Description

Technical Parameters

Introduction

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product-1400-1400

Products Description

#### **1. Chemical properties and basic information**

1. **Chemical name and structure**

- **Generic name**: Oxymetholone

- **IUPAC name**: 17β-Hydroxy-2-(hydroxymethylene)-17α-methyl-5α-androstan-3-one

- **Molecular formula**: C₂₁H₃₂O₃

- **Molecular weight**: 332.48 g/mol

- **CAS number**: 434-07-1

2. **Chemical structure characteristics**

- A synthetic derivative based on testosterone with the following key modifications:

- **17α-Methyl**: Enhances oral bioavailability and prevents first-pass metabolism in the liver.

- **2-Hydroxymethylene**: Enhances protein anabolic activity and reduces androgenic side effects.

- **Stereochemistry**: 5α-reduced configuration, optimizes binding ability to androgen receptors.

3. **Physical properties**

- **Appearance**: White to off-white crystalline powder.

- **Solubility**: Slightly soluble in water (<0.1 mg/mL), easily soluble in organic solvents (such as ethanol, chloroform).

- **Stability**: Store away from light and at low temperature (2-8°C) to avoid oxidative degradation.

#### **2. Pharmacological effects and mechanisms**

1. **Target**

- **Androgen receptor (AR)**: Promotes muscle protein synthesis and erythropoiesis by activating AR.

- **Glucocorticoid receptor antagonism**: Inhibits the catabolic effect of cortisol and reduces muscle consumption.

2. **Core pharmacological effects**

- **Erythropoiesis**: Stimulates the kidneys to release erythropoietin (EPO) and increases hemoglobin concentration.

- **Nitrogen retention effect**: Increases the uptake of amino acids by muscle cells, accelerates tissue repair and muscle growth.

- **Bone metabolism regulation**: Enhances calcium deposition and improves osteoporosis (requires long-term high-dose use).

3. **Pharmacokinetics**

- **Oral absorption rate**: about 95%, reaching the peak blood drug level in 1-2 hours.

- **Half-life**: 8-9 hours, metabolized by the liver into active metabolites (such as 17-ketosteroids).

- **Excretion route**: mainly through the kidneys (60%), and a small amount is excreted through bile.

#### **3. Medical application and clinical value**

1. **Indications**

- **Aplastic anemia**: by stimulating bone marrow hematopoietic function, significantly improve the level of red blood cells and platelets (dose: 1-5 mg/kg/day).

- **Chemotherapy-related anemia**: used to correct anemia after chemotherapy in patients with leukemia and lymphoma.

- **Adjuvant treatment for osteoporosis**: limited to male patients, calcium and vitamin D must be combined.

2. **Efficacy advantage**

- **Rapid onset**: hemoglobin levels increase significantly within 2-4 weeks.

- **Low-dose high-efficiency**: Compared with other steroids, 50-150 mg/day can reach the therapeutic threshold.

3. **Combination therapy**

- **Combined with EPO**: Synergistically enhance erythropoiesis and reduce transfusion dependence.

- **Combined with immunosuppressants**: Used for severe aplastic anemia (such as combined with cyclosporine A).

#### **4. Non-medical applications and controversies**

1. **Sports and bodybuilding**

- **Muscle-building effect**: In the short term (4-6 weeks), lean body weight can be increased by 5-7 kg, but it is accompanied by water retention.

- **Abuse mode**: Often used as a "shock period" drug, the dose is as high as 100-150 mg/day, which can easily lead to liver toxicity.

2. **Side effects and risks**

- **Hepatotoxicity**: The 17α-methyl structure can cause elevated liver enzymes and cholestatic hepatitis (the incidence is about 15%).

- **Cardiovascular effects**: Increase LDL, decrease HDL, and increase the risk of atherosclerosis.

- **Endocrine disorders**: Inhibit endogenous testosterone secretion, and PCT (Post Cycle Therapy) is required.

#### **5. API production and market analysis**

1. **Global supply chain**

- **Major producing countries**: China (accounting for 60% of global production capacity), India, and Eastern Europe.

- **Quality control standards**: Must comply with USP/EP/ChP standards, purity ≥ 98% (HPLC detection).

2. **Synthesis process**

- **Key steps**:

1. Using dehydroepiandrosterone (DHEA) as the starting material, introduce 17α-methyl through Mitsunobu reaction.

2. Add 2-hydroxymethylene groups through Aldol condensation.

- **Environmental challenges**: It is necessary to deal with heavy metal catalyst residues (such as mercury) and promote the development of green chemical processes.

3. **Price and market dynamics**

- **Price of API**: about $2000-$5000/kg (depending on purity and purchase volume fluctuations).

- **Demand drivers**: Hidden demand in emerging market generic drug production and non-regulatory fitness markets.

#### **6. Legal supervision and compliance requirements**

1. **International control classification**

- **United States**: DEA Schedule III controlled drugs (special prescription required).

- **China**: listed in the "Regulations on the Administration of Narcotic Drugs and Psychotropic Drugs", unauthorized production is strictly prohibited.

- **WADA list**: The World Anti-Doping Agency explicitly prohibits it, and the threshold for urine testing in competitions is ≤10 ng/mL.

2. **Compliance production requirements**

- **GMP certification**: API production must comply with FDA/EMA cGMP standards.

- **Export control**: An import license from the drug regulatory agency of the importing country is required.

#### **7. Future research and development of alternatives**

1. **Structural optimization direction**

- **Reducing liver toxicity**: Developing non-17α-alkylated analogs (such as selective androgen receptor modulators).

- **Improving selectivity**: Enhancing targeting to muscle tissue through computer-aided design (CADD).

2. **Clinical research trends**

- **Applications in rare diseases**: Exploring efficacy in myelofibrosis and sickle cell anemia.

- **Long-acting preparation development**: Such as transdermal patches or sustained-release microspheres, reducing the frequency of daily medication.

#### **8. Conclusion**

Anadrol (Oxymetholone), as a highly effective anabolic steroid, has demonstrated irreplaceable clinical value in the medical field, but its abuse risk and side effects also need to be strictly controlled. Technological innovation and compliance management of API production are the key to balancing its pros and cons. In the future, with the development of precision medicine, safer derivatives or alternatives are expected to gradually replace traditional steroid drugs.