Anastrozole 1 mg Tablet, Coated, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Aromatase Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Anastrozole is used with other treatments, such as surgery or radiation, to treat early breast cancer in women who have experienced menopause (change of life; end of monthly menstrual periods). This medication is also used in women, who have experienced menopause, as a first treatment of breast cancer that has spread within the breast or to other areas of the body. This medication is also used to treat breast cancer in women whose breast cancer has worsened after taking tamoxifen (Nolvadex). Anastrozole is in a class of medications called nonsteroidal aromatase inhibitors. It works by decreasi...
Read the full MedlinePlus article ↗- Great question. After menopause, your body still makes small amounts of estrogen through an enzyme called aromatase — and many breast cancers use that estrogen as fuel to grow. Ana...
- What exactly is anastrozole doing in my body to fight breast cancer?
- You can take it either way — with or without food. Food does slow down how quickly your body absorbs it, but the total amount that gets into your system stays the same. Pick whatev...
- Can I take anastrozole with food, or does it have to be on an empty stomach?
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII 3NXW29V3WO
Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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Lactose is a natural sugar derived from milk. In medications, it serves as a filler and binder to add bulk and help hold tablet or capsule ingredients together during manufacturing.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
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Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
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A starch-based powder made from potatoes and processed with sodium. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the medicine can be absorbed.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
7 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.140 | $4.20 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $0.3200 | $9.60 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $0.3837 | $11.51 / 30 tablets |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Anastrozole 1 mg 69117-0003-01 | Yiling | 30 tablets | $0.108 | AB | FDA listed | save 23% |
| Anastrozole 1 mg 00093-7536-56 | Teva | 30 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 16729-0035-10 | Accord | 30 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 23155-0857-03 | Avet | 30 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 50268-0075-15 | AvPAK | 50 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 51991-0620-10 | Breckenridge | 1000 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 59651-0236-30 | Aurobindo | 30 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 60687-0112-21 | American | 1 tablet | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 62135-0490-30 | Chartwell | 30 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mg 68001-0155-04 | BluePoint | 30 tablets | $0.140 | AB | Availability likely | — |
| Anastrozole 1 mgthis 68382-0209-06 | Zydus | 30 tablets | $0.140 | AB | Availability likely | — |
| Arimidex 1 mg 62559-0670-30 | ANI | 30 tablets | $52.862 | AB | Availability likely | +37639% |
| Anastrozole 1 mg 24979-0725-06 | Upsher-Smith | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 42291-0016-30 | AvKARE | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 42291-0085-30 | AvKARE | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 43063-0383-06 | PD-Rx | 6 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 50090-2453-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 50090-5002-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 63187-0080-18 | Proficient | 18 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 63629-5269-00 | Bryant | 28 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 63850-0010-01 | Natco | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 65841-0743-06 | Zydus | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-1543-09 | NuCare | 90 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-1682-03 | NuCare | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-2791-05 | NuCare | 15 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-3838-09 | NuCare | 90 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-3853-07 | NuCare | 12 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-3999-03 | NuCare | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-4038-03 | NuCare | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 68071-5203-03 | NuCare | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 71335-1879-00 | Bryant | 28 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 71335-3145-00 | Bryant | 28 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 72189-0415-30 | Direct_Rx | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 72789-0008-15 | PD-Rx | 15 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 72789-0342-15 | PD-Rx | 15 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 72789-0575-15 | PD-Rx | 15 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 76420-0004-12 | Asclemed | 120 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 82804-0162-30 | Proficient | 30 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 87063-0224-05 | ASCLEMED | 500 tablets | — | AB | FDA listed | — |
| Anastrozole 1 mg 72189-0682-30 | Direct_Rx | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 68382-0209-06 You're viewing this | 30 TABLET, COATED in 1 BOTTLE (68382-209-06) | $0.1401 / ea | $4.20 | 2010-06-27 | Active |
| 68382-0209-10 | 1000 TABLET, COATED in 1 BOTTLE (68382-209-10) | — | — | 2010-06-27 | Active |
You're viewing the smallest of 2 pack sizes for this product.
In Medicaid, this is the most-dispensed pack of this product — about 100% of fills over the last four reported quarters. See all packs ↓
Pack size FAQ
What quantity is in NDC 68382-0209-06?
What is the difference between NDC 68382-0209-06 and NDC 68382-0209-10?
What NDC number is used to bill for this package of Anastrozole 1 mg Tablet, Coated?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Anastrozole is an aromatase inhibitor indicated for: Adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer ( 1.1 ) First-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown locally advanced or metastatic breast cancer ( 1.2 ) Treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. Patients with ER-negative disease and patients who did not respond to previous tamoxifen therapy rarely responded to anastrozole ( 1.3 )
1.1Adjuvant Treatment Anastrozole tablets are indicated for adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer.
1.2First-Line Treatment Anastrozole tablets are indicated for the first-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown locally advanced or metastatic breast cancer.
1.3Second-Line Treatment Anastrozole tablets are indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. Patients with ER-negative disease and patients who did not respond to previous tamoxifen therapy rarely responded to anastrozole tablets.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION One 1 mg tablet taken once daily ( 2.1 )
2.1Recommended Dose The dose of anastrozole tablet is one 1 mg tablet taken once a day. For patients with advanced breast cancer, anastrozole tablet should be continued until tumor progression. Anastrozole tablets can be taken with or without food.
For adjuvant treatment of early breast cancer in postmenopausal women, the optimal duration of therapy is unknown. In the ATAC trial, anastrozole tablets were administered for five years [see Clinical Studies ( 14.1 )]. No dosage adjustment is necessary for patients with renal impairment or for elderly patients [see Use in Specific Populations ( 8.6 )].
2.2Patients with Hepatic Impairment No changes in dose are recommended for patients with mild-to-moderate hepatic impairment. Anastrozole tablet has not been studied in patients with severe hepatic impairment [see Use in Specific Populations ( 8.7 )].
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 1 mg tablets ( 3 ) The tablets are white, biconvex, round coated containing 1 mg of anastrozole. The tablets are debossed on one side with "A7" and plain on the other side.
⛔ Contraindications ▾
4 CONTRAINDICATIONS Hypersensitivity Anastrozole tablets are contraindicated in any patient who has shown a hypersensitivity reaction to the drug or to any of the excipients. Observed reactions include anaphylaxis, angioedema, and urticaria [see Adverse Reactions ( 6.2 ) ] . Patients with demonstrated hypersensitivity to anastrozole or any excipient ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS In women with pre-existing ischemic heart disease, an increased incidence of ischemic cardiovascular events occurred with anastrozole use compared to tamoxifen use. Consider risks and benefits. ( 5.1 , 6.1 ) Decreases in bone mineral density may occur.
Consider bone mineral density monitoring. ( 5.2 , 6.1 ) Increases in total cholesterol may occur. Consider cholesterol monitoring.
( 5.3 , 6.1 ) Embryo-Fetal Toxicity: anastrozole tablets may cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception. ( 5.4 , 8.1 )
5.1Ischemic Cardiovascular Events In women with pre-existing ischemic heart disease, an increased incidence of ischemic cardiovascular events was observed with anastrozole tablets in the ATAC trial (17% of patients on anastrozole tablets and 10% of patients on tamoxifen). Consider risk and benefits of anastrozole tablets therapy in patients with pre-existing ischemic heart disease [see Adverse Reactions ( 6.1 )].
5.2Bone Effects Results from the ATAC trial bone substudy at 12 and 24 months demonstrated that patients receiving anastrozole tablets had a mean decrease in both lumbar spine and total hip bone mineral density (BMD) compared to baseline. Patients receiving tamoxifen had a mean increase in both lumbar spine and total hip BMD compared to baseline. Consider bone mineral density monitoring in patients treated with anastrozole tablets [see Adverse Reactions ( 6.1 )].
5.3Cholesterol During the ATAC trial, more patients receiving anastrozole tablets were reported to have elevated serum cholesterol compared to patients receiving tamoxifen (9% versus 3.5%, respectively) [see Adverse Reactions ( 6.1 )].
5.4Embryo-Fetal Toxicity Based on findings from animal studies and its mechanism of action, anastrozole tablets can cause fetal harm when administered to a pregnant woman. Anastrozole caused embryo-fetal toxicities in rats at maternal exposure that were 9 times the human clinical exposure, based on area under the curve (AUC). In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 16 times the recommended human dose on a mg/m 2 basis.
Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during therapy with anastrozole tablets and for at least 3 weeks after the last dose [see Use in Specific Populations ( 8.1 , 8.3 ) and Clinical Pharmacology ( 12.1 )].
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS In the early breast cancer (ATAC) study, the most common (occurring with an incidence of ≥10%) side effects occurring in women taking anastrozole included: hot flashes, asthenia, arthritis, pain, arthralgia, pharyngitis, hypertension, depression, nausea and vomiting, rash, osteoporosis, fractures, back pain, insomnia, headache, peripheral edema and lymphedema, regardless of causality. ( 6.1 ) In the advanced breast cancer studies, the most common (occurring with an incidence of >10%) side effects occurring in women taking anastrozole included: hot flashes, nausea, asthenia, pain, headache, back pain, bone pain, increased cough, dyspnea, pharyngitis and peripheral edema.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Zydus Pharmaceuticals (USA) Inc. at 1-877-993-8779 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch Serious adverse reactions with anastrozole tablets occurring in less than 1 in 10,000 patients, are: 1) skin reactions such as lesions, ulcers, or blisters; 2) allergic reactions with swelling of the face, lips, tongue, and/or throat. This may cause difficulty in swallowing and/or breathing; and 3) changes in blood tests of the liver function, including inflammation of the liver with symptoms that may include a general feeling of not being well, with or without jaundice, liver pain or liver swelling [see Adverse Reactions ( 6.2 )].
Common adverse reactions (occurring with an incidence of ≥ 10%) in women taking anastrozole tablets included: hot flashes, asthenia, arthritis, pain, arthralgia, hypertension, depression, nausea and vomiting, rash, osteoporosis, fractures, back pain, insomnia, headache, bone pain, peripheral edema, increased cough, dyspnea, pharyngitis and lymphedema. In the ATAC trial, the most common reported adverse reaction (> 0.1%) leading to discontinuation of therapy for both treatment groups was hot flashes, although there were fewer patients who discontinued therapy as a result of hot flashes in the anastrozole tablets group.
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
6.1Clinical Trials Experience Adjuvant Therapy Adverse reaction data for adjuvant therapy are based on the ATAC trial [see Clinical Studies ( 14.1 )]. The median duration of adjuvant treatment for safety evaluation was 59.8 months and 59.6 months for patients receiving anastrozole tablets 1 mg and tamoxifen 20 mg, respectively. Adverse reactions occurring with an incidence of at least 5% in either treatment group during treatment or within 14 days of the end of treatment are presented in Table 1.
Table 1 Adverse reactions occurring with an incidence of at least 5% in either treatment group during treatment, or within 14 days of the end of treatment in the ATAC trial * * The combination arm was discontinued due to lack of efficacy benefit at 33 months of follow-up. † COSTART Coding Symbols for Thesaurus of Adverse Reaction Terms. ‡ A patient may have had more than 1 adverse reaction, including more than 1 adverse reaction in the same body system. § N=Number of patients receiving the treatment. ¶ Vaginal Hemorrhage without further diagnosis.
Body system and adverse reactions by COSTART † preferred term ‡ Anastrozole Tablets 1 mg (N § = 3092) Tamoxifen 20 mg (N § = 3094) Body as a whole Asthenia 575 (19) 544 (18) Pain 533 (17) 485 (16) Back pain 321 (10) 309 (10) Headache 314 (10) 249 (8) Abdominal pain 271 (9) 276 (9) Infection 285 (9) 276 (9) Accidental injury 311 (10) 303 (10) Flu syndrome 175 (6) 195 (6) Chest pain 200 (7) 150 (5) Neoplasm 162 (5) 144 (5) Cyst 138 (5) 162 (5) Cardiovascular Vasodilatation 1104 (36) 1264 (41) Hypertension 402 (13) 349 (11) Digestive Nausea 343 (11) 335 (11) Constipation 249 (8) 252 (8) Diarrhea 265 (9) 216 (7) Dyspepsia 206 (7) 169 (6) Gastrointestinal di…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Tamoxifen: Do not use in combination with anastrozole. No additional benefit seen over tamoxifen monotherapy. ( 7.1 , 14.1 ) Estrogen-containing products: Combination use may diminish activity of anastrozole. ( 7.2 )
7.1Tamoxifen Co-administration of anastrozole and tamoxifen in breast cancer patients reduced anastrozole plasma concentration by 27%. However, the co-administration of anastrozole and tamoxifen did not affect the pharmacokinetics of tamoxifen or N-desmethyltamoxifen. At a median follow-up of 33 months, the combination of anastrozole tablets and tamoxifen did not demonstrate any efficacy benefit when compared with tamoxifen in all patients as well as in the hormone receptor-positive subpopulation.
This treatment arm was discontinued from the trial [see Clinical Studies ( 14.1 )]. Based on clinical and pharmacokinetic results from the ATAC trial, tamoxifen should not be administered with anastrozole.
7.2Estrogen Estrogen-containing therapies should not be used with anastrozole tablets as they may diminish its pharmacological action.
7.3Warfarin In a study conducted in 16 male volunteers, anastrozole did not alter the exposure (as measured by C max and AUC) and anticoagulant activity (as measured by prothrombin time, activated partial thromboplastin time, and thrombin time) of both R- and S-warfarin.
7.4Cytochrome P450 Based on in vitro and in vivo results, it is unlikely that co-administration of anastrozole tablets 1 mg will affect other drugs as a result of inhibition of cytochrome P450 [see Clinical Pharmacology ( 12.3 )].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation: Do not breastfeed. ( 8.2 ) Females and Males of Reproductive Potential: Verify pregnancy status prior to initiation of anastrozole. ( 8.3 ) Pediatric patients: Efficacy has not been demonstrated for pubertal boys of adolescent age with gynecomastia or girls with McCune-Albright Syndrome and progressive precocious puberty. ( 8.4 )
8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, anastrozole tablets may cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )]. There are no studies of anastrozole tablets use in pregnant women. Anastrozole caused embryo-fetal toxicities in rats at maternal exposure that were 9 times the human clinical exposure, based on area under the curve (AUC).
In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 16 times the recommended human dose on a mg/m 2 basis. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In animal reproduction studies, pregnant rats and rabbits received anastrozole during organogenesis at doses equal to or greater than 0.1 and 0.02 mg/kg/day, respectively, (about 1 and 1/3 the recommended human dose on a mg/m 2 basis, respectively). In both species, anastrozole crossed the placenta, and there was increased pregnancy loss (increased pre-and/ or post-implantation loss, increased resorption, and decreased numbers of live fetuses).
In rats, these effects were dose related, and placental weights were significantly increased at doses equal to or greater than 0.1 mg/kg/day. Fetotoxicity, including delayed fetal development (i.e., incomplete ossification and depressed fetal body weights), occurred in rats at anastrozole doses of 1 mg/kg/day that produced peak plasma levels 19 times higher than serum levels in humans at the therapeutic dose (AUC 0-24hr 9 times higher). In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 1.0 mg/kg/day (about 16 times the recommended human dose on a mg/m 2 basis).
8.2Lactation Risk Summary There are no data on the presence of anastrozole or its metabolites in human milk, or its effects on the breast-fed child or on milk production. Because many drugs are excreted in human milk and because of the tumorigenicity shown for anastrozole in animal studies, or the potential for serious adverse reactions in the breast-fed child from anastrozole tablets, advise lactating women not to breastfeed during treatment with anastrozole tablets and for 2 weeks after the last dose.
8.3Females and Males of Reproductive Potential Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to initiation of anastrozole tablets. Contraception Females Based on animal studies, anastrozole tablets can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations ( 8.1 )]. Advise females of reproductive potential to use effective contraception during treatment with anastrozole tablets and for at least 3 weeks after the last dose.
Infertility Females Based on studies in female animals, anastrozole tablets may impair fertility in females of reproductive potential [see Nonclinical Toxicology ( 13.1 )].
8.4Pediatric Use Clinical studies in pediatric patients included a placebo-controlled trial in pubertal boys of adolescent age with gynecomastia and a single-arm trial in girls with McCune-Albright Syndrome and progressive precocious puberty. The efficacy of anastrozole in the treatment of pubertal gynecomastia in adolescent boys and in the treatment of precocious puberty in girls with McCune-Albright Syndrome has not been…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, anastrozole tablets may cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )]. There are no studies of anastrozole tablets use in pregnant women. Anastrozole caused embryo-fetal toxicities in rats at maternal exposure that were 9 times the human clinical exposure, based on area under the curve (AUC).
In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 16 times the recommended human dose on a mg/m 2 basis. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In animal reproduction studies, pregnant rats and rabbits received anastrozole during organogenesis at doses equal to or greater than 0.1 and 0.02 mg/kg/day, respectively, (about 1 and 1/3 the recommended human dose on a mg/m 2 basis, respectively). In both species, anastrozole crossed the placenta, and there was increased pregnancy loss (increased pre-and/ or post-implantation loss, increased resorption, and decreased numbers of live fetuses).
In rats, these effects were dose related, and placental weights were significantly increased at doses equal to or greater than 0.1 mg/kg/day. Fetotoxicity, including delayed fetal development (i.e., incomplete ossification and depressed fetal body weights), occurred in rats at anastrozole doses of 1 mg/kg/day that produced peak plasma levels 19 times higher than serum levels in humans at the therapeutic dose (AUC 0-24hr 9 times higher). In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 1.0 mg/kg/day (about 16 times the recommended human dose on a mg/m 2 basis).
🧒 Pediatric Use ▾
8.4Pediatric Use Clinical studies in pediatric patients included a placebo-controlled trial in pubertal boys of adolescent age with gynecomastia and a single-arm trial in girls with McCune-Albright Syndrome and progressive precocious puberty. The efficacy of anastrozole in the treatment of pubertal gynecomastia in adolescent boys and in the treatment of precocious puberty in girls with McCune-Albright Syndrome has not been demonstrated. Gynecomastia Study A randomized, double-blind, placebo-controlled, multi-center study enrolled 80 boys with pubertal gynecomastia aged 11 to 18 years.
Patients were randomized to a daily regimen of either anastrozole 1 mg or placebo. After 6 months of treatment there was no statistically significant difference in the percentage of patients who experienced a ≥ 50% reduction in gynecomastia (primary efficacy analysis). Secondary efficacy analyses (absolute change in breast volume, the percentage of patients who had any reduction in the calculated volume of gynecomastia, breast pain resolution) were consistent with the primary efficacy analysis.
Serum estradiol concentrations at Month 6 of treatment were reduced by 15.4% in the anastrozole group and 4.5% in the placebo group. Adverse reactions that were assessed as treatment-related by the investigators occurred in 16.3% of the anastrozole-treated patients and 8.1% of the placebo-treated patients with the most frequent being acne (7% anastrozole and 2.7% placebo) and headache (7% anastrozole and 0% placebo); all other adverse reactions showed small differences between treatment groups. One patient treated with anastrozole discontinued the trial because of testicular enlargement.
The mean baseline-subtracted change in testicular volume after 6 months of treatment was + 6.6 ± 7.9 cm 3 in the anastrozole-treated patients and + 5.2 ± 8.0 cm 3 in the placebo group. McCune-Albright Syndrome Study A multi-center, single-arm, open-label study was conducted in 28 girls with McCune-Albright Syndrome and progressive precocious puberty aged 2 to < 10 years. All patients received a 1 mg daily dose of anastrozole.
The trial duration was 12 months. Patients were enrolled on the basis of a diagnosis of typical (27/28) or atypical (1/27) McCune-Albright Syndrome, precocious puberty, history of vaginal bleeding, and/or advanced bone age. Patients' baseline characteristics included the following: a mean chronological age of 5.9 ± 2.0 years, a mean bone age of 8.6 ± 2.6 years, a mean growth rate of 7.9 ± 2.9 cm/year and a mean Tanner stage for breast of 2.7 ± 0.81.
Compared to pre-treatment data there were no on-treatment statistically significant reductions in the frequency of vaginal bleeding days, or in the rate of increase of bone age (defined as a ratio between the change in bone age over the change of chronological age). There were no clinically significant changes in Tanner staging, mean ovarian volume, mean uterine volume and mean predicted adult height. A small but statistically significant reduction of growth rate from 7.9 ± 2.9 cm/year to 6.5 ± 2.8 cm/year was observed but the absence of a control group precludes attribution of this effect to treatment or to other confounding factors such as variations in endogenous estrogen levels commonly seen in McCune-Albright Syndrome patients.
Five patients (18%) experienced adverse reactions that were considered possibly related to anastrozole. These were nausea, acne, pain in an extremity, increased alanine transaminase and aspartate transaminase, and allergic dermatitis. Pharmacokinetics in Pediatric Patients Following 1 mg once daily multiple administration in pediatric patients, the mean time to reach the maximum anastrozole concentration was 1 hr.
The mean (range) disposition parameters of anastrozole in pediatric patients were described by a CL/F of
1.54L/h (0.77 to
4.53 L/h) and V/F of
98.4L (50.7 to 330.0 L). The terminal elimination half-life was 46.8 h, which was similar to that observed in postmenopaus…
🧓 Geriatric Use ▾
8.5Geriatric Use In studies 0030 and 0027, about 50% of patients were 65 or older. Patients ≥ 65 years of age had moderately better tumor response and time to tumor progression than patients < 65 years of age regardless of randomized treatment. In studies 0004 and 0005, 50% of patients were 65 or older.
Response rates and time to progression were similar for the over 65 and younger patients. In the ATAC study, 45% of patients were 65 years of age or older. The efficacy of anastrozole tablets compared to tamoxifen in patients who were 65 years or older (N=1413 for anastrozole tablets and N=1410 for tamoxifen, the hazard ratio for disease-free survival was 0.93 [95% CI: 0.80, 1.08]) was less than efficacy observed in patients who were less than 65 years of age (N=1712 for anastrozole tablets and N=1706 for tamoxifen, the hazard ratio for disease-free survival was 0.79 [95% CI: 0.67, 0.94]).
The pharmacokinetics of anastrozole are not affected by age.
🆘 Overdosage ▾
10 OVERDOSAGE Clinical trials have been conducted with anastrozole tablets, up to 60 mg in a single dose given to healthy male volunteers and up to 10 mg daily given to postmenopausal women with advanced breast cancer; these dosages were tolerated. A single dose of anastrozole tablets that results in life-threatening symptoms has not been established. There is no specific antidote to overdosage and treatment must be symptomatic.
In the management of an overdose, consider that multiple agents may have been taken. Vomiting may be induced if the patient is alert. Dialysis may be helpful because anastrozole tablet is not highly protein bound.
General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action The growth of many cancers of the breast is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme.
Anastrozole is a selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
12.2Pharmacodynamics Effect on Estradiol Mean serum concentrations of estradiol were evaluated in multiple daily dosing trials with 0.5, 1, 3, 5, and 10 mg of anastrozole tablets in postmenopausal women with advanced breast cancer. Clinically significant suppression of serum estradiol was seen with all doses. Doses of 1 mg and higher resulted in suppression of mean serum concentrations of estradiol to the lower limit of detection (3.7 pmol/L).
The recommended daily dose, anastrozole tablets 1 mg, reduced estradiol by approximately 70% within 24 hours and by approximately 80% after 14 days of daily dosing. Suppression of serum estradiol was maintained for up to 6 days after cessation of daily dosing with anastrozole tablets 1 mg. The effect of anastrozole tablets in premenopausal women with early or advanced breast cancer has not been studied.
Because aromatization of adrenal androgens is not a significant source of estradiol in premenopausal women, anastrozole tablets would not be expected to lower estradiol levels in premenopausal women. Effect on Corticosteroids In multiple daily dosing trials with 3, 5, and 10 mg, the selectivity of anastrozole was assessed by examining effects on corticosteroid synthesis. For all doses, anastrozole did not affect cortisol or aldosterone secretion at baseline or in response to ACTH.
No glucocorticoid or mineralocorticoid replacement therapy is necessary with anastrozole. Other Endocrine Effects In multiple daily dosing trials with 5 and 10 mg, thyroid stimulating hormone (TSH) was measured; there was no increase in TSH during the administration of anastrozole tablets. Anastrozole tablet does not possess direct progestogenic, androgenic, or estrogenic activity in animals, but does perturb the circulating levels of progesterone, androgens, and estrogens.
12.3Pharmacokinetics Absorption Inhibition of aromatase activity is primarily due to anastrozole, the parent drug. Absorption of anastrozole is rapid and maximum plasma concentrations typically occur within 2 hours of dosing under fasted conditions. Studies with radiolabeled drug have demonstrated that orally administered anastrozole is well absorbed into the systemic circulation.
Food reduces the rate but not the overall extent of anastrozole absorption. The mean C max of anastrozole decreased by 16% and the median T max was delayed from 2 to 5 hours when anastrozole was administered 30 minutes after food. The pharmacokinetics of anastrozole are linear over the dose range of 1 to 20 mg, and do not change with repeated dosing.
The pharmacokinetics of anastrozole were similar in patients and healthy volunteers. Distribution Steady-state plasma levels are approximately 3- to 4-fold higher than levels observed after a single dose of anastrozole tablets. Plasma concentrations approach steady-state levels at about 7 days of once daily dosing.
Anastrozole is 40% bound to plasma proteins in the therapeutic range. Metabolism Metabolism of anastrozole occurs by N-dealkylation, hydroxylation and glucuronidation. Three metabolites of anastrozole (triazole, a glucuronide conjugate of hydroxy-anastrozole, and a glucuronide conjugate of anastrozole itself) have been identified in human plasma and urine.
The major circulating metabolite of anastrozole, triazole, la…
🧬 Mechanism of Action ▾
12.1Mechanism of Action The growth of many cancers of the breast is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme.
Anastrozole is a selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Anastrozole Tablets USP, 1 mg are white, biconvex, round coated tablets, debossed with 'A7' on one side and plain on other side and are supplied as follows: NDC 68382-209-06 in bottle of 30 tablets with child-resistant closure (unit-of-use package) NDC 68382-209-10 in bottle of 1000 tablets Storage Store at 20°C to 25°C (68°F to 77°F) [See USP Controlled Room Temperature]. Preserve in tight containers.
📋 Description ▾
11 DESCRIPTION Anastrozole tablets, USP for oral administration contain 1 mg of anastrozole, a non-steroidal aromatase inhibitor. It is chemically described as 1,3-Benzenediacetonitrile, a, a, a', a'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl). Its molecular formula is C 17 H 19 N 5 and its structural formula is: Anastrozole, USP is an off-white powder with a molecular weight of 293.4.
Anastrozole has moderate aqueous solubility (0.5 mg/mL at 25°C); solubility is independent of pH in the physiological range. Anastrozole is freely soluble in methanol, acetone, ethanol, and tetrahydrofuran, and very soluble in acetonitrile. Each tablet contains as inactive ingredients: lactose, magnesium stearate, hydroxypropylmethylcellulose, polyethylene glycol, povidone, sodium starch glycolate, and titanium dioxide.
Structured formula for Anastrozole Tablets
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION See FDA approved patient labeling (Patient Information). Hypersensitivity Reactions Inform patients of the possibility of serious allergic reactions with swelling of the face, lips, tongue and/or throat (angioedema) which may cause difficulty in swallowing and/or breathing and to seek medical attention immediately [see Contraindications ( 4 )]. Ischemic Cardiovascular Events Patients with pre-existing ischemic heart disease should be informed that an increased incidence of cardiovascular events has been observed with anastrozole tablets use compared to tamoxifen use.
Advise patients if new or worsening chest pain or shortness of breath occurs to seek medical attention immediately [see Warnings and Precautions ( 5.1 )]. Bone Effects Inform patients that anastrozole tablets lowers the level of estrogen. This may lead to a loss of the mineral content of bones, which might decrease bone strength.
A possible consequence of decreased mineral content of bones is an increase in the risk of fractures [see Warnings and Precautions ( 5.2 )]. Cholesterol Inform patients that an increased level of cholesterol might be seen while receiving anastrozole tablets [see Warnings and Precautions ( 5.3 )]. Carpal Tunnel Patients should be informed that if they experience tickling, tingling, or numbness they should notify their health care provider [see Adverse Reactions ( 6.1 )].
Tamoxifen Patients should be advised not to take anastrozole tablets with Tamoxifen [see Clinical Studies ( 14.1 )]. Missed Doses Inform patients that if they miss a dose, take it as soon as they remember. If it is almost time for their next dose, skip the missed dose and take the next regularly scheduled dose.
Patients should not take two doses at the same time. Embryo-Fetal Toxicity Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception during anastrozole tablets therapy and for at least 3 weeks after the last dose. Advise females to contact their healthcare provider if they become pregnant, or if pregnancy is suspected, during treatment with anastrozole tablets [see Warning and Precautions ( 5.4 ) and Use in Specific Populations ( 8.1 , 8.3 )].
Lactation Advise women not to breastfeed during anastrozole tablets treatment and for at least 2 weeks after the last dose [see Use in Specific Population ( 8.2 )]. Manufactured by: Zydus Lifesciences Ltd. Ahmedabad, India Distributed by: Zydus Pharmaceuticals (USA) Inc.
Pennington, NJ 08534 Rev.: 01/25