Tlando (testosterone undecanoate) drug profile, 2024?

Tlando® (testosterone undecanoate) – 2024 Drug Profile

Drug class:

• Anabolic–androgenic steroid (AAS)
• Long‑acting testosterone ester

Manufacturer:

• T. – “Tlando” (formerly T-Health; see FDA drug code 2051)

Formulation & Strength:

• Injectable oil suspension (ethanol–propylene glycol vehicle)
• 200 mg/mL testosterone undecanoate
• 1 mL vial (200 mg)

Routes of Administration:

• Intramuscular (IM) injection (gluteal or ventro‑lateral thigh)

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1. Indications

Indication	Approved Dose & Schedule	Key Points
Hypogonadal men (low endogenous testosterone)	Initial: 200 mg IM × 2 weeks (or 1 month per manufacturer guidance) Maintenance: 200 mg IM every 4 weeks (≈6 months)	• Effective in restoring serum testosterone to mid‑normal range (≈250–800 ng/dL). • Must be used under supervision of a qualified clinician.
Gender‑affirming hormone therapy (female-to-male)	Initiation: 200 mg IM 2 weeks apart (2–4 weeks) Maintenance: 200 mg IM every 4 weeks	• Testosterone undecanoate provides sustained masculinization with minimal peaks.
Atypical or off‑label uses	No official approval	• Off‑label use (e.g., for athletic performance enhancement, muscle building) is discouraged due to safety concerns and regulatory restrictions.

Note: In 2024, Tlando remains FDA‑approved only for the above indications. The European Medicines Agency (EMA) has not granted a marketing authorization for any testosterone undecanoate product; physicians in the EU must rely on alternative preparations (e.g., testosterone enanthate, cypionate).

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2. Mechanism of Action

• Testosterone undecanoate is a long‑acting ester of testosterone.
• After IM injection, the ester is hydrolyzed slowly by plasma esterases, releasing free testosterone over ~4–5 weeks.
• Free testosterone binds to the androgen receptor (AR) in target tissues (muscle, bone, prostate, CNS) to modulate gene transcription and protein synthesis.

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3. Pharmacokinetics (average values for 200 mg dose)

Parameter	Value (approx.)	Comments
Cmax	3–5 ng/mL (≈10–20 nmol/L)	Occurs ~4–7 days post‑dose.
Tmax	4–7 days	Due to slow ester hydrolysis.
Half‑life (t½)	4–5 weeks	Reflects depot release rather than testosterone clearance.
AUC (0–∞)	~100 ng·day/mL	Linear with dose.
Protein binding	> 99 % to albumin and SHBG	Saturation may occur with high doses.
Metabolism	Primarily hepatic aromatization (to estradiol) and 5α‑reduction (to dihydrotestosterone).
Excretion	Urine (conjugates) and feces (bile‑excretion).

Drug–Drug Interaction (DDI) Potential:
• Enzyme induction (CYP3A4) or inhibition can alter testosterone levels.
• Aromatase inhibitors (e.g., anastrozole) reduce estradiol conversion; may increase testosterone concentration.
• CYP3A4 inducers (e.g., rifampin, carbamazepine) may lower testosterone levels; consider dose adjustment.

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4. Dosage & Administration

Population	Starting Dose	Maintenance Dose	Titration Notes
Hypogonadal men	200 mg IM 2 weeks apart	200 mg IM every 4 weeks	• Evaluate serum testosterone 2–4 weeks after the second injection. • Adjust dose (e.g., 400 mg or 300 mg) if levels remain sub‑therapeutic (<250 ng/dL).
Gender‑affirming therapy	200 mg IM 2 weeks apart (2–4 weeks)	200 mg IM every 4 weeks	• Monitor feminizing signs (e.g., breast size, body composition). • Adjust per patient response.
Pregnancy/lactation	Contraindicated	N/A	• Testosterone can cross placenta; avoid during pregnancy.
Elderly or hepatic impairment	Start 200 mg IM 2 weeks apart	200 mg IM every 6 weeks (optional)	• Monitor liver enzymes and testosterone levels closely.

Administration Technique
• Use a 22‑24 gauge needle and a 1‑2 mL syringe.
• Inject into the gluteus maximus or vastus lateralis.
• Rotate sites to minimize injection site reactions.

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5. Contraindications

Category	Specifics
Known hypersensitivity	To testosterone, undecanoate ester, or any excipient.
Active prostate or breast cancer	Testosterone can stimulate hormone‑responsive tumors.
Uncontrolled hypertension	Testosterone may worsen blood pressure.
History of thromboembolic disease	Testosterone can increase coagulability.
Untreated sleep apnea	Testosterone may worsen apnoea.
Pregnancy/Lactation	Testosterone crosses the placenta; avoid.

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6. Precautions & Monitoring

Parameter	Monitoring Frequency	Target	Notes
Serum total testosterone	2–4 weeks after 2nd dose, then every 6–8 weeks	300–800 ng/dL	Adjust dose to stay within this range.
Prostate‑specific antigen (PSA)	Every 6–12 months (men > 50 yr)	≤ 4 ng/mL	Monitor for prostate pathology.
Liver function tests	Every 3–6 months	AST/ALT ≤ 2 × ULN	Avoid in severe hepatic disease.
Hemoglobin/hematocrit	Every 3–6 months	Hematocrit ≤ 50 % (men)	Red blood cell count can rise; watch for polycythemia.
Blood pressure	Every visit	< 140/90 mmHg	Treat hypertension as needed.
Lipid profile	Every 6–12 months	LDL < 130 mg/dL	Testosterone may modestly worsen lipids.
Estradiol	Optional	< 40 pg/mL	May guide aromatase inhibitor use.
Signs of androgen excess	Every visit	N/A	Monitor acne, hirsutism, voice changes.

Important: Do not exceed 400 mg/IM if serum testosterone > 800 ng/dL to avoid supraphysiologic levels.

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7. Adverse Reactions (Common ≥ 5 %, Rare < 1 %)

System	Typical Symptoms	Management
Endocrine	Acne, oily skin, hirsutism, gynecomastia (in females)	Topical retinoids, anti‑androgens, consider dose reduction.
Hematologic	Polycythemia, erythrocytosis	Phlebotomy, reduce dose, or stop therapy.
Cardiovascular	Elevated blood pressure, edema	Monitor BP, consider antihypertensives.
Psychiatric	Mood swings, aggression, insomnia	Counsel, consider dose adjustment.
Gastro‑intestinal	Injection site pain, myalgias	Warm compress, rotate sites.
Reproductive	Decreased sperm count, infertility (male)	Discuss fertility desires; may need sperm banking.
Liver	Elevated transaminases	Monitor LFTs; stop if > 3 × ULN.
Allergic	Rash, anaphylaxis (rare)	Discontinue, treat with antihistamines/epinephrine.

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8. Drug Interactions

| Drug/Agent | Interaction Type | Clinical Impact | Mitigation |