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General Description:

Testosterone enanthate, identified by CAS number 315-37-7, is a notable compound with significant therapeutic applications. Testosterone enanthate is an esterified variant of testosterone that comes as an injectable compound with a slow-release rate. This slow release is achieved by the presence of the enanthate ester functional group attached to the testosterone molecule. This testosterone derivative was first approved on December 24, 1953. In 2017, about 6.5 million retail prescriptions for testosterone therapy were filled . The majority of the prescriptions written were for injectable (66%) and topical (32%) testosterone products. As recent as 1 October 2018, the US FDA approved Antares Pharma Inc.'s Xyosted - a subcutaneous testosterone enanthate product for once-weekly, at-home self-administration with an easy-to-use, single dose, disposable autoinjector . As the first subcutaneous autoinjector product designed for testosterone replacement therapy, this innovative formulation removes transfer concerns commonly associated with testosterone gels and potentially reduces the need for in-office/in-clinic injection procedures that may inconvenience patients with frequent visits to the clinic .

Indications:

This drug is primarily indicated for: Testosterone enanthate in males is indicated as a replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone. Some of the treated conditions are 1) primary hypogonadism, defined as testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome or orchidectomy; 2) hypogonadotropic hypogonadism due to an idiopathic gonadotropin or luteinizing hormone-releasing hormone deficiency or due to a pituitary-hypothalamic injury from tumors, trauma or radiation, in this case it is important to accompany the treatment with adrenal cortical and thyroid hormone replacement therapy; 3) to stimulate puberty in patients with delayed puberty not secondary to a pathological disorder. If the conditions 1 and 2 occur prior to puberty, the androgen replacement therapy will be needed during adolescent years for the development of secondary sexual characteristics and prolonged androgen treatment might be needed it to maintain sexual characteristics after puberty. In females, testosterone enanthate is indicated to be used secondarily in presence of advanced inoperable metastatic mammary cancer in women who are from one to five years postmenopausal. It has also been used in premenopausal women with breast cancer who have benefited from oophorectomy and are considered to have a hormone-responsive tumor. Testosterone enanthate injections that are currently formulated for subcutaneous use are specifically indicated only for primary hypogonadism and hypogonadotropic hypogonadism . The use of such formulations is limited because the safety and efficacy of these subcutaneous products in adult males with late-onset hypogonadism and males less than 18 years old have not yet been established . Moreover, subcutaneously administered testosterone enanthate is indicated only for the treatment of men with hypogonadal conditions associated with structural or genetic etiologies, considering the medication could cause blood pressure increases that can raise the risk of major adverse cardiovascular events like non-fatal myocardial infarction, non-fatal stroke, and cardiovascular death . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Testosterone enanthate undergoes metabolic processing primarily in: To start its activity, testosterone enanthate has to be processed by enzymes in the bloodstream. These enzymes will catalyze the molecule at the ester location of the moiety. Once processed in this manner, the testosterone enanthate molecule is metabolized to various 17-keto steroids through two different pathways. Subsequently, the major active metabolites are estradiol and DHTd. Testosterone is metabolized to DHT by steroid 5α-reductase in skin, liver and urogenital tract. In reproductive tissues DHT is further metabolized to androstanediol. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Testosterone enanthate are crucial for its therapeutic efficacy: The pharmacokinetic profile of testosterone enanthate was studied in a regime of multiple dosing and the testosterone level was reported to present a Cmax above 1200 ng/dl after 24 hours of the last dose. The concentration decreased sequentially until it reached 600 ng/dl after one week. The pharmacokinetic profile of testosterone enanthate presented differences depending on the administered dose in which the tmax was shifted to a range of 36-48 hours. The plasma testosterone level plateaued below the therapeutic range after 3-4 weeks. This reports showed that the different formulation of testosterone enanthate and testosterone cypionate generates a different profile and thus, they are not therapeutically equivalent. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Testosterone enanthate is an important consideration for its dosing schedule: Testosterone enanthate presents a long half-life in the range of 7-9 days. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Testosterone enanthate exhibits a strong affinity for binding with plasma proteins: Circulating testosterone is primarily bound in serum to sex hormone-binding globulin (SHBG) and albumin. Approximately 98% of testosterone in plasma is bound to SHBG while 2% remains unbound (i.e. free). This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Testosterone enanthate from the body primarily occurs through: About 90% of a dose of testosterone given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form. The inactivation of testosterone occurs primarily in the liver. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Testosterone enanthate is distributed throughout the body with a volume of distribution of: The volume of distribution following intravenous administration of testosterone is of approximately 1 L/kg. This metric indicates how extensively the drug permeates into body tissues.

Pharmacodynamics:

Testosterone enanthate exerts its therapeutic effects through: Administration of ester derivatives of testosterone as testosterone enanthate generates an increase in serum testosterone to levels reaching 400% from the baseline within 24 hours of administration. These androgen levels remain elevated for 3-5 days after initial administration. Continuous administration of testosterone enanthate shows a significant suppression of dihydrotestosterone, serum PSA, HDL and FSH, as well as a slight increase in serum estradiol. The levels of dihydrotestosterone and FSH can remain suppressed even 14 days after treatment termination. There are no changes in mood and sexual activity by the presence of testosterone enanthate. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Testosterone enanthate functions by: The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing androgen effects. Such activities are useful as endogenous androgens like testosterone and dihydrotestosterone are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics . These effects include the growth and maturation of the prostate, seminal vesicles, penis, and scrotum; the development of male hair distribution, such as facial, pubic, chest, and axillary hair; laryngeal enlargement, vocal cord thickening, and alterations in body musculature and fat distribution . Male hypogonadism, a clinical syndrome resulting from insufficient secretion of testosterone, has two main etiologies . Primary hypogonadism is caused by defects of the gonads, such as Klinefelter’s syndrome or Leydig cell aplasia, whereas secondary hypogonadism is the failure of the hypothalamus (or pituitary) to produce sufficient gonadotropins (FSH, LH) . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Testosterone enanthate belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group, classified under the direct parent group Steroid esters. This compound is a part of the Organic compounds, falling under the Lipids and lipid-like molecules superclass, and categorized within the Steroids and steroid derivatives class, specifically within the Steroid esters subclass.

Categories:

Testosterone enanthate is categorized under the following therapeutic classes: Adrenal Cortex Hormones, Androgens, Androstanes, Androstenes, Androstenols, BCRP/ABCG2 Substrates, Contraceptive Agents, Male, Cytochrome P-450 CYP2B6 Substrates, Cytochrome P-450 CYP2C19 Substrates, Cytochrome P-450 CYP2C8 Substrates, Cytochrome P-450 CYP2C9 Substrates, Cytochrome P-450 CYP3A Inducers, Cytochrome P-450 CYP3A Inhibitors, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (strength unknown), Cytochrome P-450 CYP3A4 Inhibitors, Cytochrome P-450 CYP3A4 Inhibitors (strength unknown), Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 CYP3A5 Substrates, Cytochrome P-450 CYP3A7 Substrates, Cytochrome P-450 Enzyme Inducers, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Substrates, Drugs that are Mainly Renally Excreted, Fused-Ring Compounds, Gonadal Hormones, Gonadal Steroid Hormones, Hormonal Contraceptives for Systemic Use, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, OAT3/SLC22A8 Inducers, P-glycoprotein inhibitors, Steroids, Testosterone and derivatives, Testosterone Congeners, Thyroxine-binding globulin inhibitors. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Testosterone enanthate include:

• Water Solubility: Insoluble
• Melting Point: 34-39ºC
• logP: 3.58