Chemistry:Halofuginone
 | |
 | |
| Clinical data | |
|---|---|
| Trade names | Halocur |
| AHFS/Drugs.com | International Drug Names |
| ATCvet code | |
| Legal status | |
| Legal status |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C16H17BrClN3O3 |
| Molar mass | 414.68 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
  (what is this?) (verify) | |
Halofuginone, sold under the brand name Halocur, is a coccidiostat used in veterinary medicine. It is a synthetic halogenated derivative of febrifugine, a natural quinazolinone alkaloid which can be found in the Chinese herb Dichroa febrifuga (Chang Shan).[1] Collgard Biopharmaceuticals is developing halofuginone for the treatment of scleroderma and it has received orphan drug designation from the U.S. Food and Drug Administration.[2]
Halofuginone inhibits the development of T helper 17 cells, immune cells that play an important role in autoimmune disease, but it does not affect other kinds of T cells which are involved in normal immune function.[3] Halofuginone therefore has potential for the treatment of autoimmune disorders.[4]
Halofuginone is also an inhibitor of collagen type I gene expression and as a consequence it may inhibit tumor cell growth.[1] Halofuginone exerts its effects by acting as a high affinity inhibitor of the enzyme glutamyl-prolyl tRNA synthetase. Inhibition of prolyl tRNA charging leads to the accumulation of uncharged prolyl tRNAs, which serve as a signal to initiate the amino acid starvation response, which in turn exerts anti-inflammatory and anti-fibrotic effects.[5]
References
- ↑ 1.0 1.1 "Halofuginone hydrobromide". NCI Drug Dictionary. National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services. http://www.cancer.gov/drugdictionary/?CdrID=38485.
- ↑ "Halofuginone Receives FDA Orphan Drug Status For Scleroderma". WebCite. 10 March 2000. http://www.pslgroup.com/dg/18dff6.htm.
- ↑ "Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response". Science 324 (5932): 1334–8. June 2009. doi:10.1126/science.1172638. PMID 19498172. Bibcode: 2009Sci...324.1334S.
- ↑ "Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response". Science 324 (5932): 1334–8. June 2009. doi:10.1126/science.1172638. PMID 19498172. Bibcode: 2009Sci...324.1334S.
- "A new lead for autoimmune disease". EurekAlert! (Press release). 4 June 2009.
- ↑ "Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase". Nature Chemical Biology 8 (3): 311–7. February 2012. doi:10.1038/nchembio.790. PMID 22327401.
 |  |
