Kyzatrex
(Testosterone Undecanoate)Kyzatrex Prescribing Information
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.
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Capsules:
- 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
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KYZATREX® is contraindicated in:
- Patients with carcinoma of the breast or known or suspected carcinoma of the prostate [see.]
5.4 Blood Pressure IncreasesKYZATREX® can increase blood pressure. Based on ambulatory blood monitoring in Study MRS-TU-2019EXT, KYZATREX® increased mean systolic/diastolic blood pressure by 1.7/0.6 mm Hg from baseline after 4 months of treatment and 1.8/0.6 mm Hg from baseline after 6 months of treatment
[see Adverse Reactions(6.1)]. In patients with hypertension on antihypertensive therapy, KYZATREX® increased the mean systolic/diastolic BP by 3.4/0.7 mm Hg from baseline after 4 months of treatment and 3.1/1.0 mm Hg from baseline after 6 months of treatment.[see Adverse Reactions(6.1)].Blood pressure increases can increase cardiovascular (CV) risk over time.The CV risk associated with topical testosterone gel was evaluated in TRAVERSE, a randomized, double-blind, placebo controlled, CV outcomes study in men with a history of CV disease or multiple CV risk factors. In TRAVERSE, topical testosterone gel increased mean systolic blood pressure by 1.0 mm Hg from baseline to 36 months, whereas a mean decrease from baseline of 0.5 mm Hg. However, the incidences of major adverse cardiovascular events (MACE), including cardiovascular death, non-fatal myocardial infarction [MI] and non-fatal stroke, were similar between treatment groups (7% for topical testosterone gel vs 7.3% for placebo)
[See Adverse Reactions(6.1)]Monitor BP periodically in men using KYZATREX®, especially men with hypertension. KYZATREX® is not recommended for use in patients with uncontrolled hypertension.
- Women who are pregnant. Testosterone can cause virilization of the female fetus when administered to a pregnant woman [ see].
8.1 Pregnancy-
Risk SummaryKYZATREX® 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.DataAnimal DataIn 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.
- Patients with known hypersensitivity to KYZATREX® or any of its ingredients [see.]
11 DESCRIPTIONKYZATREX® 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 C30H48O3and a molecular weight of 456.7 g/mol. The structural formula for testosterone undecanoate is presented in Figure 1.
Figure 1: Testosterone UndecanoateKYZATREX® (testosterone undecanoate) capsules for oral use are available in three dosage strengths- 100 mg, 150 mg, and 200 mg. 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
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