Testosterone / Anastrozole Pellets

Available Dosage Strengths

100 mg / 4 mg | 200 mg / 8 mg | 200 mg / 20 mg

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Disclaimer: Images are for reference only; actual products may vary.

Product Overview

Description

Anastrozole_Testosterone is a combination of an aromatase inhibitor (anastrozole) and the steroid hormone testosterone in a long-acting pellet.

Anastrozole Description^1-4

Anastrozole is a selective non-steroidal aromatase inhibitor, The drug blocks the conversion of androgens to estrogen. It has clinical applications in both women and men.

The drug has FDA approval for the following indications:

Adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer
First-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown locally advanced or metastatic breast cancer
Second-line treatment of advanced breast cancer that has progressed on Tamoxifen therapy
Treatment of male gynecomastia
Second-line treatment for the prevention of hormone-receptor-positive breast cancer

Testosterone Description^5,6

Micronized testosterone (natural) is derived from plants, most commonly, yams. This starting material undergoes a synthetic process to bioidentical testosterone. Unlike injectable testosterone, free testosterone is metabolized rapidly after absorption, requiring more frequent administration opposed to the weekly-monthly injections (cypionate, enanthate etc…). It is used commonly to treat male hypogonadism that is due to low testosterone and improve libido in both men and women. Micronized testosterone is used for compounded dosage forms including sterile implantable pellets.

Mechanism of Action

Anastrozole^1-4

Anastrozole is a selective non-steroidal aromatase inhibitor. 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. Suppression of estrogen biosynthesis in peripheral tissues and in cancer cells can be achieved by specifically inhibiting the aromatase enzyme. Therapeutically, this inhibition results in decreased systemic estrogen levels and increased systemic testosterone levels, which is therapeutic in estrogen-dependent breast cancers and in disease states where increased testosterone is important.^1,2

In men, LH, FSH and testosterone levels are increased when the enzyme aromatase is inhibited. The drug has been used in hypogonadism and in obese men where there an increased conversion of androgens to estrogen in the adipose tissue.

Testosterone^5-8

Testosterone binds to androgen receptors in various tissues, exerting anabolic and androgenic effects. These effects may include the development and maintenance of male secondary sexual characteristics, stimulation of muscle and bone growth, and regulation of libido and mood in both men and women.

Adverse Reactions

Anastrozole^1-4

Common

Hot flashes
Gastrointestinal (nausea, vomiting, abdominal pain)
Headache
Weight gain
Osteopenia
Insomnia

Testosterone^5-8

Common

Acne
Hypertension
Mood swings or irritability
Increased or decreased libido
Gynecomastia
Local reaction at implant site

Contraindications & Precautions

Contraindications^1-8

Known intolerance or hypersensitivity to anastrozole or testosterone.
Males with carcinoma of the breast or known or suspected carcinoma of the prostate.
Pregnant or breastfeeding women.
Patients with serious cardiac, hepatic, or renal disease.

Precautions^1-8

Monitor hematocrit and hemoglobin levels.
Regularly assess liver function tests.
Evaluate lipid profiles periodically.
Monitor for signs of sleep apnea.
Use cautiously in patients with a history of cardiovascular disease.
Wear gloves with topical preparations (creams/gels) and wash hands thoroughly after each application.
Use with caution in patients with pre-existing hypercholesterolemia.
Use with caution in patients with pre-existing osteoporosis; consider bone mineral density (BMD) monitoring in patients treated with anastrozole.
Not recommended in patients who are pregnant.

Storage

Store at room temperature 20°C to 25°C (68°F to 77°F) in a dry place, away from heat and light. Do not freeze. Keep out of reach of children. ^1,3

References

Clinical Pharmacology anastrozole clinical monograph 2025 https://www.clinicalkey.com/pharmacology/
de Ronde W, de Jong FH. Aromatase inhibitors in men: effects and therapeutic options. Reprod Biol Endocrinol. 2011 Jun 21;9:93.
Anastrozole (Ascend Laboratories, LLC): FDA Package Insert. https://medlibrary.org/lib/rx/meds/anstrozole-15/. Anastrozole package insert. Revised 03/11 Accessed May 20, 2025
Peters A, Tadi P. Aromatase Inhibitors. StatPearls. https://www.ncbi.nlm.nih.gov/books/NBK557856/ July 4, 2023. Accessed August 20, 2025
Clinical Pharmacology Testosterone clinical monograph accessed June 17 2025 ; https://www.clinicalkey.com/pharmacology/monograph/595?n=Testosterone
Tauchen J, Jurášek M, Huml L, Rimpelová S. Medicinal Use of Testosterone and Related Steroids Revisited. Molecules. 2021 Feb 15;26(4):1032. doi: 10.3390/molecules26041032. PMID: 33672087; PMCID: PMC7919692.
AndroGel (testosterone gel 1.62% for topical use) [package insert] AbbVie US LLC , revised May 2013, accessed June 2025 through: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021015s036lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/085635s040lbl.pdf
Clayton AH, Goldstein I, Kim NN, Althof SE, Faubion SS, Faught BM, Parish SJ, Simon JA, Vignozzi L, Christiansen K, Davis SR, Freedman MA, Kingsberg SA, Kirana PS, Larkin L, McCabe M, Sadovsky R. The International Society for the Study of Women’s Sexual Health Process of Care for Management of Hypoactive Sexual Desire Disorder in Women. Mayo Clin Proc. 2018 Apr;93(4):467-487. doi: 10.1016/j.mayocp.2017.11.002. Epub 2018 Mar 12. PMID: 29545008.

Disclaimer

This information is for educational purposes only. This compounded product has not been reviewed, approved, or evaluated by the Food and Drug Administration for safety and effectiveness. This product is not intended to diagnose, treat, cure, or prevent any disease. No claims are made regarding treatment, cure, or prevention of any disease or condition.

This information may not cover all possible drug information about this product. Call your doctor for medical advice and/or about side effects. You may report side effects to the FDA at 1-800-FDA-1088. A Wells Pharmacy Network pharmacist will be happy to answer any questions. For consultation, please call 1-800-622-4510.