Femara: Advanced Aromatase Inhibition for Hormone-Sensitive Breast Cancer
| Product dosage: 2.5mg | |||
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Synonyms | |||
Femara (letrozole) is a potent, third-generation nonsteroidal aromatase inhibitor indicated for the adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer. It is also approved for the extended adjuvant treatment of early breast cancer following standard tamoxifen therapy, as well as for the first-line treatment of advanced or metastatic breast cancer in postmenopausal women. By selectively inhibiting the aromatase enzyme, Femara significantly reduces estrogen production, depriving hormone-sensitive tumor cells of their primary growth stimulus. Its targeted mechanism offers a sophisticated endocrine therapy option with a well-established efficacy and safety profile in clinical oncology.
Features
- Contains letrozole 2.5 mg per tablet
- Nonsteroidal aromatase inhibitor class
- High specificity for cytochrome P450 aromatase enzyme
- Oral administration with once-daily dosing
- Bioavailability of 99.9% with low protein binding
- Mean elimination half-life of approximately 2 days
- Metabolized primarily via CYP3A4 and CYP2A6 pathways
- Excreted mainly as inactive glucuronide metabolites via urine
Benefits
- Significantly reduces the risk of cancer recurrence in hormone receptor-positive early breast cancer
- Demonstrates superior efficacy compared to tamoxifen in first-line treatment of advanced disease
- Improves disease-free survival rates in extended adjuvant therapy settings
- Offers convenient oral administration without requirement for injection or hospitalization
- Provides predictable pharmacokinetics with minimal food interaction
- Generally well-tolerated with manageable side effect profile in most patients
Common use
Femara is primarily prescribed for the adjuvant treatment of hormone receptor-positive early breast cancer in postmenopausal women. It is also indicated for extended adjuvant treatment following completion of standard tamoxifen therapy, typically administered for 5 years. In advanced or metastatic breast cancer settings, Femara serves as first-line endocrine therapy. Off-label uses include ovulation induction in fertility treatments, though this application requires careful specialist supervision due to different dosing regimens and monitoring requirements.
Dosage and direction
The recommended dosage of Femara is 2.5 mg administered orally once daily, with or without food. Tablets should be swallowed whole with water. For adjuvant treatment of early breast cancer, treatment duration is typically 5 years. For extended adjuvant treatment following tamoxifen therapy, treatment duration is generally 5 additional years. In advanced breast cancer, treatment continues until tumor progression is documented. Dosage adjustment is not typically required for elderly patients, but careful monitoring is advised in patients with severe hepatic impairment.
Precautions
Patients should undergo comprehensive baseline assessment including bone mineral density evaluation due to Femara’s potential to accelerate bone loss. Regular monitoring of lipid profiles is recommended as letrozole may increase cholesterol levels. Caution is advised in patients with pre-existing hepatic impairment, though no dosage adjustment is necessary for mild to moderate impairment. Patients should be advised about potential dizziness and cautioned against driving or operating machinery until they know how Femara affects them. Vitamin D and calcium supplementation is generally recommended to mitigate bone density effects.
Contraindications
Femara is contraindicated in premenopausal women, as it is ineffective without chemical suppression of ovarian function. It must not be used during pregnancy (Pregnancy Category D) or breastfeeding due to potential fetal harm. Additional contraindications include hypersensitivity to letrozole or any component of the formulation, and co-administration with estrogen-containing therapies as these may diminish Femara’s therapeutic effect. The medication is not indicated for use in pediatric populations.
Possible side effects
The most frequently reported adverse reactions include hot flashes (27-33%), arthralgia (21-25%), fatigue (13-16%), and increased sweating (11-14%). Musculoskeletal events such as arthritis, osteoporosis, and fractures occur in approximately 10-15% of patients. Other common side effects comprise nausea (9-12%), headache (9-10%), and peripheral edema (5-7%). Less frequent but serious adverse reactions may include cardiovascular events (myocardial infarction, angina), thromboembolic events, and cerebrovascular accidents. Elevated cholesterol levels are observed in approximately 16-20% of patients.
Drug interaction
Femara demonstrates minimal potential for clinically significant drug interactions due to its low protein binding and extensive metabolism. However, potent CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) may decrease letrozole concentrations, potentially reducing efficacy. Conversely, strong CYP3A4 inhibitors (ketoconazole, ritonavir) may increase letrozole exposure. Tamoxifen co-administration reduces letrozole plasma concentrations by approximately 38% and is not recommended. No significant interactions have been observed with warfarin, though monitoring of INR is prudent during concomitant therapy.
Missed dose
If a dose is missed, patients should take it as soon as remembered unless it is nearly time for the next scheduled dose. In such cases, the missed dose should be skipped and the regular dosing schedule resumed. Patients should never take a double dose to make up for a missed dose. Maintaining consistent dosing times is recommended to ensure stable drug concentrations, though Femara’s long half-life provides some forgiveness for occasional dosing irregularities.
Overdose
Limited data exists regarding Femara overdose. Single doses up to 62.5 mg have been administered without severe adverse effects. Expected manifestations of overdose would likely include exaggerated pharmacological effects such as severe hot flashes, nausea, and dizziness. No specific antidote exists; treatment should consist of supportive measures and symptomatic management. Gastric lavage may be considered if ingestion occurred within a short timeframe. Hemodialysis is unlikely to be beneficial due to Femara’s high protein binding and extensive tissue distribution.
Storage
Store Femara tablets at room temperature (15-30°C or 59-86°F) in their original container. Protect from light and moisture. Keep the bottle tightly closed and out of reach of children. Do not use beyond the expiration date printed on the packaging. Proper disposal of unused medication through take-back programs is recommended to prevent accidental ingestion or environmental contamination.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient characteristics and comprehensive clinical assessment. Patients should consult their oncologist or healthcare provider for personalized medical advice and report any adverse reactions promptly. The prescribing information provided here may not include all possible uses, directions, precautions, or interactions.
Reviews
Clinical trials demonstrate Femara’s consistent efficacy across multiple breast cancer settings. The BIG 1-98 trial, involving 8,010 postmenopausal women with hormone receptor-positive early breast cancer, showed significant improvement in disease-free survival compared to tamoxifen. The MA-17 trial established Femara’s benefit in extended adjuvant therapy, reducing recurrence risk by 42% compared to placebo. Real-world evidence supports these findings, with oncologists reporting favorable outcomes in appropriately selected patients. Common practitioner observations include generally manageable side effects and good long-term adherence rates due to once-daily oral administration.