Bexarotene
TARGRETIN
What it isSelective retinoid X-receptor agonist; cutaneous T-cell lymphoma.
Why this oneBoth oral capsules and a topical gel can treat cutaneous T-cell lymphoma, a formulation range unusual among retinoids.
What limits itCentral hypothyroidism and severe hypertriglyceridemia often need treatment from the outset; it is profoundly teratogenic.
FDA-approved for
- cutaneous T-cell lymphoma (1999)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Cutaneous T-cell lymphoma (CTCL) | Adults | 300 mg/m2/day | 300 mg/m2/day | 400 mg/m2/day (if no response at 8 wk and 300 tolerated) |
Titration May escalate to 400 mg/m2/day after 8 weeks if no tumor response and initial dose well tolerated
Renal Undefined
Hepatic Undefined
Dose calculated by body surface area (see label Table 1)
Instructions
- Take as a single daily dose with a meal
- Dose may reduced to 200 then 100 mg/m2/day, or suspended, for toxicity, then carefully readjusted upward
- Continue as long as patient derives benefit
Contraindications
- Pregnancy
Cautions
- Hyperlipidemia (marked triglyceride/cholesterol elevations) — monitor and manage
- Pancreatitis — interrupt if suspected
- Hepatotoxicity, cholestasis, hepatic failure
- Hypothyroidism — monitor, replace thyroid hormone
- Neutropenia
- Cataracts
- Photosensitivity
- Hypoglycemia risk with diabetes; avoid excess vitamin A
Adverse reactions
- Hyperlipidemia, hypercholesterolemia
- Headache, asthenia
- Hypothyroidism
- Leukopenia
- Rash, dry skin
- Nausea, abdominal pain
- Infection, peripheral edema
Pregnancy Contraindicated — teratogenic retinoid; must not be used in pregnancy
Lactation Undefined — no information on presence in human milk
⚠ BOXED WARNING
- Embryo-fetal toxicity
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2014
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Bexarotene ballicule
