Pegaspargase

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Information about Pegaspargase

Bexarotene is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL). 

Liver safety of Pegaspargase

Bexarotene therapy is associated with a high rate of serum enzyme elevations and rare instances of clinically apparent acute liver injury

Mechanism of action of Pegaspargase

Bexarotene (bex ar' oh teen) is a synthetic retinoid analogue and antineoplastic agent that acts through engagement of the retinoid receptors to regulate genes involved in cellular differentiation and growth.  Bexarotene is considered a third generation retinoid because it has vitamin A-like activities, but is designed to optimize binding to retinoid X receptors (RXRs) which typically lead to malignant cell apoptosis as opposed to retinoic acid receptors (RARs) which affect cellular differentiation and cell growth.  Bexarotene has potent activity on tumor cell lines and has been shown to induce partial or complete remissions in up to half of patients with cutaneous T cell lymphoma (CTCL) refractory to standard therapy. 

FDA approval information for Pegaspargase

Bexarotene was approved for use in CTCL in 2000 and remains a second line therapy for the cutaneous manifestations of this form of lymphoma.  Bexarotene is available as capsules of 75 mg under the brand name Targretin.  The recommended dosage is 300 mg/m2 daily.

Side effects of Pegaspargase

Common side effects include hyperlipidemia, headache, weakness, leukopenia, anemia, infection, dry skin, rash and photosensitivity.  Rare, but severe adverse events include cataracts, neutropenia, hypothyroidism, pancreatitis and hepatitis.  Bexarotene, like other retinoids, is teratogenic and contraindicated during pregnancy and in women who are unable to practice adequate methods of birth control.

 

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