TLANDO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TLANDO (TLANDO).
TLANDO (testosterone undecanoate) is an androgen that binds to and activates androgen receptors, leading to increased protein synthesis, muscle mass, bone density, and secondary sexual characteristics. Testosterone is converted to dihydrotestosterone (DHT) via 5α-reductase in target tissues, exerting both androgenic and anabolic effects.
| Metabolism | Testosterone undecanoate is metabolized primarily in the liver via esterases to release free testosterone. Testosterone is further metabolized via 5α-reductase to DHT and via aromatase to estradiol. The major pathway involves oxidation and glucuronidation; metabolites are excreted in urine and feces. |
| Excretion | Approximately 90% of a dose is excreted in urine as glucuronide and sulfate conjugates of testosterone and its metabolites; about 6% is excreted in feces via bile. Unchanged testosterone accounts for less than 1% of urinary excretion. |
| Half-life | The terminal elimination half-life of testosterone is 10-100 minutes; however, for TLANDO (testosterone undecanoate) after oral administration, the apparent half-life is approximately 7-10 hours due to the slow release from chylomicrons and prolonged absorption. |
| Protein binding | Testosterone is 98% bound in plasma, primarily to sex hormone-binding globulin (SHBG) and albumin. |
| Volume of Distribution | The apparent volume of distribution of testosterone is approximately 1.0 L/kg, indicating distribution into total body water and extensive tissue binding. |
| Bioavailability | Oral bioavailability of TLANDO is approximately 3-7% due to extensive first-pass metabolism; it is enhanced when taken with a fatty meal (up to 2-fold increase). |
| Onset of Action | After oral administration, serum testosterone levels begin to rise within 1-2 hours, with maximal concentrations achieved at 4-6 hours. Clinical effects (e.g., on libido, energy) may be observed within days to weeks. |
| Duration of Action | After a single oral dose of TLANDO, serum testosterone levels remain above baseline for approximately 24-48 hours. For replacement therapy, daily dosing maintains stable levels; clinical effects are sustained with continuous use. |
| Molecular Weight | 288.42 |
TLANDO (testosterone undecanoate) is administered orally. The recommended adult dose is 225 mg twice daily (approximately every 12 hours) with a meal containing fat. Swallow capsules whole; do not chew or crush.
| Dosage form | CAPSULE |
| Renal impairment | No specific dose adjustment provided by manufacturer. Use with caution in patients with severe renal impairment (eGFR <30 mL/min/1.73 m²) due to potential for fluid retention. Monitor serum testosterone levels and clinical response. |
| Liver impairment | Contraindicated in patients with Child-Pugh Class C (severe) hepatic impairment. For Child-Pugh Class A or B, initiate at 225 mg once daily and titrate based on serum testosterone levels. Monitor hepatic function closely. |
| Pediatric use | Not approved for use in pediatric patients (<18 years). Safety and efficacy not established. Testosterone therapy may cause premature epiphyseal closure and virilization. |
| Geriatric use | Patients >65 years may be at increased risk for adverse effects such as polycythemia, sleep apnea, and prostate-related events. Initiate at 225 mg once daily and titrate based on serum testosterone levels. Monitor hematocrit, prostate-specific antigen, and cardiovascular status. |
| 1st trimester | Contraindicated. Testosterone is associated with virilization of female fetuses. Risk of clitoromegaly, labial fusion, urogenital sinus abnormalities. |
| 2nd trimester | Contraindicated. Continued risk of fetal virilization. Potential for premature closure of epiphyseal plates. |
| 3rd trimester | Contraindicated. Risk of fetal virilization persists. Potential for premature epiphyseal closure and reduced birth weight. |
Clinical note
Comprehensive clinical and safety monograph for TLANDO (TLANDO).
| Placental transfer | Testosterone crosses the placenta. Evidence from animal studies and human cases demonstrates significant transfer leading to fetal exposure and concentration in fetal tissues. |
| Breastfeeding | Testosterone is excreted in breast milk in small amounts. However, potential for virilization or endocrine disruption in the infant. Generally considered contraindicated during breastfeeding. If used, monitor infant for signs of androgen excess. |
■ FDA Black Box Warning
WARNING: VENOUS THROMBOEMBOLISM, CARDIOVASCULAR RISK, AND BLOOD PRESSURE INCREASE. Androgens, including TLANDO, have been associated with increased risk of deep vein thrombosis (DVT) and pulmonary embolism (PE), major adverse cardiovascular events (MACE), and clinically significant increases in blood pressure that may require antihypertensive therapy. TLANDO should be used only in men with hypogonadal conditions confirmed by clinical and laboratory criteria.
| Serious Effects |
Hypersensitivity to testosterone or any component of TLANDOWomen who are or may become pregnantBreastfeeding womenMen with breast cancerMen with known or suspected prostate cancerSevere hepatic impairment
| Precautions | Cardiovascular risk: increased risk of MACE and venous thromboembolism, Blood pressure elevation: monitor blood pressure regularly, Polycythemia: increased hematocrit may require dose adjustment or discontinuation, Prostate cancer: possible worsening of existing prostate cancer; monitor prostate-specific antigen, Benign prostatic hyperplasia: may exacerbate urinary symptoms, Hepatic effects: rare cases of hepatic neoplasia; monitor liver function, Lipid profile changes: may decrease HDL and increase LDL, Gynecomastia: possible development or worsening, Sleep apnea: may worsen in predisposed patients, Fertility: may suppress spermatogenesis |
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| Lactation Rating | L5 |
| Teratogenic Risk | TLANDO (testosterone undecanoate) is contraindicated in pregnancy. Testosterone can cause virilization of the female fetus, particularly during the first trimester when external genitalia differentiation occurs. Exposure in the first trimester may result in clitoromegaly, labial fusion, and other ambiguous genitalia. Later exposure risk is lower but may still cause virilization. Use is not recommended at any gestational age. |
| Fetal Monitoring | Monitor maternal signs of virilization, excessive androgen effects, and liver function. If accidental exposure occurs during pregnancy, fetal ultrasound should be considered to assess genital development (e.g., ambiguous genitalia). No routine fetal monitoring is indicated; pregnancy should be avoided. |
| Fertility Effects | TLANDO may reversibly suppress spermatogenesis via negative feedback on gonadotropins (LH, FSH). Long-term use can lead to oligospermia or azoospermia, reducing male fertility. Women of reproductive potential should use effective contraception. Effects on female fertility are not well studied but may include menstrual irregularities. |
| Food/Dietary | Grapefruit and grapefruit juice may increase testosterone levels. Avoid excessive alcohol intake as it may decrease testosterone levels. High-fat meals may affect absorption; apply gel consistently relative to meals. |
| Clinical Pearls | Testosterone replacement therapy. Monitor serum testosterone levels 3-6 months after initiation. Contraindicated in men with breast cancer or suspected prostate cancer. May cause polycythemia; check hematocrit at baseline and periodically. Use with caution in patients with severe renal or hepatic impairment. Not indicated for age-related hypogonadism. |
| Patient Advice | Apply the gel once daily to clean, dry skin on the shoulders or upper arms. · Wash hands immediately after application. · Avoid showering or swimming for at least 2 hours after application. · Cover application site with clothing to prevent transfer to others. · Report signs of excessive testosterone: persistent erections, acne, swelling, or changes in mood. · Do not use in women or children. · Keep out of reach of children and pets. · May cause changes in lipid profile and red blood cell count. · May worsen sleep apnea. · Do not use if you have breast cancer or prostate cancer. |