Bexarotene - Warnings and Precautions
The following warnings and precautions are taken directly from the US FDA-approved drug label for Bexarotene. This is the same information dispensing pharmacists read.
\u26a0\ufe0f Boxed Warning (Highest FDA Alert)
WARNING: BIRTH DEFECTS Bexarotene is a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene also caused birth defects when administered orally to pregnant rats. Bexarotene must not be administered to a pregnant woman. WARNING: BIRTH DEFECTS See full prescribing information for complete boxed warning. Bexarotene is a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene also caused birth defects when administered orally to pregnant rats. Bexarotene must not be administered to a pregnant woman.
5 WARNINGS AND PRECAUTIONS • Hyperlipidemia: Bexarotene causes elevations in blood lipids.
Obtain baseline values, monitor, and manage elevations during therapy by dose reduction, interruption, discontinuation and/or lipid lowering therapy. ( 5.1 , 5.11 ) • Pancreatitis: Interrupt bexarotene and evaluate if suspected. • Hepatotoxicity, cholestasis, and hepatic failure: Interrupt or discontinue bexarotene and evaluate if liver chemistry tests exceed three times the upper limit of normal values. • Hypothyroidism: Bexarotene therapy can cause hypothyroidism.
Monitor and replace thyroid hormone if needed • Neutropenia: Monitor for neutropenia.
Reduce bexarotene dose or interrupt as indicated. • Photosensitivity: Minimize exposure to sunlight and artificial ultraviolet light during treatment.
5.1 Hyperlipidemia Bexarotene induces substantial elevations in lipids in most patients.
About 70% of patients with CTCL who received an initial dose of ≥300 mg/m 2 /day of bexarotene had fasting triglyceride levels greater than 2.5 times the upper limit of normal.
About 55% had values over 800 mg/dL with a median of about 1,200 mg/dL in those patients.
Cholesterol elevations above 300 mg/dL occurred in approximately 60% and 75% of patients with CTCL who received an initial dose of 300 mg/m 2 /day or greater than 300 mg/m 2 /day, respectively.
Decreases in high density lipoprotein (HDL) cholesterol to less than 25 mg/dL were seen in about 55% and 90% of patients receiving an initial dose of 300 mg/m 2 /day or greater than 300 mg/m 2 /day, respectively, of bexarotene.
Monitor lipid changes and treat abnormalities during therapy.
The effects on triglycerides, HDL cholesterol, and total cholesterol were reversible with cessation of therapy, and could generally be mitigated by dose reduction and/or concomitant antilipemic therapy.
Perform fasting blood lipid determinations before bexarotene therapy is initiated and weekly until the lipid response to bexarotene is established, which usually occurs within two to four weeks, and monitor at eight week intervals thereafter.
Fasting triglycerides should be normal or normalized with appropriate intervention prior to initiating bexarotene therapy.
Maintain triglyceride levels below 400 mg/dL to reduce the risk of clinical sequelae [ see Warnings and Precautions ].
If fasting triglycerides are elevated or become elevated during treatment, institute antilipemic therapy, and if necessary, reduce or interrupt the dose of bexarotene.
In the 300 mg/m 2 /day initial dose group, 60% of patients were given lipid lowering drugs.
Atorvastatin was used in 48% (73/152) of patients with CTCL.
Because of a potential drug-drug interaction, avoid gemfibrozil use with bexarotene [ see Drug Interactions ].
5.2 Pancreatitis Acute pancreatitis, including a fatal case, has been reported in four patients with CTCL and in six patients with non-CTCL cancers treated with bexarotene; the cases were associated with marked elevations of fasting serum triglycerides, the lowest being 770 mg/dL in one patient.
One patient with advanced non‑CTCL cancer died of pancreatitis.
Interrupt bexarotene and evaluate if pancreatitis is suspected.
Patients with CTCL who have risk factors for pancreatitis (e.g., prior pancreatitis, uncontrolled hyperlipidemia, excessive alcohol consumption, uncontrolled diabetes mellitus, biliary tract disease, and medications known to increase triglyceride levels or to be associated with pancreatic toxicity) may be at greater risk for pancreatitis associated with bexarotene [ see Warnings and Precautions ].
5.3 Hepatotoxicity, cholestasis, and hepatic failure Bexarotene caused elevations in liver chemistry tests (LFTs) in 5% (AST), 2% (ALT), and 0% (bilirubin) in patients with CTCL receiving an initial dose of 300 mg/m 2 /day.
In contrast, with an initial dose greater than 300 mg/m 2 /day of bexarotene, the incidence of LFT elevations was higher at 7% (SGOT/AST), 9% (SGPT/ALT), and 6% (bilirubin).
Two patients developed cholestasis, including one patient who died of liver failure.
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