Bexarotene

TARGRETIN

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Pronunciation: bex-AIR-oe-teen (tar-GRET-in)

Bexarotene ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Bexarotene ballicule

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.

Bexarotene molecular structure (skeletal formula) — Molecular structure: Bexarotene

FDA-approved for

cutaneous T-cell lymphoma (1999)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Birth defects: bexarotene is a retinoid associated with birth defects in humans; must not be given to a pregnant woman

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

Available strengths

cap 75 mg
gel 1 %

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

Cost

Bexarotene (TARGRETIN)

Strength		#/mo	generic $/unit	CostPlus
75 mg	cap	per unit		offered
1 %	gel	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Bexarotene is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2014

⚠ BOXED WARNING

Embryo-fetal toxicity

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk4 / 4

Legacy pregnancy categoryX

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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