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- 2-Methoxyestradiol
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2-Methoxyestradiol | CAS No: 362-07-2 | GMP-certified suppliers
A medication that targets breast cancer and inflammatory diseases like rheumatoid arthritis by inhibiting tumor growth and modulating cellular proliferation.
Therapeutic categories
Primary indications
- For the treatment of breast cancer and inflammatory diseases such as rheumatoid arthritis
Product Snapshot
- 2-Methoxyestradiol is an oral small molecule formulation
- It is primarily developed for oncological use in breast cancer and for inflammatory conditions like rheumatoid arthritis
- The compound is currently in investigational status and not approved by major regulatory agencies
Clinical Overview
Pharmacodynamically, 2-methoxyestradiol acts predominantly as an angiogenesis inhibitor, disrupting the formation of new blood vessels essential for tumor growth and survival. Additionally, it exhibits vasodilatory properties. Mechanistically, 2ME2 targets both tumor cells and their supporting vasculature, interfering with cellular proliferation and survival pathways. It is notable that, despite being a metabolite of estradiol, 2-methoxyestradiol lacks significant estrogenic activity, distinguishing it from other steroid hormones in this class.
The compound is classified within several pharmacological categories including antimitotic agents, antineoplastic agents, tubulin modulators, and gonadal steroid hormone derivatives. Its mode of action involves modulation of microtubule dynamics, thereby impairing mitosis and inducing tumor cell cytotoxicity.
Pharmacokinetic data for 2-methoxyestradiol, including absorption, distribution, metabolism, and excretion parameters, remain limited given its investigational status. However, its endogenous origin as an estrogen metabolite suggests metabolic pathways involving hepatic biotransformation and renal excretion.
From a safety and toxicity standpoint, clinical experience is predominantly confined to early phase trials. No undesired estrogenic effects have been reported, but comprehensive safety profiles await further clinical evaluation.
Currently, 2-methoxyestradiol is not commercially approved and is utilized primarily within clinical research frameworks. Notable investigational formulations have been explored for intravenous and oral administration.
When sourcing 2-methoxyestradiol API, considerations should include verification of purity, stereochemical integrity, and absence of contaminants. Given its investigational status, procurement must comply with regulatory guidelines governing clinical trial materials and maintain stringent quality control to ensure consistency and reproducibility in pharmaceutical development.
Identification & chemistry
| Generic name | 2-Methoxyestradiol |
|---|---|
| Molecule type | Small molecule |
| CAS | 362-07-2 |
| UNII | 6I2QW73SR5 |
| DrugBank ID | DB02342 |
Pharmacology
| Summary | 2-Methoxyestradiol is an angiogenesis inhibitor that targets tumor cells and their blood supply by modulating hypoxia-inducible factor 1-alpha and multiple cytochrome P450 enzymes. It also exhibits vasodilatory effects and lacks estrogenic activity despite being an estrogen metabolite. The compound is investigated for therapeutic applications in breast cancer and inflammatory conditions such as rheumatoid arthritis. |
|---|---|
| Mechanism of action | 2-Methoxyestradiol is an angiogenesis inhibitor, and has been shown to attack both tumor cells and their blood supply in preclinical testing. 2-methoxyestradiol is a naturally occurring estrogen metabolite but has no undesired estrogenic activity. |
| Pharmacodynamics | 2-Methoxyestradiol belongs to the family of drugs called angiogenesis inhibitors. It also acts as a vasodilator. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Catechol O-methyltransferase | Humans | |
| Cytochrome P450 1A1 | Humans | |
| Cytochrome P450 1B1 | Humans |
ADME / PK
| Protein binding | 2ME2 was found to bind in decreasing order to plasma>albumin>alpha1-acid glycoprotein>sex-hormone-binding globulin. Plasma concentration-time profiles of total 2ME2 and unbound 2ME2 concentrations in a patient with cancer receiving 2ME2 as a single oral dose were parallel to each other. Thus, indicating that plasma protein binding is not an important consideration in pharmacokinetic monitoring of 2ME2. |
|---|---|
| Metabolism | In vivo metabolism, assessed using 24-h collections of urine from cancer patients treated with 2ME2 revealed that <0.01% of the total administered dose of 2ME2 is excreted unchanged in urine and about 1% excreted as glucuronides. Collectively, this suggests that glucuronidation and subsequent urinary excretion are elimination pathways for 2ME2. |
Formulation & handling
- 2-Methoxyestradiol is a small molecule solid with low water solubility, favoring non-aqueous formulation approaches.
- Due to its lipophilicity (LogP 3.59), formulation strategies should consider solubility enhancement to improve bioavailability for oral administration.
- Stability considerations include minimizing exposure to moisture and light to preserve compound integrity during handling and storage.
Regulatory status
2-Methoxyestradiol is a type of Antineoplastics
Antineoplastics are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of cancer. These powerful substances inhibit or destroy the growth of cancer cells, thus impeding the progression of malignancies.
Antineoplastics exert their therapeutic effects through various mechanisms. Some APIs interfere with DNA replication, inhibiting the division and proliferation of cancer cells. Others target specific proteins or enzymes involved in tumor growth, effectively blocking their function. Additionally, certain antineoplastic agents induce programmed cell death, known as apoptosis, in cancer cells.
These APIs find application in a wide range of cancer treatments, including chemotherapy, targeted therapy, immunotherapy, and hormone therapy. They are often administered in combination with other drugs to optimize therapeutic outcomes and minimize drug resistance.
Antineoplastics are typically synthesized through complex chemical processes, ensuring high purity and potency. Stringent quality control measures are implemented throughout manufacturing to meet regulatory standards and ensure patient safety.
Although antineoplastics offer significant benefits in treating cancer, they can also cause adverse effects due to their cytotoxic nature. Common side effects include bone marrow suppression, gastrointestinal disturbances, hair loss, and immune system suppression. Close monitoring and supportive care are essential to manage these side effects effectively.
In conclusion, antineoplastics are a vital category of pharmaceutical APIs used in the treatment of cancer. Through their diverse mechanisms of action, these compounds play a critical role in combating malignancies and improving patient outcomes.
