bexarotene (Targretin)
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Indications
- treatment of cutaneous T cell lymphoma
- used off-label for lung cancer, breast cancer, & Kaposi's sarcoma
Contraindications
Dosage
Capsules: 75 mg
Adverse effects
Mechanism of action
- binds retinoid X receptors subtypes (RXR-alpha, RXR-beta, RXR-gamma).
- stimulates production of apoE
Clinical trials
- phase 2A proof-of-concept clinical trial at Cleveland clinic Dec 2013, to treat patients with Alzheimer's disease (BEAT-AD)[5]
Comparative biology
- in transgenic mice overexpressing beta-amyloid, bexarotene
- increases expression of apoE in the brain
- reduces beta-amyloid (both soluble & in plaques)
- reverses cognitive impairment & loss of behavioral skills
More general terms
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: https://www.ncbi.nlm.nih.gov/pubmed/22323736
Strittmatter WJ. Old drug, new hope for Alzheimer's disease. Science 2012 Mar 23; 335:1447. PMID: https://www.ncbi.nlm.nih.gov/pubmed/22442467 - ↑ 5.0 5.1 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
- ↑ 6.0 6.1 Targretin <TM> (bexarotene) capsules, 75 mg http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021055s006lbl.pdf