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bexarotene (Targretin)
Indications:
- treatment of cutaneous T cell lymphoma
- used off-label for lung cancer, breast cancer, & Kaposi's sarcoma
Contraindications:
- pregnancy category X
Dosage:
- oral agent
Capsules: 75 mg
Adverse effects:
- dyslipidemia:
- hypercholesterolemia
- hypertriglyceridemia
- pancreatitis
- hypothyroidism
- hepatotoxicity
- leukopenia
- cataracts [6]
Mechanism of action:
- binds retinoid X receptors subtypes (RXR-alpha, RXR-beta, RXR-gamma).
- stimulates production of apoE
Comparative biology:
- in transgenic mice overexpressing beta-amyloid, bexarotene
a) increases expression of apoE in the brain
b) reduces beta-amyloid (both soluble & in plaques)
c) reverses cognitive impairment & loss of behavioral skills
Clinical trials:
- phase 2A proof-of-concept clinical trial at Cleveland clinic Dec 2013, to treat patients with Alzheimer's disease (BEAT-AD) [5]
General
antineoplastic agent (chemotherapeutic agent)
dermatologic agent
References
- PubMed Health: Bexarotene
http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000433/
- National Cancer Institute: Bexarotene
http://www.cancer.gov/cancertopics/druginfo/bexarotene
- Wikipedia: Bexarotene
http://en.wikipedia.org/wiki/Bexarotene
- Cramer PE et al.
ApoE-directed therapeutics rapidly clear beta-amyloid and
reverse deficits in AD mouse models.
Science 2012 Mar 23; 335:1503
PMID: 22323736
- Strittmatter WJ.
Old drug, new hope for Alzheimer's disease.
Science 2012 Mar 23; 335:1447.
PMID: 22442467
- Cummings JL and Zhong K
Beraxotene for Alzheimer's disease: Innovative Clinical Trial
Could Open the Door to Disease-Modifying Therapy.
Cleveland Clinic: Neurosciences Pathways.
CLEVELANDCLINIC.ORG/NEUROSCIENCE
- Targretin (bexarotene) capsules, 75 mg
http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021055s006lbl.pdf