Estradiol dienanthate API Manufacturers

General Description:

Estradiol dienanthate, identified by CAS number 7732-97-0, is a notable compound with significant therapeutic applications. Estradiol Dienanthate is a pro-drug ester of , a naturally occurring hormone that circulates endogenously within the human body. Estradiol is the most potent form of all mammalian estrogenic steroids and acts as the major female sex hormone. As a pro-drug of estradiol, estradiol benzoate therefore has the same downstream effects within the body through binding to the Estrogen Receptor (ER) including ERα and ERβ subtypes, which are located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter systemic circulation and exert its estrogenic effects . Esterification of estradiol aims to improves absorption and bioavailability after oral administration (such as with Estradiol valerate) or to sustain release from depot intramuscular injections (such as with Estradiol Cypionate) through improved lipophilicity. Following absorption, the esters are cleaved, resulting in the release of endogenous estradiol, or 17β-estradiol. Ester pro-drugs of estradiol are therefore considered to be bioidentical forms of estrogen . Estradiol dienanthate is not currently available in any commercially available products in Canada or the US.

Indications:

This drug is primarily indicated for: Estradiol dienanthate is not currently available in any FDA or Health Canada approved products. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Estradiol dienanthate undergoes metabolic processing primarily in: Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Protein Binding:

Estradiol dienanthate exhibits a strong affinity for binding with plasma proteins: Estrogens circulate in the blood largely (>95%) bound to sex hormone binding globulin (SHBG) and to albumin. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Estradiol dienanthate from the body primarily occurs through: Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Pharmacodynamics:

Estradiol dienanthate exerts its therapeutic effects through: Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Estradiol dienanthate functions by: Estradiol enters target cells freely (e.g, female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Classification:

Estradiol dienanthate 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:

Estradiol dienanthate is categorized under the following therapeutic classes: BCRP/ABCG2 Inhibitors, Cytochrome P-450 CYP1A2 Inhibitors, Cytochrome P-450 CYP1A2 Inhibitors (strength unknown), Cytochrome P-450 CYP1A2 Inhibitors (weak), Cytochrome P-450 CYP1A2 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 Substrates, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (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, Estradiol Congeners, Estranes, Estrenes, Fused-Ring Compounds, Gonadal Hormones, Gonadal Steroid Hormones, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, OATP1B1/SLCO1B1 Inhibitors, OCT1 inhibitors, OCT2 Inhibitors, Organic Anion Transporting Polypeptide 2B1 Inhibitors, P-glycoprotein substrates, Steroids, UGT1A1 Substrates. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.