Lenor 2.5 Mg (Letrozole) Tablets

Introduction

Lenor 2.5 mg (Letrozole) represents a significant advancement in hormonal therapy for postmenopausal women with breast cancer. As a potent and highly specific nonsteroidal aromatase inhibitor, Lenor effectively reduces estrogen production in peripheral tissues and tumor sites, depriving estrogen-dependent breast cancer cells of their primary growth stimulus. This targeted approach to breast cancer treatment offers improved outcomes with manageable side effects, making it a cornerstone therapy in modern oncology protocols for hormone receptor-positive breast cancer.

Therapeutic Applications

Lenor 2.5 mg demonstrates remarkable efficacy across various stages of breast cancer treatment:

Early Stage Breast Cancer

Primary Adjuvant Therapy: First-line hormonal treatment for postmenopausal women with hormone receptor-positive early breast cancer
Extended Adjuvant Therapy: Continued treatment for women who have completed 5 years of tamoxifen therapy, reducing recurrence risk
Pre-Operative (Neoadjuvant) Therapy: Enables breast-conserving surgery in women initially considered unsuitable candidates

Advanced Breast Cancer

First-Line Treatment: For postmenopausal women with hormone-dependent advanced breast cancer
Second-Line Treatment: Effective option for women who have progressed after prior antiestrogen therapy (such as tamoxifen)
Post-Artificial Menopause: Suitable for women with artificially induced postmenopausal status

Mechanism of Action

Lenor works through a precise biological mechanism to combat estrogen-dependent breast cancer:

Aromatase Enzyme Inhibition

Competitive Binding: Letrozole binds to the haem of cytochrome P450 in the aromatase enzyme
Estrogen Suppression: This binding prevents conversion of androgens to estrogens
Rapid Response: Achieves 75-95% suppression of estrogen levels within 48-78 hours
Selective Action: Blocks only estrogen production without affecting other steroid hormones

Tissue-Specific Effects

Peripheral Tissues: Blocks conversion of androgens to estrogens in fat, muscle, and breast tissue
Tumor Environment: Directly reduces estrogen availability in breast cancer tissue
Minimal Impact on Adrenal Function: No significant impairment of adrenal steroidogenesis
Androgen Preservation: Does not lead to accumulation of androgenic precursors

Pharmacokinetic Profile

Lenor exhibits favorable pharmacokinetic properties that contribute to its clinical efficacy:

Absorption and Distribution

Complete Bioavailability: Nearly 100% absorption from the gastrointestinal tract
Food Independence: Minor effect of food on absorption rate, not clinically significant
Flexible Administration: Can be taken with or without food
Plasma Protein Binding: Approximately 60% bound, primarily to albumin (55%)
Tissue Distribution: Concentrates in erythrocytes at about 80% of plasma levels

Metabolism and Elimination

Metabolic Pathway: Primarily converted to inactive carbinol metabolite
Enzyme Systems: Metabolized by cytochrome P450 isoenzymes 3A4 and 2A6
Half-Life: Approximately 2 days terminal elimination half-life
Steady State: Achieved within 2-6 weeks of daily administration
Clearance Pattern: Relatively slow compared to hepatic blood flow

Dosage Guidelines

Lenor features a simple, once-daily dosing regimen appropriate for various treatment scenarios:

Standard Dosing

Recommended Dose: 2.5mg once daily
Administration: Oral tablet, can be taken regardless of food intake
Duration:
- Adjuvant/Extended Adjuvant Setting: Continue for 5 years or until tumor relapse
- Metastatic Disease: Continue until disease progression is evident

Special Population Considerations

Elderly Patients: No dose adjustment necessary
Renal Impairment: No dose adjustment required, even with creatinine clearance as low as 10 mL/min
Hepatic Impairment:
- Mild to Moderate: No dose adjustment required
- Severe Impairment (Child-Pugh C): Use with caution and close monitoring

Clinical Considerations

Important factors for healthcare providers when prescribing Lenor:

Drug Interactions

Minimal Drug Interaction Profile: Limited clinically significant interactions
Cimetidine: Co-administration does not result in clinically significant interactions despite CYP450 inhibition
Warfarin: No significant interaction observed with concomitant use
Dialysis Compatibility: Can be removed by dialysis if necessary due to weak plasma protein binding

Contraindications

Lenor should not be administered in cases of:

Known hypersensitivity to letrozole or other aromatase inhibitors
Pregnancy or lactation
Pre-menopausal women
Severe hepatic dysfunction

Special Monitoring Requirements

Bone Mineral Density: Regular monitoring recommended due to increased risk of osteoporosis
Cholesterol Levels: Periodic lipid profile assessment
Liver Function: Baseline and periodic monitoring in patients with hepatic impairment
Cardiovascular Status: Regular blood pressure checks and assessment for edema

Managing Side Effects

Understanding and addressing potential adverse effects improves treatment adherence:

Common Side Effects

Vasomotor Symptoms: Hot flashes and increased sweating
Musculoskeletal Effects: Arthralgia (joint pain) and myalgia (muscle pain)
Bone Health Concerns: Risk of osteoporosis and potential for fractures
Metabolic Changes: Hypercholesterolemia and weight changes
Gastrointestinal Effects: Nausea, vomiting, indigestion, constipation or diarrhea
General Symptoms: Fatigue, headache, dizziness

Management Strategies

Bone Health: Calcium and vitamin D supplementation; consider bisphosphonates
Vasomotor Symptoms: Lifestyle modifications and non-hormonal interventions
Joint/Muscle Pain: Appropriate pain management and physical therapy
Gastrointestinal Symptoms: Dietary modifications and supportive medications
Fatigue Management: Activity pacing and energy conservation techniques

Special Population Considerations

Attention to specific patient groups enhances safe and effective use:

Postmenopausal Status Confirmation

Ensure true postmenopausal status before initiating therapy
Consider alternative hormonal agents for pre-menopausal women

Hepatic Function

Caution in moderate hepatic dysfunction
Careful monitoring in impaired hepatic function
Not recommended in severe hepatic impairment

Cognitive Function

Advise patients about potential effects on mental alertness
Caution regarding driving or operating machinery if experiencing fatigue or dizziness

Quality Assurance

Lenor 2.5 mg tablets are manufactured by Eskayef Pharmaceuticals Ltd., a leading pharmaceutical company with over three decades of excellence in medication production. Each tablet undergoes rigorous quality control procedures to ensure potency, purity, and consistency for optimal therapeutic outcomes.

Storage Recommendations

To maintain product integrity:

Store below 30°C
Protect from light and moisture
Keep out of reach of children

Conclusion

Lenor 2.5 mg (Letrozole) represents a cornerstone in hormone-dependent breast cancer therapy, offering postmenopausal women an effective treatment option with a favorable safety profile. Through its precise inhibition of aromatase, Lenor provides targeted suppression of estrogen biosynthesis, effectively depriving estrogen-sensitive tumor cells of their growth stimulus. Available through Orio Pharma with worldwide delivery within 3-7 working days, Lenor exemplifies our commitment to providing high-quality oncology medications to improve outcomes for breast cancer patients globally.