Description

Technical Parameters

Introduction

pill

product-1400-1400

Products Description

### Systematic introduction of STADA brand Arimidex (Anastrozole) 1mg tablets

#### 1. Drug overview

**Arimidex (Anastrozole)** is a non-steroidal aromatase inhibitor (AI) produced by the international pharmaceutical company **STADA**, mainly used to treat hormone receptor-positive postmenopausal female breast cancer patients. As a representative drug of the third-generation aromatase inhibitor, its 1mg tablet has become one of the core drugs for endocrine therapy of breast cancer by effectively inhibiting estrogen synthesis and significantly reducing the proliferation activity of tumor cells. As a world-renowned generic drug company, STADA's Anastrozole tablets are widely used in many countries with high bioequivalence, strict quality control and cost advantages.

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#### 2. Pharmacological properties and mechanism of action

1. **Target**

Anastrozole competitively inhibits aromatase (CYP19A1) to block the conversion of androgens (such as androstenedione) to estrogens (estrone, estradiol). Its inhibition efficiency exceeds 96%, significantly reducing plasma estradiol levels to below the detection limit.

2. **Selective advantage**

As a non-steroidal drug, Anastrozole does not interfere with adrenal cortical hormone synthesis, avoids metabolic disorders of glucocorticoids or mineralocorticoids, and is safer than early steroid inhibitors (such as exemestane).

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#### 3. Physical and chemical properties

1. **Chemical structure**

- **Chemical name**: 2,2'-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenyl]bis(2-methylpropionitrile)

- **Molecular formula**: C17H19N5

- **Molecular weight**: 293.37 g/mol

- **CAS number**: 120511-73-1

2. **Physical and chemical parameters**

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

- **Solubility**: slightly soluble in water (about 0.5 mg/mL), easily soluble in organic solvents such as methanol and ethanol.

- **Stability**: stable at room temperature, may degrade under light or humid environment, and needs to be sealed and stored away from light.

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#### 4. Dosage form and appearance characteristics

1. **Tablet design**

- **Specification**: Each tablet contains 1 mg of Anastrozole, which is a film-coated tablet.

- **Color and marking**: The tablets produced by STADA are usually **white or light yellow round tablets**, with "AN1" or brand logo engraved on one side and smooth or divided lines on the other side for dosage division.

- **Coating ingredients**: Use inert materials such as hydroxypropyl methylcellulose (HPMC) to improve stability and swallowing palatability.

2. **Packaging specifications**

Commonly used are aluminum-plastic blister packaging, 14 or 28 tablets per box, with desiccant to ensure moisture-proof.

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#### 5. Indications and clinical applications

1. **Main indications**

- **Adjuvant treatment of early breast cancer**: used to prevent recurrence in postmenopausal women after surgery, the course of treatment is usually 5 years.

- **Treatment of advanced breast cancer**: used as a first-line drug for metastatic breast cancer that is positive for estrogen receptor (ER+) or progesterone receptor (PR+).

- **Neoadjuvant therapy**: combined with chemotherapy to reduce tumor volume and improve surgical success rate.

2. **Efficacy advantage**

- **Improved survival rate**: Compared with tamoxifen, Anastrozole significantly reduces the risk of recurrence by 40%.

- **Control of bone metastasis**: By inhibiting estrogen, it reduces the progression of osteolytic lesions.

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#### 6. Product advantages and core advantages

1. **High efficiency and selectivity**

- The inhibitory activity against aromatase is more than 100 times that of early drugs, and there is no risk of cross-reaction with steroid drugs.

2. **Good tolerability**

- The incidence of common side effects (such as hot flashes and joint pain) is lower than that of chemotherapy drugs, and patient compliance is high.

3. **Oral convenience**

- A 1mg dose once a day, no need to monitor blood drug concentration, suitable for long-term home treatment.

4. **Economical**

- As a generic drug brand, STADA's price is 30%-50% lower than that of the original drug, reducing the economic burden on patients.

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#### 7. Pharmacokinetic properties

1. **Absorption and distribution**

- **Bioavailability**: Rapid absorption after oral administration, reaching peak blood drug concentration (Cmax) in about 2 hours, and food does not affect absorption.

- **Protein binding rate**: About 40%, mainly bound to albumin.

2. **Metabolism and excretion**

- **Metabolic pathway**: Metabolized by liver CYP3A4 and N-dealkylation, no active metabolites.

- **Half-life**: About 50 hours, allowing once-daily administration.

- **Excretion**: 85% is excreted through feces, and 10% is excreted through urine.

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#### 8. Safety and side effects

1. **Common adverse reactions**

- **Hot flashes** (incidence is about 30%-40%), **Joint pain** (25%-30%), fatigue, headache.

- **Bone loss**: Long-term use may increase the risk of osteoporosis, and calcium and vitamin D supplementation are required.

2. **Serious but rare risks**

- **Cardiovascular events**: such as myocardial ischemia (<1%).

- **Elevated liver enzymes**: Liver function needs to be monitored regularly.

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#### 9. Drug interactions

1. **Estrogen drugs** (such as birth control pills) may antagonize the efficacy of Anastrozole and should be avoided in combination.

2. **CYP3A4 inducers** (such as rifampicin, phenytoin) may reduce its blood concentration and the dose needs to be adjusted.

3. **Tamoxifen**: Combined use may antagonize each other. Sequential treatment is recommended rather than simultaneous use.

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#### 10. Patient Guidelines

1. **Dosage and Usage**

- **Standard dose**: 1 tablet (1 mg) per day, orally at a fixed time, regardless of meals.

- **Missed dose treatment**: If you miss a dose, do not double the dose the next day.

2. **Contraindications**

- Premenopausal women, severe hepatic insufficiency (Child-Pugh C grade), and known drug allergies are contraindicated.

3. **Storage conditions**

- Store in a dark place below 30°C and keep the original packaging moisture-proof.

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#### 11. Market and brand information

1. **STADA company background**

Founded in 1895, STADA AG of Germany focuses on generic drugs and biosimilars. Its products cover 120 countries around the world and are known for its strict compliance with GMP standards and cost-effectiveness.

2. **Quality Certification**

Certified by multiple drug regulatory agencies such as the European Union EMA and the US FDA to ensure bioequivalence with the original drug (AstraZeneca Arimidex®).

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#### 12. Research progress and future directions

1. **Combination therapy exploration**

- Combined with CDK4/6 inhibitors (such as Palbociclib) to prolong the progression-free survival of advanced patients.

2. **Preventive application**

- Targeting high-risk groups with BRCA gene mutations, study its potential to prevent breast cancer.

3. **Development of new dosage forms**

- Transdermal patches or long-acting injections to reduce the frequency of oral administration.

#### Conclusion

Anastrozole 1mg tablets produced by STADA have become the cornerstone drug for endocrine therapy of breast cancer due to its efficient estrogen inhibition ability, good tolerability and economy. With the development of personalized medicine, its application prospects in combination therapy and prevention are broad. Patients need to take medication under the guidance of a doctor and regularly monitor bone density and blood lipid levels to achieve the best balance between efficacy and safety.