0.001). Most sexual and mental function PROs were comparable to Androgel 1.62. TLANDO therapy was well tolerated through 52 weeks of treatment exposure. In conclusion, TLANDO, a novel easy to use and prescribe TRT not requiring dose titration, demonstrated improvement in sexual and mental PROs, a significant unmet need in hypogonadal males. Further placebo-controlled studies are warranted to better elucidate these improvements.

scholarly journals Effect of testosterone undecanoate on hematological profiles, blood lipid and viscosity and plasma testosterone level in castrated rabbits

2013 ◽  
Vol 7 (3-4) ◽  
pp. e221-5 ◽  
Author(s):  
Chen Zhao ◽  
Du Geon Moon ◽  
Jong Kwan Park
Keyword(s):  
Cardiovascular Disease ◽  
Replacement Therapy ◽  
Blood Viscosity ◽  
Whole Blood ◽  
Density Lipoprotein ◽  
Plasma Testosterone ◽  
Testosterone Replacement Therapy ◽  
Testosterone Undecanoate ◽  
Whole Blood Viscosity ◽  
Long Acting

Objective: The association between testosterone replacement therapy and cardiovascular risk remains controversial. Blood viscosity is a known individual risk factor for cardiovascular disease mortality. The objective of the present study was to investigate the effects of the long-acting injectable testosterone undecanoate (TU) on risk factors of cardiovascular disease. Methods: Twenty four male New Zealand white rabbits (2.5 kg) were randomly divided into three groups of eight. The first group was used as control. The second group was castrated bilaterally. The third group was administrated with 6 mg/kg of TU at 1 day and 6 weeks after castration. Whole blood viscosity, total plasma testosterone, hemoglobin (Hb), hematocrit (Hct), fibrinogen (FBN), total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C) levels were measured at baseline, 6 weeks and 18 weeks. Results: In control group, whole blood viscosity and FBN were significantly increased at 6 and 18 weeks. Castration significantly increased the levels of TC, TG, HDL-C and LDL-C, but decreased Hct and Hb. In the TU injection group, whole blood viscosity was markedly decreased in all share rates, whereas the FBN level was increased. Hb and Hct showed a tendency for higher concentration at 6 weeks. Conclusions: Long-acting injectable TU provides another reliable treatment option for testosterone replacement therapy. Moreover, the patients may receive additional beneficial effect in lowered whole blood viscosity.

Cryptozoospermia after treatment with clomiphene citrate following long-term use of intramuscular testosterone undecanoate depot injection (Nebido®)

2019 ◽  
Vol 39 (2) ◽  
Author(s):  
Tanja Grubić Kezele
Keyword(s):  
Clomiphene Citrate ◽  
Hypogonadotropic Hypogonadism ◽  
Human Reproduction ◽  
Testosterone Replacement Therapy ◽  
Testosterone Undecanoate ◽  
Clinical Hospital ◽  
Receptor Modulator ◽  
Depot Injection ◽  
Gonadal Failure ◽  
Hospital Center

Abstract Objective To illustrate the importance of treatment duration with intramuscular testosterone undecanoate (Nebido®) for the final spermatogenesis recovery after treatment cessation. Also, to show a subsequent poor efficacy of the selective estrogen receptor modulator (SERM) clomiphene citrate (CC) in treating steroid-induced azoospermia following Nebido® cessation and describe that initial oligozoospermia, existing before starting Nebido®, largely contributes to that treatment outcome. Methodology Setting: Department of Human Reproduction and Department of Endocrinology, Clinical Hospital Center Rijeka, Rijeka, and Department of Endocrinology, Clinical Hospital Center Sestre milosrdnice, Zagreb, Croatia. Patient: A male patient having been diagnosed with primary hypogonadotropic hypogonadism, oligozoospermia and low testosterone (T) level, was treated with intramuscular testosterone undecanoate (TU) depot 1 g (Nebido®) to prevent further progression of testosterone deficiency symptoms (low mood, energy and concentration, fatigue, muscle weakness). Interventions: Stopping Nebido® and treatment with CC 50 mg per day 5 days per week for 3–6 month to recover spermatogenesis. Main outcome measures: T levels and semen analyses. Results Semen analyses did not return to values before taking Nebido® 1 year after cessation nor after 3 months of treatment with CC. Values of T, follicle stimulating hormone (FSH) and luteinizing hormone (LH) dropped even more than before starting Nebido®, after 1 year of cessation. Conclusions Here we describe a case of initially idiopathic gonadal failure with subsequent secondary gonadal failure and infertility resulting from testosterone replacement therapy (TRT) treatment, and poor spermatogenesis recovery outcome of CC used post Nebido® cessation.

scholarly journals Systemic glucocorticoid usage in dogs under primary veterinary care in the UK: prevalence and risk factors

2019 ◽  
Vol 185 (4) ◽  
pp. 108-108 ◽  
Author(s):  
Doaa A Elkholly ◽  
Dan O’Neill ◽  
Andrea K Wright ◽  
Kennedy Mwacalimba ◽  
Laura S Nolan ◽  
...  
Keyword(s):  
Primary Care ◽  
Medium Size ◽  
Age Group ◽  
Systemic Glucocorticoid ◽  
Oral Preparation ◽  
Systemic Glucocorticoids ◽  
Study Population ◽  
Long Acting ◽  
The Uk ◽  
To Receive

Glucocorticoids are widely used in primary care veterinary practices. The study aimed to quantify the usage of systemic glucocorticoids (SGC) in dogs in the UK using primary care treatment records recorded during 2013 in the VetCompass Programme. From a study population of 455 557 dogs, 28 472 dogs (6.2 per cent, 95 per cent CI 6.2 to 6.3) received a total of 50 971 SGC therapy events in 2013. Prednisolone represented the most frequently used oral preparation (27 362 events, 90.0 per cent of oral events). Dexamethasone sodium phosphate was the most commonly used injectable agent (12 796 events, 62.7 per cent of injectable events). The most common breed treated was Staffordshire Bull Terriers (2236/28 472 dogs, 7.9 per cent, 95 per cent CI 7.5 to 8.2) and within-breed prevalence of SGC usage was 2236/32 635, 6.9 per cent, 95 per cent CI 6.6 to 7.1. The most commonly treated age group was dogs older than eight years (8931/28472, 31.4 per cent) and the most commonly treated bodyweight group was 10.01–20.0 kg (7918/28 472, 27.8 per cent). Dexamethasone and prednisolone were the most commonly prescribed SGC. Short-acting and intermediate-acting injectable SGC were more commonly used compared with long-acting injectable SGC. Older and medium size dogs were most likely to receive SGC and certain breeds appeared predisposed. These data can provide a useful benchmark for glucocorticoid usage and highlight the benefits from ‘Big Data’ analyses.

scholarly journals Klinefelter syndrome in children and adolescents

2018 ◽  
Vol 64 (5) ◽  
pp. 321-328
Author(s):  
Darya A. Bespalyuk ◽  
Igor S. Chugunov
Keyword(s):  
Klinefelter Syndrome ◽  
Onset Time ◽  
Speech Disorders ◽  
Current Data ◽  
Testosterone Replacement Therapy ◽  
Male Hypogonadism ◽  
Main Diagnosis ◽  
Delayed Treatment ◽  
High Incidence ◽  
High Level

Klinefelter syndrome is a chromosomal pathology, which is the most common anomaly of sex chromosomes and the most common form of primary male hypogonadism. The presence of an extra X-chromosome in the karyotype causes infertility, azoospermia, small size of testicles, high level of gonadotropins and low level of testosterone, tallness and disproportionate physique, learning difficulties, and developmental speech disorders. Despite the high incidence of the syndrome in the population, only 25% of patients are aware of their disease during their lifetime. Late diagnosis and delayed treatment are often due to pronounced clinical polymorphism of the disease, different symptom onset time, as well as high incidence of associated conditions, so that these patients are followed by various specialists, but they are not aware of the main diagnosis. This review presents data on the history, etiology of the syndrome, clinical and laboratory features characteristic of children, adolescents, and adults. The most common associated diseases are listed and current data on their prevalence and the effect of testosterone replacement therapy on these conditions are provided.

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