Dosing & Uses
Dosage Forms & Strengths
capsule
- 75mg
gel
- 1%
Cutaneous T-Cell Lymphoma
300 mg/m² PO qDay with food; titrate based on response or toxicity; may increase to 400 mg/m²/day if no response after 8 weeks of therapy
Topical: Apply to lesions every other day for 1 week initially, THEN increase qWeek up to q6hr
Monitor: WBC, LFTs, lipids, thyroid function
Refractory Mycosis Fungoides/Sezary Syndrome (Off-label)
75-150 mg PO qDay in combination with PUVA; not to exceed 300 mg/day
Renal Impairment
Not studied; use caution
Hepatic Impairment
Not studied; use caution
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Oral (CTCL trial)
- Peripheral edema (11-13%)
- Headache (30-42%), fever (5-17%), chills (10-13%), insomnia (5-11%)
- Exfoliative dermatitis (10-28%), rash (16-23%), alopecia (4-12%), dry skin (10-11%)
- Diarrhea (7-41%), nausea (8-16%), vomiting (4-13%), abdominal pain (4-11%)
- Bacterial infection (1-13%), flu syndrome (4-13%), infections (13-23%)
- Leukopenia (17-47%), anemia (6-25%), lactic dehydrogenase increased (7-13%), hypochromic anemia (4-13%)
- Hyperlipidemia (78-79%), hypercholesteremia (32-62%), hypothyroidism (29-52%)
- Back pain (2-11%)
Topical
- Rash (72%)
- Pruritus (36%)
- Pain (30%)
- Infection (18%)
- Contact dermatitis (14%)
- Headache (14%)
1-10%
Oral
- Hemorrhage
- Hypertension
- Hypothyroidism
- Heart failure
- Tachycardia
- Acne
- Depression
- Pustular rash
- Sunburn
- Pharyngitis
- Rhinitis
- Arthralgia
- Blephartis
- Corneal lesion
- Renal dysfunction
Topical
- Edema (10%)
- Hyperlipemia (10%)
- Asthenia (6%)
- Exfoliative dermatitis (6%)
- Leukopenia (6%), lymphadenopathy (6%), WBC changes (6%)
- Cough increased (6%), pharyngitis (6%)
- Sweating (6%)
Warnings
Black Box Warnings
Bexarotene is a retinoid
Retinoids are associated with birth control defects in humans and are contraindicated during pregnancy
Effective contraception must be in place 1 month before initiation of therapy, during therapy, and for at least 1 month after discontinuation of therapy
Contraindications
Hypersensitivity to retinoids
Pregnancy (use 2 forms of contraception)
Cautions
Oral
- Suppresses TSH levels; may cause hypothyroidism; may require supplementatoin
- Neutropenia and leukopenia may occur
- May induce significant lipid abnormalities in a majority of patients
- ALT, AST, and bilirubin elevation reported
- Pancreatitis secondary to hypertriglyceridemia reported
- Photosensitivity and phototoxicity may occur
- Evaluate visual abnormalities experienced by patient
- Use caution in diabetes mellitus and hepatic impairment
Topical
- Do not use occlusive dressings with gel
- May induce significant lipid abnormalities; use caution in patients with hypertriglyceridemia
- May cause photosensitization
- Neutropenia and leukopenia may occur
Pregnancy & Lactation
Pregnancy Category: X
Lactation: It is not known whether bexarotene is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from bexarotene, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Retinoid X receptor activator, regulates genes that control cell differentiation; induces tumor regression
Pharmacokinetics
Half-Life: 7 hr
Peak Plasma Time: 2 hr
Protein Bound: >99%
Metabolism: Liver (CYP3A4)
Metabolites: 6- & 7- hydroxy- bexarotene, 6- & 7- oxo- bexarotene
Excretion: Feces (primarily); urine (<1%)
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
