Altraz: Advanced Aromatase Inhibition for Estrogen-Sensitive Cancers
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Synonyms | |||
Altraz (anastrozole) is a potent, non-steroidal aromatase inhibitor indicated for the adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer. It is also approved for the first-line treatment of advanced or metastatic breast cancer in this patient population and for treatment following tamoxifen therapy. By selectively inhibiting the aromatase enzyme, Altraz significantly reduces estrogen biosynthesis, depriving hormone-dependent tumor cells of their primary growth stimulus. This targeted mechanism offers a sophisticated endocrine therapy option with a well-established efficacy and safety profile, making it a cornerstone in the management of estrogen-sensitive malignancies.
Features
- Active ingredient: Anastrozole 1 mg
- Pharmacological class: Non-steroidal aromatase inhibitor
- Presentation: Film-coated tablets
- Bioavailability: Approximately 80–85% following oral administration
- Half-life: 40–50 hours
- Metabolism: Hepatic (85%), primarily via N-dealkylation, hydroxylation, and glucuronidation
- Excretion: Primarily hepatic (85%), with renal excretion accounting for approximately 11%
- Protein binding: 40%
- Special packaging: Blister packs for stability and patient compliance
Benefits
- Superior Estrogen Suppression: Achieves >97% suppression of plasma estradiol levels within 24 hours, creating a hostile microenvironment for estrogen-dependent tumor growth.
- Proven Survival Benefit: Demonstrated significant improvement in disease-free survival and reduction in contralateral breast cancer incidence in large-scale clinical trials.
- Favorable Safety Profile: Non-steroidal structure avoids the androgen precursor effects associated with steroidal inhibitors, reducing certain androgenic side effects.
- Oral Administration Convenience: Once-daily dosing regimen supports treatment adherence and quality of life during extended therapy periods.
- Reduced Thrombotic Risk: Unlike tamoxifen, shows no associated increase in risk for venous thromboembolic events or endometrial cancer.
- Bone Density Monitoring Compatibility: Predictable endocrine effects allow for structured bone health management protocols during treatment.
Common use
Altraz is primarily prescribed for the adjuvant treatment of hormone receptor-positive early breast cancer in postmenopausal women. It is also indicated for the first-line treatment of locally advanced or metastatic hormone receptor-positive breast cancer in this population. Additionally, it is used sequentially after tamoxifen therapy in women who have received 2–3 years of tamoxifen and are switched to complete a total of 5 years of adjuvant endocrine therapy. Off-label uses may include neoadjuvant therapy for locally advanced breast cancer and treatment of estrogen-dependent conditions such as gynecomastia or precocious puberty in specific clinical scenarios, though these applications require careful specialist evaluation.
Dosage and direction
The recommended dosage of Altraz is one 1 mg tablet taken orally once daily, with or without food. Tablets should be swallowed whole with water and not crushed or chewed. For adjuvant treatment of early breast cancer, therapy should continue for 5 years, unless disease recurrence or unacceptable toxicity occurs earlier. For advanced breast cancer, treatment continues until tumor progression is documented. No dosage adjustment is necessary for elderly patients or those with mild to moderate hepatic impairment. For patients with severe hepatic impairment or creatinine clearance <20 mL/min, careful monitoring is recommended, though formal dosage adjustments have not been established. Treatment should be initiated and supervised by a physician experienced in anticancer therapy.
Precautions
Patients should undergo comprehensive baseline assessment including bone mineral density measurement before initiating therapy due to the accelerated bone loss associated with estrogen suppression. Regular monitoring of lipid profiles is recommended, particularly in patients with pre-existing dyslipidemia. Hepatic function should be assessed periodically, although anastrozole is not extensively hepatotoxic. Patients with pre-existing ischemic heart disease should be closely monitored for cardiovascular symptoms. Caution is advised when prescribing to patients with moderate to severe osteoporosis or those at high risk of fracture. Pre-menopausal women must not receive Altraz unless ovarian function has been permanently ablated. Patients should be advised that Altraz may impair driving ability or operation of machinery due to possible fatigue or dizziness.
Contraindications
Altraz is contraindicated in pre-menopausal women, as it will not suppress ovarian estrogen production and may lead to hormonal imbalance. It is contraindicated in patients with known hypersensitivity to anastrozole or any excipients in the formulation. Patients with severe hepatic impairment (Child-Pugh Class C) should not receive Altraz due to insufficient safety data. Concomitant use with estrogen-containing therapies is contraindicated as it would counteract the therapeutic effect. The medication is contraindicated in pregnancy (Pregnancy Category D) and breastfeeding, due to potential fetal harm and excretion in breast milk. Patients with unresolved deep vein thrombosis or pulmonary embolism should not initiate therapy until the condition is stabilized.
Possible side effect
The most frequently reported adverse reactions (≥10%) include hot flashes (35%), asthenia (16%), arthritis/arthralgia (11–25%), pain (11–17%), nausea (9–15%), headache (9–13%), and pharyngitis (12%). Less common but clinically significant effects include vaginal dryness (1–5%), mood disturbances (4–8%), carpal tunnel syndrome (2–5%), and elevated cholesterol (2–9%). Rare but serious adverse events (<1%) include ischemic cardiovascular events, osteoporosis with fractures, hepatic enzyme elevations, and hypersensitivity reactions including angioedema and urticaria. Most side effects are mild to moderate in severity and often diminish with continued therapy. Patients should report persistent joint pain, unusual fractures, or signs of hypercholesterolemia to their healthcare provider.
Drug interaction
Altraz is primarily metabolized by CYP3A4 and CYP3A5, with potential interactions with strong CYP3A4 inhibitors (ketoconazole, ritonavir) which may increase anastrozole concentrations. Concomitant use with tamoxifen should be avoided as it reduces anastrozole plasma concentrations by 27%. Estrogen-containing therapies (HRT, oral contraceptives) may diminish the therapeutic effect of Altraz. No clinically significant interactions have been observed with warfarin, cimetidine, or other commonly co-administered medications. Caution is advised with medications that affect bone metabolism (corticosteroids, anticonvulsants) or lipid profiles (statins, fibrates). Healthcare providers should review all concomitant medications, including over-the-counter products and herbal supplements.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed dose. Consistent daily administration is important for maintaining stable estrogen suppression. If multiple doses are missed, patients should contact their healthcare provider for guidance. The long half-life of anastrozole (40–50 hours) provides some buffer against temporary fluctuations in plasma concentrations, but adherence to the prescribed regimen is crucial for optimal therapeutic outcomes.
Overdose
No specific antidote for anastrozole overdose exists. Single doses up to 60 mg have been administered without severe adverse effects. Expected manifestations of significant overdose would likely include exaggerated pharmacological effects: severe estrogen suppression with potential for pronounced hot flashes, nausea, and dizziness. In case of suspected overdose, symptomatic and supportive care should be instituted. Gastric lavage may be considered if ingestion was recent. Vital signs should be monitored, and appropriate symptomatic treatment provided. Due to high protein binding, dialysis is unlikely to be effective. Medical toxicology consultation is recommended for significant overdoses.
Storage
Store at controlled room temperature (20–25°C or 68–77°F) with excursions permitted between 15–30°C (59–86°F). Protect from light and moisture. Keep in the original blister packaging until time of administration to maintain stability. Do not store in bathrooms or other areas with high humidity. Keep out of reach of children and pets. Do not use tablets that appear discolored, cracked, or otherwise damaged. Properly dispose of expired or unused medication through take-back programs or according to local regulations—do not flush down toilets or pour into drains.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Altraz is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Individual patient responses may vary, and treatment decisions should be based on comprehensive clinical evaluation. The prescribing physician should be consulted for specific dosage recommendations and management of adverse effects. Full prescribing information including boxed warnings should be reviewed before initiation of therapy. Patients should report any unexpected symptoms or side effects to their healthcare provider promptly.
Reviews
Clinical studies involving over 10,000 patients have established Altraz as a well-tolerated and effective endocrine therapy. The ATAC (Arimidex, Tamoxifen Alone or in Combination) trial, a landmark study with 9,366 participants, demonstrated superior disease-free survival with anastrozole compared to tamoxifen (HR 0.87, p=0.01) with a median follow-up of 100 months. The IBIS-II prevention trial showed a 53% reduction in invasive breast cancer incidence in high-risk postmenopausal women. Meta-analyses confirm consistent benefits across patient subgroups, particularly in women with strongly ER-positive disease. Real-world evidence supports the maintained efficacy and manageable toxicity profile observed in clinical trials, with particular appreciation for the reduced thromboembolic risk compared to tamoxifen-based regimens.