Multidisciplinary Cutaneous Lymphoma Group

Patient on Targretin®

Information for the Physician

We have recommended oral Targretin® therapy for your patient. Targretin® (bexarotene) is a retinoid medication that is approved for the treatment of Cutaneous T-cell Lymphoma (CTCL). It is supplied as 75 mg capsules which should be taken with a meal (dinner is usually preferred). The recommended dose is 200-300mg/m 2 /day. At Stanford, we recommend starting at a dose of 150-300mg daily and increasing the dose by 75-150 mg every 1-2 weeks as tolerated until the maximum desired dose of 200-300 mg/m2/day is attained. Of note, the maximum desired dose is dependent on severity of disease and other medical conditions, for example renal insufficiency, hepatic insufficiency, diabetes mellitus, a history of hypertriglyceridemia or pancreatitis , and the concurrent use cytochrome P450 inhibitors or inducers.

Targretin® use is commonly associated with reversible hypertriglyceridemia and centrally-induced hypothyroidism. Thus, baseline fasting lipids and free T4 levels should be obtained prior to initiating therapy with Targretin®. At Stanford, we suggest prophylactically treating patients with an anti- lipemic medication and thyroid hormone replacement starting 7-10 days prior to initiating treatment with Targretin®. The anti- lipemic medications that are most effective for hypertriglycerdemia are atorvastatin ( Lipitor®) and fenofibrate ( Tricor®). Anti- lipemic medication doses should be increased and maximized as needed. Atorvastatin and fenofibrate use may be combined; however, their concurrent use warrants cautious monitoring due to a potential risk of myopathy and rhabdomyolysis with renal failure.

GEMFIBROZIL (LOPID ®) USE IS CONTRAINDICATED WITH TARGRETIN © USE due to elevated Targretin® levels and extremely high triglyceride levels.

Levothyroxine should be started at a dose of 50 mcg daily and the dose adjusted as needed. Of note, free T4, not TSH , should be monitored since the hypothyroidism associated with Targretin® use is centrally-induced.

Less commonly, reversible cytopenias (mostly leukopenia ) and liver function test abnormalities can be seen. Rare cases of acute pancreatitis have also been reported in association with marked elevations of fasting serum triglycerides.

Monitoring and adjusting Targretin® after initiation involves careful monitoring by the prescribing physician. Blood tests including fasting lipids, free T4, LFTs , and CBC should be obtained prior to initiating any therapy. After starting therapy with Targretin® , fasting lipids levels should be checked weekly and LFTs should be checked every 4 weeks. A CBC and free T4 should be checked 4 weeks after starting Targretin® . Once the lab values stabilize and maximum medication doses are achieved, fasting lipid levels should be checked monthly and free T4, LFTs , and CBC should be checked every 1-2 months. If the triglyceride level is above 600 mg/ mL , we recommend suspending the Targretin® for 7 days and maximizing the anti- lipemic medications. After normalization of lipid levels to a reasonable range (varies depending on patient's concurrent medical conditions), restart the Targretin® at half the suspended dose and then increase the dose incrementally as described above. After any change in the Targretin® dose, check the fasting lipids weekly for 4 weeks until they stabilize and then monthly as described above.

The development of new cataracts or the worsening of previous cataracts is rare, but a potential risk associated with the use of Targretin® . We recommend an ophthalmologic evaluation prior to initiating therapy and then periodically during therapy or if the patient develops visual difficulties.

TARGRETIN ® IS CATEGORY X. PREGNANCY IS A CONTRAINDICATION.

The most common symptomatic side effects reported are fatigue/lethargy, headache, asthenia, rash, nausea, abdominal pain, infection, peripheral edema and dry skin.

Please review the package insert for Targretin® capsules.

Feel free to contact us with any questions or concerns.

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