Armidyn (Anastrozole)

About the Product

Armidyn is a research compound from Driada Medical, containing Anastrozole. Anastrozole is a potent, non-steroidal, and highly selective aromatase inhibitor . Its chemical formula is C₁₇H₁₉N₅, with a molecular weight of 293.4 g/mol and a CAS number of 120511-73-1 .

The compound functions by inhibiting the aromatase enzyme (cytochrome P450 19A1), which is responsible for the conversion of androgens (such as androstenedione and testosterone) to estrogens (estrone and estradiol) . This mechanism makes it a valuable research tool for studying estrogen-dependent pathways.

• Product Name: Armidyn (Anastrozole)

• Brand: Driada Medical

• Form: Solution for research applications

• CAS: 120511-73-1

• For Research Use Only.

Research Applications & Mechanism of Action

• Potent Aromatase Inhibition: Anastrozole is a benchmark compound for studying estrogen biosynthesis due to its high potency and selectivity . It acts as a competitive inhibitor of the aromatase enzyme, with an IC₅₀ of approximately 9.4–15 nM in vitro . This high affinity allows researchers to effectively suppress estrogen production in experimental models.

• Estrogen Deprivation Research: As a tool to deplete estrogens, anastrozole is widely used to study hormone-dependent cellular processes, including gene regulation, cell proliferation, and apoptosis in various tissue types .

• Receptor Biology & Endocrine Research: Anastrozole's ability to lower estradiol without affecting adrenal corticosteroid synthesis makes it valuable for isolating the effects of estrogen from other endocrine pathways .

• Drug Metabolism & CYP450 Studies: Anastrozole is known to inhibit certain cytochrome P450 enzymes (CYP1A2, CYP2C9, CYP3A) at high concentrations, making it relevant for drug-drug interaction research . These interactions occur at concentrations approximately 30 times higher than therapeutic levels, which is an important consideration for in vitro studies .

• Pharmacogenomics Research: Genomic studies have identified genetic variants (such as SNPs in the CSMD1 gene) that may influence individual responses to anastrozole . This makes it a key compound for investigating the genetic basis of treatment response variability.

• Cancer Research: Anastrozole is a principal compound for studying hormone-sensitive cancers, particularly ER-positive breast cancer models, including research on mechanisms of resistance .

Research & Scientific Background

• Mechanism: Anastrozole's triazole ring binds reversibly to the heme iron in the aromatase enzyme's catalytic site, blocking the enzyme from converting androgens to estrogens . In postmenopausal research models, it reduces serum estradiol by approximately 70% within 24 hours and up to 80% after 14 days of dosing .

• Selectivity: Anastrozole is highly selective for aromatase and does not affect the formation of adrenal corticosteroids or aldosterone . It also does not possess direct progestogenic, androgenic, or estrogenic activity .

• Metabolism: Anastrozole is primarily metabolized in the liver via N-dealkylation, hydroxylation, and glucuronidation by cytochrome P450 enzymes . Its major metabolite, triazole, lacks pharmacological activity . Approximately 85% of the compound is eliminated via hepatic metabolism, with about 10% excreted renally .

• Pharmacokinetics: Anastrozole is rapidly absorbed, reaching peak plasma concentrations within 2 hours . It has a terminal elimination half-life of approximately 50 hours (range 30-60 h) . Steady-state plasma levels are achieved after approximately 7 days of daily dosing and are 3- to 4-fold higher than after a single dose . The compound is approximately 40% bound to plasma proteins .

• Genetic Variability: Research has shown that inter-individual variability in response to anastrozole may be linked to genetic factors. A study identified that a SNP in the CSMD1 gene was associated with differential patient outcomes and that CSMD1 regulates CYP19 expression in a drug-dependent fashion, specifically affecting anastrozole sensitivity . Additionally, polymorphisms in genes encoding UGT2B17 have been shown to influence the metabolism and detection of exogenous hormones like testosterone cypionate, highlighting the growing importance of pharmacogenomics in endocrine research. This suggests that genetic differences in drug-metabolizing enzymes and regulatory pathways may impact compound metabolism and response.

• Dose-Response Studies: In clinical research, doses of anastrozole from 0.5 mg to 10 mg have been evaluated for estrogen suppression . Recent studies indicate that approximately 30% of individuals on standard 1 mg/day dosing may achieve inadequate estrogen suppression, and dose escalation to 10 mg/day can help achieve adequate suppression in about 76% of those cases . This highlights the importance of dosing optimization in research models.