Research ArticleDrug Development

A potent peptide-steroid conjugate accumulates in cartilage and reverses arthritis without evidence of systemic corticosteroid exposure

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Science Translational Medicine  04 Mar 2020:
Vol. 12, Issue 533, eaay1041
DOI: 10.1126/scitranslmed.aay1041

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Peptide targeting prevents toxicity

Treatments that target anti-arthritic drugs to joints can help avoid systemic toxicity. Cook Sangar et al. identified a cystine-dense peptide that accumulates in cartilage. Imaging agents conjugated to the peptide distributed to cartilage in rodents when delivered systemically and bound to human cartilage explants ex vivo. Conjugating the steroid triamcinolone acetonide to the peptide alleviated inflammation in the joints of a rat model of collagen-induced rheumatoid arthritis without systemic toxicity, suggesting that the conjugate could have potential joint-targeting therapeutic utility.

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