Home › NDC Lookup › Ingredients › Anastrozole › 42291-0016-30
Anastrozole 1 mg Tablet, 30-count — NDC 42291-0016-30 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

Anastrozole 1 mg Tablet, 30-count — NDC 42291-016-30 (Billing 42291-0016-30)

by AvKARE · 30 TABLET in 1 BOTTLE

This is a package of 30 tablets of Anastrozole 1 mg Tablet from AvKARE, marketed since Feb 2023 and currently FDA-listed. It is the main listing for this product, which comes in 2 package sizes.

NDC 42291-0016-30
🏷️ FDA NDC (as labeled) 42291-016-30 billing pads the product segment with a zero
This package
Contains30-count Pack sizes2 compare ↓
Also priced by: Part D plans $0.3837/unit — full pricing hub ↓
Main listing for product 42291-016 · Also comes in: 90 tablets 42291-016-90
Rx only Generic On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 42291-016-30
Product NDC 42291-016
11-digit billing NDC 42291001630
NCPDP billing unit EA — each (per item)
RxCUI 199224
UNII 2Z07MYW1AZ
UPC 0342291016309, 0342291016903
Application # ANDA079220
SPL Set ID f40b925f-9f43-321d-e053-2a95a90aca8b
Established class (EPC) Aromatase Inhibitor
Mechanism of action Aromatase Inhibitors
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2023-02-06
Route ORAL
Dosage form TABLET
Substance ANASTROZOLE
TE code (Orange Book) AB · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GCN Seq No 024515
GCN 24410
HICL code 010249
Ingredient (HICL) Anastrozole
HIC1 code V
Therapeutic class — broad (HIC1) Neoplasms
HIC2 code V3
Therapeutic class — intermediate (HIC2) Antineoplastic Drugs (Continued 1)
HIC3 code V3F
Therapeutic class — specific (HIC3) Antineoplastic - Aromatase Inhibitors
AHFS code 10:00.00.00
AHFS class Antineoplastic Agents
FDB label name ANASTROZOLE 1 MG TABLET
FDB brand name Anastrozole
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 024515
  • GCN: 24410
  • HICL (First Databank): 010249
  • AHFS class code: 10:00.00.00
  • RxCUI (RxNorm): 199224
Why two NDCs? The FDA registers this code as 42291-016-30 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 42291-0016-30. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Aromatase Inhibitor class.

Pharmacologic class Aromatase Inhibitor
Drug family (ATC) Aromatase inhibitors
How it works Aromatase Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name ANASTROZOLE 1 MG TABLET Ingredient Anastrozole
📖 What it is MedlinePlus · NLM

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 ↗
📗 Our plain-language guide HelloPharmacist
  • 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?
📖 Read our full Anastrozole guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

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 systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $0.3837 $11.51 / 30 tablets
Medicare Part B allowsASP · J8999 No ASP payment limit on file for J8999 this quarter.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Billing & reimbursement

FDA NDC (as labeled)42291-016-30
11-digit billing NDC42291-0016-30
Format5-3-2 as registered → padded to 5-4-2 for billing (zero added to the product segment)
HCPCS J-codeJ8999
DescriptorPRESCRIPTION DRUG, ORAL, CHEMOTHERAPEUTIC, NOS
Billing units / pkg1 units
How the units are derivedThis package is 30 EA; the HCPCS unit is 1 EA, so one package = 1 billing unit.
Crosswalk sourcePDAC NDC-HCPCS crosswalk (DME MAC / DMEPOS)
Where does this data come from?
The HCPCS J-code crosswalk comes from the CMS ASP NDC-HCPCS crosswalk and the DMEPDAC (DME MAC) NDC-HCPCS crosswalk — free public CMS data. Billing units are derived from the code’s descriptor and the package amount.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
42291-0016-30 You're viewing this Main listing 30 TABLET in 1 BOTTLE 2023-02-06 — Active
42291-0016-90 42291-016-90 90 TABLET in 1 BOTTLE 2023-02-06 — Active

You're viewing the smallest of 2 pack sizes for this product.

Pack size FAQ

What quantity is in this package?
This is a 30-count package — 30 tablet in 1 bottle.
How does this package differ from NDC 42291-0016-90?
Both are Anastrozole 1 mg Tablet — the drug itself is identical. This page's package is the 30-count one, while NDC 42291-0016-90 is the 90 tablets package.
What NDC number is used to bill for this package of Anastrozole 1 mg Tablet?
Use the 11-digit billing form listed in the identifiers section of this page. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Anastrozole 1 mg 69117-0003-01 Yiling 30 tablets $0.108 AB FDA listed —
Anastrozole 1 mg 00093-7536-56 Teva 30 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 16729-0035-10 Accord 30 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 23155-0857-03 Avet 30 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 50268-0075-15 AvPAK 50 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 51991-0620-10 Breckenridge 1000 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 59651-0236-30 Aurobindo 30 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 60687-0112-21 American 1 tablet $0.142 AB Availability likely —
Anastrozole 1 mg 62135-0490-30 Chartwell 30 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 68001-0155-04 BluePoint 30 tablets $0.142 AB Availability likely —
Anastrozole 1 mg 68382-0209-06 Zydus 30 tablets $0.142 AB Availability likely —
Arimidex 1 mg 62559-0670-30 ANI 30 tablets $52.862 AB Availability likely —
Anastrozole 1 mg 24979-0725-06 Upsher-Smith 30 tablets — AB FDA listed —
Anastrozole 1 mgthis 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 —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2023
On the market since
Feb 2023
📍
2026
Currently FDA-listed
3 years listed
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

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?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

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.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerAvKARE
Application holderNATCO PHARMA LTD
FDA applicationANDA079220 (ANDA)
Labeler code42291
First marketedFeb 2023
Product typeHuman Prescription Drug
Portfolio384 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📦 Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Patient Package Insert 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 171 words ▾

1 INDICATIONS AND USAGE Anastrozole tablets are 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 tablets ( 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 146 words ▾

2 DOSAGE AND ADMINISTRATION One 1 mg tablet taken once daily ( 2.1 )

2.1Recommended Dose The dose of anastrozole tablets are one 1 mg tablet taken once a day. For patients with advanced breast cancer, anastrozole tablets 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 tablets have not been studied in patients with severe hepatic impairment [see Use in Specific Populations (8.7) ].

💊 Dosage Forms and Strengths 42 words ▾

3 DOSAGE FORMS AND STRENGTHS The tablets are white to off-white, round, film-coated containing 1 mg of anastrozole. The tablets are debossed with "AN" and "1" on one side and plain surface on the other side. 1 mg tablets ( 3 )

⛔ Contraindications 50 words ▾

4 CONTRAINDICATIONS Patients with demonstrated hypersensitivity to anastrozole tablets or any excipient ( 4 ) 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) ].

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS In women with pre-existing ischemic heart disease, an increased incidence of ischemic cardiovascular events occurred with anastrozole tablet 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 ~3 min read ▾

6 ADVERSE REACTIONS 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. In the early breast cancer (ATAC) study, the most common (occurring with an incidence of ≥10%) side effects occurring in women taking anastrozole tablets 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 tablets 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 contact AvKARE at 1-855-361-3993 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

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. Body system and adverse reactions by COSTART COSTART Coding Symbols for Thesaurus of Adverse Reaction Terms. preferred term A patient may have had more than 1 adverse reaction, including more than 1 adverse reaction in the same body system. Anastrozole tablets 1 mg (N N=Number of patients receiving the treatment. = 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 disorder 210 (7) 158 (5) Hemic and lymphatic Lymphedema 304 (10) 341 (1… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Tamoxifen: Do not use in combination with anastrozole tablets. No additional benefit seen over tamoxifen monotherapy ( 7.1 , 14.1 ) Estrogen-containing products: Combination use may diminish activity of anastrozole tablets ( 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 ~3 min read ▾

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 tablets. ( 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 tablets in the treatment of pubertal gynecomastia in adolescent boys and in the treatment of precocious puberty in girls with McCune-Albright Synd… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~1 min read ▾

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 ~3 min read ▾

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 tablets 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 tablets 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 tablets 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 tablets-treated patients and 8.1% of the placebo-treated patients with the most frequent being acne (7% anastrozole tablets and 2.7% placebo) and headache (7% anastrozole tablets and 0% placebo); all other adverse reactions showed small differences between treatment groups.

One patient treated with anastrozole tablets 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 tablets-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 tablets. 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 tablets. 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 (0.77-4.53 L/h) and V/F of

98.4L (50.7-330.0 L). The terminal elimination… [Excerpted — this section continues on DailyMed.]

🧓 Geriatric Use 164 words ▾

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 120 words ▾

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 tablets are not highly protein bound.

General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.

🧬 Clinical Pharmacology ~3 min read ▾

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 tablets 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, l… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 93 words ▾

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 33 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING These tablets are supplied in bottles of 30 Tablets (NDC 42291-016-30) and bottles of 90 Tablets (NDC 42291-016-90). Storage Store at controlled room temperature, 20-25°C (68-77°F) [see USP].

📦 Storage and Handling 10 words ▾

Storage Store at controlled room temperature, 20-25°C (68-77°F) [see USP].

📋 Description 108 words ▾

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 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: hypromellose, lactose monohydrate, magnesium stearate, polyethylene glycol, povidone, sodium starch glycolate and titanium dioxide.

Chemical Structure

💬 Information for Patients ~2 min read ▾

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) ] .

🧬 Pharmacokinetics ~3 min read ▾

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, lacks pharmacologic activity. Anastrozole inhibited reactions catalyzed by cytochrome P450 1A2, 2C8/9, and 3A4 in vitro with Ki values which were approximately 30 times higher than the mean steady-state C max values observed following a 1 mg daily dose. Anastrozole had no inhibitory effect on reactions catalyzed by cytochrome P450 2A6 or 2D6 in vitro .

Administration of a single 30 mg/kg or multiple 10 mg/kg doses of anastrozole to healthy subjects had no effect on the clearance of antipyrine or urinary recovery of antipyrine metabolites. Excretion Eighty-five percent of radiolabeled anastrozole was recovered in feces and urine. Hepatic metabolism accounts for approximately 85% of anastrozole elimination.

Renal elimination accounts for approximately 10% of total clearance. The mean elimination half-life of anastrozole is 50 hours. Effect of Gender and Age Anastrozole pharmacokinetics have been investigated in postmenopausal female volunteers and patients with breast cancer.

No age-related effects were seen over the range <50 to >80 years. Effect of Race Estradiol and estrone sulfate serum levels were similar between Japanese and Caucasian postmenopausal women who received 1 mg of anastrozole daily for 16 days. Anastrozole mean steady-state minimum plasma concentrations in Caucasian and Japanese postmenopausal women were 25.7 and 30.4 ng/mL, respectively.

Effect of Renal Impairment Anastrozole pharmacokinetics have been investigated in subjects with renal impairment. Anastrozole renal clearance decreased proportionally with creatinine clearance and was approximately 50% lower in volunteers with severe renal impairment (creatinine clearance < 30 mL/min/1.73m 2 ) compared to controls. Total clearance was only reduced 10%.

No dosage adjustment is needed for renal impairment [see Dosage and Administration (2.1) and Use in Specific Populations (8.6) ]. Effect of Hepatic Impairment Anastrozole pharmacokinetics have been investigated in subjects with hepatic cirrhosis related to alcohol abuse. The apparent oral clearance (CL/F) of anastrozole was approximately 30% lower in subjects with stable hepatic cirrhosis than in control subjects with normal liver function.

However, these plasma concentrations were still with the range of values observed in normal subjects. The effect of severe hepatic impairment was not studied. No dose adjustment is necessary for stable hepatic cirrhosis [see Dosage and Administration (2.2) and Use in Specific Populations (8.7) ].

🧬 Pharmacodynamics ~1 min read ▾

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 tablets does not possess direct progestogenic, androgenic, or estrogenic activity in animals, but does perturb the circulating levels of progesterone, androgens, and estrogens.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1Adjuvant Treatment of Breast Cancer in Postmenopausal Women A multicenter, double-blind trial (ATAC) randomized 9,366 postmenopausal women with operable breast cancer to adjuvant treatment with anastrozole tablets 1 mg daily, tamoxifen 20 mg daily, or a combination of the two treatments for five years or until recurrence of the disease. The primary endpoint of the trial was disease-free survival (i.e., time to occurrence of a distant or local recurrence, or contralateral breast cancer or death from any cause). Secondary endpoints of the trial included distant disease-free survival, the incidence of contralateral breast cancer and overall survival.

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. Based on clinical and pharmacokinetic results from the ATAC trial, tamoxifen should not be administered with anastrozole [see Drug Interactions (7.1) ].

Demographic and other baseline characteristics were similar among the three treatment groups (see Table 7 ). Table 7 – Demographic and Baseline Characteristics for ATAC Trial Demographic Characteristic Anastrozole tablets 1 mg (N N=Number of patients randomized to the treatment =3125) Tamoxifen 20 mg (N =3116) Anastrozole tablets 1 mg plus Tamoxifen The combination arm was discontinued due to lack of efficacy benefit at 33 months of follow-up 20 mg (N =3125) Mean age (yrs.) 64.1 64.1

64.3Age Range (yrs.) 38.1 - 92.8 32.8 - 94.9 37.0 –

92.2Age Distribution (%) <45 yrs. 0.7 0.4 0.5 45-60 yrs. 34.6 35.0 34.5 >60 <70 yrs. 38.0 37.1 37.7 >70 yrs. 26.7 27.4

27.3Mean Weight (kg) 70.8 71.1

71.3Receptor Status (%) Positive Includes patients who were estrogen receptor (ER) positive or progesterone receptor (PgR) positive, or both positive 83.5 83.1

84.0Negative Includes patients with both ER negative and PgR negative receptor status 7.4 8.0

7.0Other Includes all other combinations of ER and PgR receptor status unknown 8.8 8.6

9.0Other Treatment (%) prior to Randomization Mastectomy 47.8 47.3

48.1Breast conservation Among the patients who had breast conservation, radiotherapy was administered to 95.0% of patients in the anastrozole tablets arm, 94.1% in the tamoxifen arm and 94.5% in the anastrozole tablets plus tamoxifen arm. 52.3 52.8

51.9Axillary surgery 95.5 95.7

95.2Radiotherapy 63.3 62.5

61.9Chemotherapy 22.3 20.8

20.8Neoadjuvant Tamoxifen 1.6 1.6

1.7Primary Tumor Size (%) T1 (≤2 cm) 63.9 62.9

64.1T2 (>2 cm and ≤5 cm) 32.6 34.2

32.9T3 (>5 cm) 2.7 2.2

2.3Nodal Status (%) Node positive 34.9 33.6 33.5 1-3 (# of nodes) 24.4 24.4 24.3 4-9 7.5 6.4 6.8 >9 2.9 2.7

2.3Tumor Grade (%) Well-differentiated 20.8 20.5

21.2Moderately differentiated 46.8 47.8

46.5Poorly/undifferentiated 23.7 23.3

23.7Not assessed/recorded 8.7 8.4

8.5Patients in the two monotherapy arms of the ATAC trial were treated for a median of 60 months (5 years) and followed for a median of 68 months. Disease-free survival in the intent-to-treat population was statistically significantly improved [Hazard Ratio (HR) = 0.87, 95% CI: 0.78, 0.97, p=0.0127] in the anastrozole tablets arm compared to the tamoxifen arm. In the hormone receptor-positive subpopulation representing about 84% of the trial patients, disease-free survival was also statistically significantly improved (HR =0.83, 95% CI: 0.73, 0.94, p=0.0049) in the anastrozole tablets arm compared to the tamoxifen arm.

Figure 1 – Disease-Free Survival Kaplan Meier Survival Curve for all Patients Randomized to Anastrozole Tablets or Tamoxifen Monotherapy in the ATAC Trial (Intent-to-Treat) Figure 2 – Disease-Free Survival for Hormone Receptor-Positive Subpopulation of Patients Randomized to Anastrozole Tablets or Tamoxifen Monotherapy in the ATAC Trial The survival data with 68 months follow-up is presen… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology ~2 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility A conventional carcinogenesis study in rats at doses of 1.0 to 25 mg/kg/day (about 10 to 243 times the daily maximum recommended human dose on a mg/m 2 basis) administered by oral gavage for up to 2 years revealed an increase in the incidence of hepatocellular adenoma and carcinoma and uterine stromal polyps in females and thyroid adenoma in males at the high dose. A dose-related increase was observed in the incidence of ovarian and uterine hyperplasia in females.

At 25 mg/kg/day, plasma AUC 0-24 hr levels in rats were 110 to 125 times higher than the level exhibited in postmenopausal volunteers at the recommended dose. A separate carcinogenicity study in mice at oral doses of 5 to 50 mg/kg/day (about 24 to 243 times the daily maximum recommended human dose on a mg/m 2 basis) for up to 2 years produced an increase in the incidence of benign ovarian stromal, epithelial and granulosa cell tumors at all dose levels. A dose-related increase in the incidence of ovarian hyperplasia was also observed in female mice.

These ovarian changes are considered to be rodent-specific effects of aromatase inhibition and are of questionable significance to humans. The incidence of lymphosarcoma was increased in males and females at the high dose. At 50 mg/kg/day, plasma AUC levels in mice were 35 to 40 times higher than the level exhibited in postmenopausal volunteers at the recommended dose.

Anastrozole tablets have not been shown to be mutagenic in in vitro tests (Ames and E. coli bacterial tests, CHO-K1 gene mutation assay) or clastogenic either in vitro (chromosome aberrations in human lymphocytes) or in vivo (micronucleus test in rats). Oral administration of anastrozole to female rats (from 2 weeks before mating to pregnancy day 7) produced significant incidence of infertility and reduced numbers of viable pregnancies at 1 mg/kg/day (about 10 times the recommended human dose on a mg/m 2 basis and 9 times higher than the AUC 0-24 hr found in postmenopausal volunteers at the recommended dose).

Pre-implantation loss of ova or fetus was increased at doses equal to or greater than 0.02 mg/kg/day (about one-fifth the recommended human dose on a mg/m 2 basis). Recovery of fertility was observed following a 5-week non-dosing period which followed 3 weeks of dosing. It is not known whether these effects observed in female rats are indicative of impaired fertility in humans.

Multiple-dose studies in rats administered anastrozole for 6 months at doses equal to or greater than 1 mg/kg/day (which produced plasma anastrozole C ssmax and AUC 0-24 hr that were 19 and 9 times higher than the respective values found in postmenopausal volunteers at the recommended dose) resulted in hypertrophy of the ovaries and the presence of follicular cysts. In addition, hyperplastic uteri were observed in 6-month studies in female dogs administered doses equal to or greater than 1 mg/kg/day (which produced plasma anastrozole C ssmax and AUC 0-24 hr that were 22 times and 16 times higher than the respective values found in postmenopausal women at the recommended dose).

It is not known whether these effects on the reproductive organs of animals are associated with impaired fertility in premenopausal women.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ~2 min read ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility A conventional carcinogenesis study in rats at doses of 1.0 to 25 mg/kg/day (about 10 to 243 times the daily maximum recommended human dose on a mg/m 2 basis) administered by oral gavage for up to 2 years revealed an increase in the incidence of hepatocellular adenoma and carcinoma and uterine stromal polyps in females and thyroid adenoma in males at the high dose. A dose-related increase was observed in the incidence of ovarian and uterine hyperplasia in females.

At 25 mg/kg/day, plasma AUC 0-24 hr levels in rats were 110 to 125 times higher than the level exhibited in postmenopausal volunteers at the recommended dose. A separate carcinogenicity study in mice at oral doses of 5 to 50 mg/kg/day (about 24 to 243 times the daily maximum recommended human dose on a mg/m 2 basis) for up to 2 years produced an increase in the incidence of benign ovarian stromal, epithelial and granulosa cell tumors at all dose levels. A dose-related increase in the incidence of ovarian hyperplasia was also observed in female mice.

These ovarian changes are considered to be rodent-specific effects of aromatase inhibition and are of questionable significance to humans. The incidence of lymphosarcoma was increased in males and females at the high dose. At 50 mg/kg/day, plasma AUC levels in mice were 35 to 40 times higher than the level exhibited in postmenopausal volunteers at the recommended dose.

Anastrozole tablets have not been shown to be mutagenic in in vitro tests (Ames and E. coli bacterial tests, CHO-K1 gene mutation assay) or clastogenic either in vitro (chromosome aberrations in human lymphocytes) or in vivo (micronucleus test in rats). Oral administration of anastrozole to female rats (from 2 weeks before mating to pregnancy day 7) produced significant incidence of infertility and reduced numbers of viable pregnancies at 1 mg/kg/day (about 10 times the recommended human dose on a mg/m 2 basis and 9 times higher than the AUC 0-24 hr found in postmenopausal volunteers at the recommended dose).

Pre-implantation loss of ova or fetus was increased at doses equal to or greater than 0.02 mg/kg/day (about one-fifth the recommended human dose on a mg/m 2 basis). Recovery of fertility was observed following a 5-week non-dosing period which followed 3 weeks of dosing. It is not known whether these effects observed in female rats are indicative of impaired fertility in humans.

Multiple-dose studies in rats administered anastrozole for 6 months at doses equal to or greater than 1 mg/kg/day (which produced plasma anastrozole C ssmax and AUC 0-24 hr that were 19 and 9 times higher than the respective values found in postmenopausal volunteers at the recommended dose) resulted in hypertrophy of the ovaries and the presence of follicular cysts. In addition, hyperplastic uteri were observed in 6-month studies in female dogs administered doses equal to or greater than 1 mg/kg/day (which produced plasma anastrozole C ssmax and AUC 0-24 hr that were 22 times and 16 times higher than the respective values found in postmenopausal women at the recommended dose).

It is not known whether these effects on the reproductive organs of animals are associated with impaired fertility in premenopausal women.

📄 Patient Package Insert ~3 min read ▾

Patient Information Anastrozole (an-AS-troe-zole) Tablets, USP What is the most important information I should know about anastrozole tablets? Anastrozole tablets may cause serious side effects including: heart disease. Women with early breast cancer, who have a history of blockage in their heart arteries (ischemic heart disease) and who take anastrozole tablets, may have an increase in symptoms of decreased blood flow to their heart compared to similar women who take tamoxifen.

Get medical help right away if you have new or worsening chest pain or shortness of breath during treatment with anastrozole tablets. What are anastrozole tablets? Anastrozole tablets are a prescription medicine used in women after menopause ("the change of life") for: treatment of early breast cancer after surgery in women whose breast cancer is hormone receptor-positive the first treatment of breast cancer that has spread to nearby tissue or lymph nodes (locally advanced) or has spread to other parts of the body (metastatic), in women whose breast cancer is hormone receptor-positive or the hormone receptors are not known. treatment of advanced breast cancer, if the cancer has grown, or the disease has spread after tamoxifen therapy Anastrozole tablets does not work in women with breast cancer who have not gone through menopause (premenopausal women).

Who should not take anastrozole tablets? Do not take anastrozole tablet if you: have had a severe allergic reaction to anastrozole or any of the ingredients in anastrozole tablets. See the end of this leaflet for a complete list of ingredients in anastrozole tablets.

Symptoms of a severe allergic reaction to anastrozole tablets include: swelling of the face, lips, tongue or throat, trouble breathing or swallowing, hives and itching. What should I tell my healthcare provider before taking anastrozole tablets? Before you take anastrozole tablets, tell your healthcare provider if you: are still having menstrual periods (are not past menopause).

Talk to your healthcare provider if you are not sure. have or had a heart problem have been told you have bone thinning or weakness (osteoporosis) have high cholesterol have any other medical conditions are pregnant or plan to become pregnant. Taking anastrozole tablets during pregnancy or within 3 weeks of becoming pregnant may harm your unborn baby. Females who are able to become pregnant should have a pregnancy test before starting treatment with anastrozole tablets.

Females who are able to become pregnant should use effective birth control (contraceptive) during treatment with anastrozole tablets and for 3 weeks after your last dose of anastrozole tablets. Tell your healthcare provider right away if you become pregnant or think you may be pregnant. are breastfeeding or plan to breastfeed. It is not known if anastrozole tablets passes into breast milk.

Do not breastfeed during treatment with anastrozole tablets and for 2 weeks after your last dose of anastrozole tablets. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take: tamoxifen.

You should not take anastrozole tablets if you take tamoxifen. Taking anastrozole tablets with tamoxifen may lower the amount of anastrozole tablets in your blood and may cause anastrozole tablets not to work as well. Medicines that contain estrogen.

Anastrozole tablets may not work if taken with any of these medicines: hormone replacement therapy birth control pills estrogen creams vaginal rings vaginal suppositories Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine. How should I take anastrozole tablets?

Take anastrozole tablets exactly as your healthcare provider tells you to take it. Continue taking anastrozole tablets until your healthcare provider tells you to stop. Anastrozole tablets can be taken with… [Excerpted — this section continues on DailyMed.]

📄 Package Label / Principal Display Panel 10 words ▾

PRINCIPAL DISPLAY PANEL - 30 Tablet Bottle Label 30 90

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Anastrozole — the program that covers self-administered drugs. 9 manufacturers.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Anastrozole. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$8.82M
Claims incl. refills
434.6K
Beneficiaries
334.3K
Spend / beneficiary
$26.38
Spend / claim
$20.30
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk ✓ Available
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by AvKARE. Listing status can change — the directory data on this page refreshes weekly.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 90 tablets (42291-0016-90). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
AvKARE is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
Does this product have a billing J-code?
Yes — this NDC cross-references HCPCS code J8999 for medical-claim billing (typically used when a product is administered in a clinical setting rather than dispensed at a retail pharmacy). See the Billing section on this page.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
← 42291-0015-01 · AvKARE 42291-0024-12 · AvKARE →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.