Kyzatrex TESTOSTERONE UNDECANOATE 100 mg Capsule, Liquid Filled, 120-count
🆔 Identity & classification
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🏭 Manufacturer & labeler
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🩺 Clinical
Testosterone is used to treat low or no testosterone levels in men. Testosterone is a male sex hormone responsible for development and functioning of male sex organs and male characteristics. Testosterone works by replacing testosterone that is normally produced by the body.
Read the full MedlinePlus article ↗- Testosterone replacement is specifically for men whose bodies aren't making enough testosterone because of a medical condition — like a problem with the testes themselves (primary...
- What exactly is testosterone replacement therapy for — do I really need it?
- Yes, this is a serious concern. Children who accidentally touch the gel on your skin or clothing can absorb testosterone and develop early puberty signs — things like pubic hair gr...
- I use the gel — do I really need to worry about my kids or partner being exposed to it?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Testosterone Undecanoate — tap one for details:
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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 H4N855PNZ1
Alpha-tocopherol is a form of vitamin E, a fat-soluble antioxidant derived from natural or synthetic sources. In medicines, it prevents oils and fats from breaking down and becoming rancid, protecting the product's stability and shelf life.
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UNII 2G86QN327L
Gelatin is a protein derived from animal collagen, commonly used in medicines as a gelling agent and capsule material. It helps create soft or hard capsule shells that hold and release medication, and can also thicken liquid formulations.
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UNII PDC6A3C0OX
Glycerin is a clear, thick liquid derived from plant oils or fats. It acts as a humectant to retain moisture, a sweetener, and a solvent in medications.
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UNII 7YC686GQ8F
A synthetic oily substance made from castor oil. It works as a solubilizer and emulsifier to help mix oily and water-based ingredients together in the medicine.
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UNII 668Z5835Z3
Propylene glycol monolaurate is a synthetic compound made by combining propylene glycol with lauric acid. It acts as an emulsifier and surfactant in medicines, helping oil and water-based ingredients mix smoothly and improving how the drug dissolves or spreads in the body.
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UNII 506T60A25R
Sorbitol is a natural sugar alcohol derived from glucose. It serves as a sweetener, humectant, and bulking agent in medications to improve taste and help maintain moisture in the product.
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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.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
8 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 mL | Per 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 · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Kyzatrex 100 mgthis 80603-0101-22 | Marius | 120 capsules | — | — | Discontinued | — |
Where does this data come from?
⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 12403146 ↗ | Method of use | U-2506 | Mar 29, 2041 |
| US 12403146 ↗ | Method of use | U-2506 | Mar 29, 2041 |
| US 12403146 ↗ | Method of use | U-2506 | Mar 29, 2041 |
| US 11617758 ↗ | Method of use | U-2506 | Mar 15, 2033 |
| US 11617758 ↗ | Method of use | U-2506 | Mar 15, 2033 |
| US 11617758 ↗ | Method of use | U-2506 | Mar 15, 2033 |
| US 12357643 ↗ | Method of use | U-2506 | Mar 15, 2033 |
| US 12357643 ↗ | Method of use | U-2506 | Mar 15, 2033 |
| US 12357643 ↗ | Method of use | U-2506 | Mar 15, 2033 |
| US 10576089 ↗ | Method of use | U-2506 | Dec 31, 2030 |
| US 10576089 ↗ | Method of use | U-2506 | Dec 31, 2030 |
| US 10576089 ↗ | Method of use | U-2506 | Dec 31, 2030 |
| US 11590146 ↗ | Drug product | — | Dec 31, 2030 |
| US 10576090 ↗ | Drug product | — | Dec 31, 2030 |
| US 10576090 ↗ | Drug product | — | Dec 31, 2030 |
| US 11590146 ↗ | Drug product | — | Dec 31, 2030 |
| US 11590146 ↗ | Drug product | — | Dec 31, 2030 |
| US 10576090 ↗ | Drug product | — | Dec 31, 2030 |
Is there a generic version of KYZATREX 100 MG CAPSULE?
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 80603-0101-11 | 90 CAPSULE, LIQUID FILLED in 1 BOTTLE (80603-101-11) | 2022-07-27 | Discontinued by firm |
| 80603-0101-22 You're viewing this | 120 CAPSULE, LIQUID FILLED in 1 BOTTLE (80603-101-22) | 2022-07-27 | Discontinued by firm |
You're viewing the largest of 2 pack sizes for this product.
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🧭 About this NDC listing & data coverage
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| 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) | ✓ 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 | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE KYZATREX® is indicated for testosterone replacement therapy in adult males for conditions associated with a deficiency or absence of endogenous testosterone: Primary hypogonadism (congenital or acquired): testicular failure due to conditions such as cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter syndrome, chemotherapy, or toxic damage from alcohol or heavy metals. These men usually have low serum testosterone concentrations and gonadotropins (folliclestimulating hormone (FSH), luteinizing hormone (LH)) above the normal range.
Hypogonadotropic hypogonadism (congenital or acquired): gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency, pituitary-hypothalamic injury from tumors, trauma, or radiation. These men have low serum testosterone concentrations but have gonadotropins in the normal or low range. KYZATREX® is an androgen indicated for testosterone replacement therapy in adult males for conditions associated with a deficiency or absence of endogenous testosterone ( 1 ).
Limitations of Use: Safety and efficacy of KYZATREX® in males less than 18 years old have not been established ( 1 , 8.4 ). Safety and efficacy of KYZATREX® in men with “age-related hypogonadism” have not been established (1) . Limitations of Use Safety and efficacy of KYZATREX® in males less than 18 years old have not been established [see Use in Specific Populations (8.4) ] .
Safety and efficacy of KYZATREX® in men with “age-related hypogonadism” (also referred to as “late-onset hypogonadism”) have not been established.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION - KYZATREX® is not substitutable with other oral testosterone undecanoate products ( 2.1 ). Prior to initiating KYZATREX®, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least two separate days and that these concentrations are below the normal range ( 2.2 ). Take KYZATREX® with food ( 2.3 ).
Starting dosage: 200 mg orally once in the morning and once in the evening ( 2.3 ). Adjust the dosage to a minimum of 100 mg once in the morning and a maximum of 400 mg twice daily based on serum testosterone drawn 3 to 5 hours after the morning dose at least 7 days after starting treatment or following dose adjustment and periodically thereafter ( 2.3 ).
2.1Important Dosage Information KYZATREX® is not substitutable with other oral testosterone undecanoate products.
2.2Confirmation of Hypogonadism Before Initiation of KYZATREX® Prior to initiating KYZATRE®, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least two separate days and that these testosterone concentrations are below the normal range.
2.3Recommended Dosage and Administration Individualize the dosage of KYZATREX® based on the patient's serum testosterone concentration response to the drug. The recommended starting dose is 200 mg orally twice daily, once in the morning and once in the evening. Take KYZATREX® with food.
Dosage Adjustment Check serum testosterone concentrations 7 days after starting treatment or after dosage adjustment, 3 to 5 hours after the morning dose. Adjust the KYZATREX® dose as necessary as shown in Table 1. Thereafter, periodically monitor serum testosterone concentrations.
The minimum recommended dose is 100 mg once daily in the morning. The maximum recommended dose is 400 mg twice daily. For total daily doses greater than 100 mg, administer the same dose in the morning and evening.
Table 1: KYZATREX® Dosage Adjustment Scheme Serum Testosterone Concentration Current KYZATREX® Dosage New KYZATREX® Dosage Less than 460 ng/dL 100 mg with breakfast only 100 mg twice daily with meals 100 mg twice daily with meals 200 mg twice daily with meals 200 mg twice daily with meals 300 mg twice daily with meals 300 mg twice daily with meals 400 mg twice daily with meals 460 to 971 ng/dL No Dosage Change More than 971 ng/dL 400 mg twice daily with meals 300 mg twice daily with meals 300 mg twice daily with meals 200 mg twice daily with meals 200 mg twice daily with meals 100 mg twice daily with meals 100 mg twice daily with meals 100 mg with breakfast only 100 mg with breakfast only Discontinue treatment
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Capsules: 50 mg, oval, opaque, white, imprinted with "MP50" in red ink 100 mg, oval, opaque, white, imprinted with "MP100" in red ink 150 mg, oblong, opaque, white, imprinted with "MP150" in red ink 200 mg, oblong, opaque, white, imprinted with "MP200" in red ink Capsules: 50 mg,100 mg, 150 mg, 200 mg ( 3 ).
⛔ Contraindications ▾
4 CONTRAINDICATIONS KYZATREX® is contraindicated in: Patients with carcinoma of the breast or known or suspected carcinoma of the prostate [see Warnings and Precautions (5.34) ] . Women who are pregnant. Testosterone can cause virilization of the female fetus when administered to a pregnant woman [ see Use in Specific Populations (8.1) ].
Patients with known hypersensitivity to KYZATREX® or any of its ingredients [see Description (11) ] . Carcinoma of the breast or known or suspected carcinoma of the prostate ( 5.4 ) Women who are pregnant. Testosterone may cause fetal harm ( 4 , 5.7 , 8.1 ) Hypersensitivity to KYZATREX® or any of its ingredients ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS - Polycythemia : Monitor hemoglobin or hematocrit approximately every 3 months to detect increased red blood cell mass and polycythemia. Discontinue KYZATREX® if necessary ( 5.1 ). Venous thromboembolism (VTE) : VTE, including deep vein thrombosis (DVT) and pulmonary embolism (PE) have been reported in patients using testosterone.
Discontinue KYZATREX® if VTE is suspected and initiate appropriate workup and management (5.2) Worsening of Benign Prostatic Hyperplasia (BPH) and Potential Risk of Prostate Cancer : Monitor patients for worsening of signs and symptoms of BPH. Evaluate patients for prostate cancer, including monitoring prostate specific antigen (PSA) prior to initiating and during treatment with androgens ( 5.3 ). Blood Pressure Increases: KYZATREX® can increase blood pressure, which can increase cardiovascular risk over time.
Measure blood pressure periodically. Not recommended for use in men with uncontrolled hypertension ( 5.4 ) Abuse of Testosterone and Monitoring of Serum Testosterone : If testosterone use at doses higher than recommended for the approved indication and in combination with other anabolic androgenic steroids is suspected, check serum testosterone concentration ( 5.5 ). Potential for Adverse Effects on Spermatogenesis : KYZATREX® may cause azoospermia ( 5.7 ).
Edema : Edema, with or without congestive heart failure (CHF), may occur in patients with pre-existing cardiac, renal, or hepatic disease. Discontinue KYZATREX® and initiate appropriate workup ( 5.9 ). Sleep Apnea : KYZATREX® may potentiate sleep apnea in those with risk factors ( 5.10 ) Lipid Changes : KYZATREX® may affect serum lipid profile.
Monitor patient lipid concentrations periodically; if necessary, adjust dosage of lipid lowering drug(s) or discontinue KYZATREX® ( 5.12 ).
5.1Polycythemia Androgens, including KYZATREX®, can cause increase in hemoglobin or hematocrit, reflective of increase in red blood cell mass. Check hematocrit prior to initiating KYZATREX®. An increase in red blood cell mass may increase the risk of thromboembolic events [see Warnings and Precautions ( 5.2 )].
Evaluate hematocrit approximately every 3 months while the patient is on KYZATREX®. If hematocrit becomes elevated, stop KYZATREX® until the hematocrit decreases to an acceptable concentration. If KYZATREX® is restarted and again causes hematocrit to become elevated, permanently discontinue KYZATREX®.
5.2Venous Thromboembolism There have been post-marketing reports of venous thromboembolic events, including deep vein thrombosis (DVT) and pulmonary embolism (PE), in patients using testosterone replacement products such as KYZATREX®. In the Testosterone Replacement therapy for Assessment of long-term Vascular Events and efficacy Response in hypogonadal men (TRAVERSE) Study, a randomized, double-blind, placebo-controlled, cardiovascular (CV) outcomes study, compared to placebo, topical testosterone gel was associated with a numerically higher incidence of VTE (1.7% vs 1.2%) which included DVT (0.6% vs 0.5%) and PE events (0.9% vs 0.5%) [see Adverse Reactions 6.1 )].
Evaluate patients who report symptoms of pain, edema, warmth, and erythema in the lower extremity for DVT and those who present with acute shortness of breath for PE. If a venous thromboembolic event is suspected, discontinue KYZATREX® and initiate appropriate workup and management [see Adverse Reactions ( 6.2 )].
5.3Worsening of Benign Prostatic Hyperplasia (BPH) and Potential Risk of Prostate Cancer Patients with BPH who are treated with androgens are at an increased risk for worsening of signs and symptoms of BPH. Monitor patients with BPH for worsening signs and symptoms. Patients treated with androgens may be at increased risk for prostate cancer.
Evaluate patients for prostate cancer prior to initiating and during treatment with androgens [see Contraindications (4)].
5.4Blood Pressure Increases KYZATREX® can increase blood pressure. Based on ambulatory blood mon…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed elsewhere in the labeling: Polycythemia [see Warnings and Precautions (5.1) ] Venous Thromboembolism [see Warnings and Precautions (5.2) ] Worsening of Benign Prostatic Hyperplasia (BPH) and Potential Risk of Prostate Cancer [ see Warnings and Precautions (5.3) ] Blood Pressure Increases [see Warnings and Precautions (5.4) ] Hepatic Adverse Effects [see Warnings and Precautions (5.8) ] Edema [see Warnings and Precautions (5.9) ] Sleep Apnea [see Warnings and Precautions (5.10) ] Gynecomastia [see Warnings and Precautions (5.11) ] Lipid Changes [see Warnings and Precautions (5.12) ] Hypercalcemia [see Warnings and Precautions (5.13) ] Decreased Thyroxine-binding Globulin [see Warnings and Precautions (5.14) ] Most common adverse reactions (incidence ≥ 2%): hypertension ( 6.1 ).
To report SUSPECTED ADVERSE REACTIONS, contact Marius Pharmaceuticals at 1-833-949-5040 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Trial Experience 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. The safety of KYZATREX® was evaluated in Study MRS-TU-2019EXT in 155 hypogonadal males [see Clinical Studies (14) ]. All patients initially received KYZATREX® 200 mg orally twice daily.
If needed, the dosage was titrated to 100 mg once daily in the morning or 100 mg, 300 mg, or 400 mg twice daily to achieve testosterone concentrations in the normal range . After the dosage titration period, patients continued their optimized dose for the remainder of the duration of the 6-month study. The mean duration of exposure was 168 days (range: 1 to 180 days).
The median age was 52 years (range: 22 to 66 years); 77% were White, 19% were Black, 3% were Asian, and 2% were American Indian, Alaskan Native or Other. Table 2 summarizes adverse reactions reported in ≥2% of patients in this 6-month study. Table 2: Adverse Reactions in ≥ 2% of Patients Receiving KYZATREX® in STUDY MRS-TU-2019EXT Adverse Reaction N = 155 n (%) Hypertensión Based upon blood pressure cuff measurements 4 (2.6) One (0.8%) patient who received KYZATREX® experienced an adverse reaction (acne) that lead to premature discontinuation from the study.
In a 12-month, open-label study in hypogonadal adult males (N=212) who received KYZATREX® 200 mg once daily to 400 mg twice daily (n=202) the following additional adverse reactions were reported: headache, arthralgia, diarrhea, hemoglobin increased, anxiety, constipation, peripheral edema, and PSA increased. Blood Pressure Increases In Study MRS-TU-2019EXT, 24-hour ambulatory blood pressure monitoring (ABPM) was conducted in 155 male patients, 135 of whom completed the study. ABPM was conducted at 3 distinct 24-hour time periods: at baseline and following approximately 4 months and 6 months of treatment with KYZATREX®.
A total of 151 patients had acceptable 24-hour ABPM recordings at both time periods. In that group, the mean change in systolic BP from Baseline to 4 months and 6 months was + 1.7 mm Hg (95% CI 0.3, 3.1) and 1.8 mm Hg (95% CI 0.3, 3.2), respectively. In that group, the mean change in diastolic BP from Baseline to 4 months and 6 months was 0.6 mm Hg (95% CI -0.3, 1.6) and 0.6 mm Hg (95% CI -0.4, 1.6), respectively.
In patients with a history of hypertension on antihypertensive therapy at baseline, the mean ABPM systolic blood pressure increased from Baseline to 4 months and 6 months by 3.4 mm Hg (95% CI 1.0, 5.9) and 3.1 mm Hg (95% CI 0.6, 5.6), respectively (n=49). In patients with no history of hypertension at baseline, the mean systolic blood pressure from Baseline increased by 0.7 mm Hg (95% CI -1.0, 2.4) at 4 months and 1.0 mm Hg (95% CI -0.7, 2.8), at six months respectively (n =90). Ambulatory (24-hour) blood pressure Cha…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS - Insulin: In patients with diabetes, concomitant use with KYZATREX® may decrease blood glucose and insulin requirements ( 7.1 ). Oral Anticoagulants: Concomitant use with KYZATREX® may cause changes in anticoagulant activity. Monitor International Normalized Ratio (INR) and prothrombin time (PT) frequently ( 7.2 ).
Corticosteroids: Concomitant use with KYZATREX® may result in increased fluid retention. Use with caution, particularly in patients with cardiac, renal, or hepatic disease ( 7.3 ). Drugs that May Also Increase Blood Pressure: Concomitant use with KYZATREX® may lead to additional increases in blood pressure ( 7.4 ).
7.1Insulin Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and therefore necessitate a decrease in the dose of anti-diabetic medication.
7.2Oral Vitamin K Antagonist Anticoagulants Changes in anticoagulant activity may be seen with androgens; therefore, more frequent monitoring of international normalized ratio (INR) and prothrombin time are recommended in patients taking warfarin, especially at the initiation and termination of androgen therapy.
7.3Corticosteroids The concurrent use of testosterone with corticosteroids may result in increased fluid retention and requires careful monitoring particularly in patients with cardiac, renal, or hepatic disease.
7.4Medications that May Also Increase Blood Pressure Some prescription medications and nonprescription analgesic and cold medications contain drugs known to increase blood pressure. Concomitant administration of these medications with KYZATREX® may lead to additional increases in blood pressure [see Warnings and Precautions (5.4)] .
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS - Geriatric Patients: Geriatric patients treated with androgens may also be at risk for worsening of signs and symptoms of BPH and hypertension ( 8.5 ). See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling and Medication Guide.
8.1Pregnancy - Risk Summary KYZATREX® is contraindicated in pregnant women and not indicated for use in females [see Contraindications (4) ]. Testosterone is teratogenic and may cause fetal harm when administered to a pregnant woman based on data from animal studies (see Data ) and its mechanism of action [see Clinical Pharmacology (12.1) ]. Exposure of a female fetus to androgens may result in varying degrees of virilization.
In animal developmental studies, exposure to testosterone in utero resulted in hormonal and behavioral changes in offspring and structural impairments of reproductive tissues in female and male offspring. These studies do not meet current standards for nonclinical development toxicity studies. Data Animal Data In developmental studies conducted in rats, rabbits, pigs, sheep, and rhesus monkeys, pregnant animals received intramuscular injections of testosterone during the period of organogenesis.
Testosterone treatment at doses that were comparable to those used for testosterone replacement therapy resulted in structural impairments in both female and male offspring. Structural impairments observed in females included increased anogenital distance, phallus development, empty scrotum, no external vagina, intrauterine growth retardation, reduced ovarian reserve, and increased ovarian follicular recruitment. Structural impairments seen in male offspring included increased testicular weight, larger seminal tubular lumen diameter, and higher frequency of occluded tubule lumen.
Increased pituitary weight was seen in both sexes. Testosterone exposure in utero also resulted in hormonal and behavioral changes in offspring. Hypertension was observed in pregnant female rats and their offspring exposed to doses approximately twice those used for testosterone replacement therapy.
8.2Lactation - Risk Summary KYZATREX® is not indicated for use in females.
8.3Females and Males of Reproductive Potential - Infertility Males During treatment with large doses of exogenous androgens, including KYZATREX®, spermatogenesis may be suppressed through feedback inhibition of the hypothalamicpituitary-testicular axis [see [See Warnings and Precautions (5.7) and Impairment of Fertility (13.1) ] , possibly leading to adverse effects on semen parameters including sperm count. Reduced fertility has been observed in some men taking testosterone replacement therapy. Testicular atrophy, subfertility, and infertility have also been reported in men who abuse anabolic androgenic steroids [see Drug Abuse and Dependence (9.2) ].
With either type of use, the impact on fertility may be irreversible.
8.4Pediatric Use The safety and efficacy of KYZATREX® in pediatric patients less than 18 years old have not been established. KYZATREX® is not recommended for use in patients less than 18 years of age because of the potential for acceleration of bone age and premature closure of epiphyses.
8.5Geriatric Use Clinical studies of KYZATREX® did not include any patients 65 years of age and older. Therefore, it cannot be determined whether these patients respond differently from younger adult patients. Additionally, there are insufficient long-term safety data in geriatric patients to assess the potentially increased risk of cardiovascular disease and prostate cancer.
Geriatric patients treated with androgens including KYZATREX® may be at risk for worsening of signs and symptoms of BPH [see (see Warnings and Precautions (5.3)] .
🤰 Pregnancy ▾
8.1Pregnancy - Risk Summary KYZATREX® is contraindicated in pregnant women and not indicated for use in females [see Contraindications (4) ]. Testosterone is teratogenic and may cause fetal harm when administered to a pregnant woman based on data from animal studies (see Data ) and its mechanism of action [see Clinical Pharmacology (12.1) ]. Exposure of a female fetus to androgens may result in varying degrees of virilization.
In animal developmental studies, exposure to testosterone in utero resulted in hormonal and behavioral changes in offspring and structural impairments of reproductive tissues in female and male offspring. These studies do not meet current standards for nonclinical development toxicity studies. Data Animal Data In developmental studies conducted in rats, rabbits, pigs, sheep, and rhesus monkeys, pregnant animals received intramuscular injections of testosterone during the period of organogenesis.
Testosterone treatment at doses that were comparable to those used for testosterone replacement therapy resulted in structural impairments in both female and male offspring. Structural impairments observed in females included increased anogenital distance, phallus development, empty scrotum, no external vagina, intrauterine growth retardation, reduced ovarian reserve, and increased ovarian follicular recruitment. Structural impairments seen in male offspring included increased testicular weight, larger seminal tubular lumen diameter, and higher frequency of occluded tubule lumen.
Increased pituitary weight was seen in both sexes. Testosterone exposure in utero also resulted in hormonal and behavioral changes in offspring. Hypertension was observed in pregnant female rats and their offspring exposed to doses approximately twice those used for testosterone replacement therapy.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and efficacy of KYZATREX® in pediatric patients less than 18 years old have not been established. KYZATREX® is not recommended for use in patients less than 18 years of age because of the potential for acceleration of bone age and premature closure of epiphyses.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of KYZATREX® did not include any patients 65 years of age and older. Therefore, it cannot be determined whether these patients respond differently from younger adult patients. Additionally, there are insufficient long-term safety data in geriatric patients to assess the potentially increased risk of cardiovascular disease and prostate cancer.
Geriatric patients treated with androgens including KYZATREX® may be at risk for worsening of signs and symptoms of BPH [see (see Warnings and Precautions (5.3)] .
🆘 Overdosage ▾
10 OVERDOSAGE There is one report of acute overdosage with use of an approved injectable testosterone product: this subject had serum testosterone levels of up to 11,400 ng/dL with a cerebrovascular accident. Treatment of overdosage consists of discontinuation of KYZATREX® and appropriate symptomatic and supportive care.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY -
12.1Mechanism of Action Endogenous androgens, including testosterone and dihydrotestosterone (DHT), are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of prostate, seminal vesicles, penis, and scrotum; the development of male hair distribution, such as facial, pubic, chest, and axillary hair; laryngeal enlargement; vocal cord thickening; alterations in body musculature; and fat distribution.
Male hypogonadism, a clinical syndrome resulting from insufficient secretion of testosterone, has two main etiologies. Primary hypogonadism is caused by defects of the gonads, such as Klinefelter syndrome or Leydig cell aplasia, whereas secondary hypogonadism (also known as hypogonadotropic hypogonadism) is the failure of the hypothalamus (or pituitary gland) to produce sufficient gonadotropins (FSH, LH).
12.2Pharmacodynamics There is insufficient data to characterize an exposure-response relationship or time course of pharmacodynamics.
12.3Pharmacokinetics - Absorption KYZATREX® was taken orally at a starting dose of 200 mg twice per day with meals in a multicenter, open-label trial in hypogonadal males. The dose was adjusted, as needed, on Days 28 and 56 from a minimum dose of 100 mg (morning-only) to a maximum dose of 400 mg twice per day based on the plasma testosterone concentration obtained by a single blood draw collected 3 to 5 hours after the morning dose. The average daily NaF/EDTA plasma testosterone concentration was 393.3 (±113.6) ng/dL after 90 days of treatment (normal eugonadal range in NaF/EDTA plasma: 222-800 ng/dL.
Note that the titration scheme for use in clinical practice is based on serum total testosterone [see Dosage and Administration (2.2) ] . KYZATREX® is expected to produce testosterone concentrations that approximate normal concentrations seen in healthy men. Table 5 summarizes the pharmacokinetic (PK) parameters for plasma total testosterone in patients completing at least 90 days of KYZATREX® treatment administered daily.
Table 5: NaF-EDTA Plasma Testosterone C avg and C max at Day 90 Visit PK Parameter Plasma (N=130) PK = pharmacokinetic; C avg = 24-hour average concentration; C max = maximum concentration C avg (ng/dL) n 127 Mean 393.3 SD 113.6 C max (ng/dL) n 130 Mean 852.4 SD 311.3 Figure 2 summarizes the mean plasma total testosterone profile at the final PK visit. Figure 2: Mean (±SEM) Concentration-Time Profile for NaF-EDTA Plasma Total Testosterone in KYZATREX®-Treated Patients at Day 90 Visit SEM = standard error of the mean Testosterone normal ranges: plasma = 222-800 ng/dL When KYZATREX® was given with breakfast containing 16%, 33%, and 45% fat, the exposure (AUC 0-24 hr ) of testosterone was increased by 37%, 87%, and 94%, respectively, compared to when given under fasted conditions.
The primary efficacy and safety study was conducted under fed conditions regardless of the type of meals and the primary efficacy endpoint of achieving testosterone C avg in normal testosterone range was met. There was no effect on testosterone PK when KYZATREX® was administered with 20% alcohol along with a high-fat meal versus a high-fat meal alone. Figure 2 Distribution Circulating testosterone is primarily bound in serum to sex hormone-binding globulin (SHBG) and albumin.
Approximately 40% of testosterone in plasma is bound to SHBG, 2% remains unbound (free), and the rest is loosely bound to albumin and other proteins. Metabolism The androgenic activity of testosterone undecanoate occurs after the ester bond linking the testosterone to the undecanoic acid is cleaved by endogenous non-specific esterases. Undecanoic acid is metabolized like all fatty acids via the beta-oxidation pathway.
Testosterone is metabolized to various 17-keto steroids through two different pathways. The major active metabolites of testosterone are dihydrotestosterone (DHT) and estradiol…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Endogenous androgens, including testosterone and dihydrotestosterone (DHT), are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of prostate, seminal vesicles, penis, and scrotum; the development of male hair distribution, such as facial, pubic, chest, and axillary hair; laryngeal enlargement; vocal cord thickening; alterations in body musculature; and fat distribution.
Male hypogonadism, a clinical syndrome resulting from insufficient secretion of testosterone, has two main etiologies. Primary hypogonadism is caused by defects of the gonads, such as Klinefelter syndrome or Leydig cell aplasia, whereas secondary hypogonadism (also known as hypogonadotropic hypogonadism) is the failure of the hypothalamus (or pituitary gland) to produce sufficient gonadotropins (FSH, LH).
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING KYZATREX® capsules are available in four strengths of 50 mg, 100 mg, 150 mg, and 200 mg packaged as 30, 60, 90 and 120 units in wide-mouth, round, white HDPE bottles with white, polypropylene, child resistant caps and induction-sealed liner 50 mg: Oval, opaque, white cpasules imprinted with "MP50" in red ink; NDC 80603-107-44 for 30 capsules. 100 mg: Oval, opaque, white capsules imprinted with "MP100" in red ink supplied in bottles; NDC 80603-101-11 for 90 capsules and NDC 80603-101-22 for 120 capsules.
150 mg: Oblong, opaque, white capsules imprinted with "MP150" in red ink supplied in bottles; NDC 80603-103-11 for 90 capsules and NDC 80603-103-22 for 120 capsules. 200 mg: Oblong, opaque, white capsules imprinted with "MP200" in red ink supplied in bottles; NDC 80603-105-33 for 60 capsules , NDC 80603-105-11 for 90 capsules and NDC 80603-105-22 for 120 capsules . Store at 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
Store the capsules in a dry place avoiding exposure to excessive moisture and humid conditions. Dispose of unused KYZATREX® via a take-back option. If a take-back option is unavailable, follow FDA instructions at www.fda.gov/drugdisposal.
📦 Storage and Handling ▾
Store at 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Store the capsules in a dry place avoiding exposure to excessive moisture and humid conditions. Dispose of unused KYZATREX® via a take-back option. If a take-back option is unavailable, follow FDA instructions at www.fda.gov/drugdisposal.
📋 Description ▾
11 DESCRIPTION KYZATREX® is provided as a gelatin capsule containing testosterone undecanoate, a fatty-acid ester of testosterone. Testosterone undecanoate is a white to off-white yellow crystalline powder. Testosterone, an androgen, is formed by cleavage of the ester side chain of testosterone undecanoate.
Testosterone undecanoate is chemically described as 17β-hydroxyandrost-4-en-3-one undecanoate. It has the empirical formula of C 30 H 48 O 3 and a molecular weight of 456.7 g/mol. The structural formula for testosterone undecanoate is presented in Figure 1.
Figure 1: Testosterone Undecanoate KYZATREX® (testosterone undecanoate) capsules for oral use are available in four dosage strengths- 50 mg, 100 mg, 150 mg, and 200 mg. The 50 mg strength is an opaque, white capsule imprinted with "MP50" in red ink. The 100 mg strength is an opaque, white capsule imprinted with "MP100" in red ink.
The 150 mg strength is an opaque white capsule imprinted with "MP150" in red ink. The 200 mg strength is an opaque white capsule imprinted with "MP200" in red ink. All capsule strengths also contain DL-alpha-tocopheryl acetate (Vitamin E), phytosterol esters, polyoxyl 40 hydrogenated castor oil, and propylene glycol monolaurate as inactive ingredients.
Gelatin capsule shells are composed of the following inactive ingredients: gelatin, glycerin, purified water, sorbitol, and titanium dioxide. Figure 1
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Medication Guide). Polycythemia Advise patients that KYZATREX® can cause an increase in hemoglobin/hematocrit levels that may increase the risk of thromboembolic events. Advise patients about the importance of completing laboratory testing as instructed by their health care provider while on KYZATREX® [see Warnings and Precautions (5.1)] .
Venous Thromboebolisn Advise patients that KYZATREX® can cause venous thromboembolism. Advise patients of the signs and symptoms of venous thromboembolism, which may include the following: lower limb pain, edema, or erythema; and dyspnea or chest pain. Advise patients to promptly report the signs and symptoms of venous thromboembolism, discontinue use of KYZATREX® and seek urgent medical care.
Worsening of Benign Prostatic Hyperplasia (BPH) Advise patients that KYZATREX® can cause increased symptoms of BPH. Advise patients to contact their health care provider if they have any prostate-related symptoms [see Warnings and Precautions (5.3)] . Blood Pressure Increases Inform patients that KYZATREX® can increase blood pressure (BP) which can increase cardiovascular risk over time Instruct patients about the importance of monitoring BP periodically while on KYZATREX®.
If BP increases while on KYZATREX®, antihypertensive medications may need to be started, added, or adjusted to control BP, or KYZATREX® may need to be discontinued [see Warnings and Precautions (5.4)] Edema Advise patients that KYZATREX® can cause edema in patients with preexisting cardiac, renal, or hepatic disease. Advise patients to notify their health care provider if edema develops or worsens [see Warnings and Precautions (5.9)]. Sleep Apnea Advise patients that KYZATREX® can worsen sleep apnea especially in patients with risk factors such as obesity or chronic lung diseases ™ [see Warnings and Precautions (5.10)].
Gynecomastia Advise patients that KYZATREX® can cause gynecomastia [see Warnings and Precautions (5.11)]. Administration Instructions Advise patients to take KYZATREX® with food [see Dosage and Administration (2.3) ].
💬 Medication Guide ▾
MEDICATION GUIDE KYZATREX® (ky-ZAH-treks) (testosterone undecanoate) capsules, for oral use, CIII What is KYZATREX®? KYZATREX® is a prescription medicine that contains testosterone. KYZATREX® is used to treat adult men who have low or no testosterone due to certain medical conditions.
It is not known if KYZATREX® is safe or effective in children younger than 18 years old. Improper use of KYZATREX® may affect bone growth in children. KYZATREX® is a controlled substance (CIII) because it contains testosterone that can be a target for people who abuse prescription medicines.
Keep your KYZATREX® in a safe place to protect it. Never give your KYZATREX® to anyone else, even if they have the same symptoms you have. Selling or giving away this medicine may harm others and is against the law.
KYZATREX® is not meant for use by women. Do not take KYZATREX® if you: have breast cancer. have or might have prostate cancer. are a woman who is pregnant. KYZATREX may harm your unborn baby. are allergic to KYZATREX® or any ingredients in KYZATREX®.
See the end of this Medication Guide for a complete list of ingredients in KYZATREX®. Before you take KYZATREX®, tell your healthcare provider about all of your medical conditions, including if you: have high blood pressure or are being treated for high blood pressure. have a history of diabetes. have heart problems. have high red blood cell count (hematocrit) or high hemoglobin laboratory value. have urinary problems due to an enlarged prostate. have liver or kidney problems. have problems breathing while you sleep (sleep apnea).
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking KYZATREX® with certain other medicines can affect each other. Especially, tell your healthcare provider if you take: insulin medicines that decrease blood clotting (blood thinners) corticosteroids medicines that increase blood pressure such as some cold medicine and pain medicines Know the medicines you take.
Ask your healthcare provider or pharmacist for a list of these medicines, if you are not sure. Keep a list of them and show it to your healthcare provider and pharmacist when you get a new medicine. How should I take KYZATREX®?
Take KYZATREX® exactly as your healthcare provider tells you take it. Take KYZATREX® by mouth 2 times daily. Take 1 time in the morning and take 1 time in the evening.
If your dose is 100 mg daily, take 1 time in the morning. Take KYZATREX® with food. Your healthcare provider may change your KYZATREX® dose.
Do not change your KYZATREX® dose without talking to your healthcare provider. What are the possible side effects of KYZATREX®? KYZATREX® may cause serious side effects including: See “What is the most important information I should know about KYZATREX®?” Increase in red blood cell count (hematocrit) or hemoglobin. - KYZATREX® increases red blood cell counts in some patients.
High red blood cell counts increase the risk of blood clots, strokes, and heart attacks. - You may need to stop KYZATREX if your red blood cell count increases. - Your healthcare provider should check your red blood cell count and hemoglobin while you take KYZATREX®. If you already have an enlarged prostate, your signs and symptoms may worsen while taking KYZATREX®. These may include: - increased urination at night - trouble starting your urine stream - urinating many times during the day - urge to go to the bathroom right away - a urine accident - inability to pass urine or weak urine flow Increased risk of prostate cancer.
Your healthcare provider should check you for prostate cancer or any other prostate problems before you start and while you take KYZATREX®. Blood clots in the legs or lungs. Signs and symptoms of a blood clot in your leg can include pain, swelling or redness.
Signs and symptoms of a blood clot in your lungs can include difficulty breathing or chest pain. Increase in blood pressure. KYZATREX can…