Alvocidib: Difference between revisions
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== Alvocidib == | == Alvocidib == | ||
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Revision as of 19:02, 16 March 2025
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Alvocidib (INN; also known as Flavopiridol) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia, by Tolero Pharmaceuticals, Inc. It has been studied also for the treatment of arthritis<ref name="pmid18209094">,
Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors, J. Immunol., 2008, Vol. 180(Issue: 3), pp. 1954–61, DOI: 10.4049/jimmunol.180.3.1954, PMID: 18209094,</ref> and atherosclerotic plaque formation<ref name="pmid10441105">, Flavopiridol inhibits smooth muscle cell proliferation in vitro and neointimal formation In vivo after carotid injury in the rat, Circulation, 1999, Vol. 100(Issue: 6), pp. 659–65, DOI: 10.1161/01.cir.100.6.659, PMID: 10441105,</ref> The target of Flavopiridol is the positive transcription elongation factor P-TEFb.<ref name="pmid10906320">, Flavopiridol inhibits P-TEFb and blocks HIV-1 replication, J. Biol. Chem., 2000, Vol. 275(Issue: 37), pp. 28345–8, DOI: 10.1074/jbc.C000446200, PMID: 10906320,</ref><ref name="pmid11431468">, Flavopiridol inactivates P-TEFb and blocks most RNA polymerase II transcription in vivo, J. Biol. Chem., 2001, Vol. 276(Issue: 34), pp. 31793–9, DOI: 10.1074/jbc.M102306200, PMID: 11431468,</ref> Treatment of cells with Flavopiridol leads to inhibition of P-TEFb and the loss of mRNA production.<ref name="pmid22244331">, Functional association of Gdown1 with RNA polymerase II poised on human genes, Mol. Cell, 2012, Vol. 45(Issue: 1), pp. 38–50, DOI: 10.1016/j.molcel.2011.10.022, PMID: 22244331, PMC: 3259526,</ref><ref name="pmid20434984">, c-Myc regulates transcriptional pause release, Cell, 2010, Vol. 141(Issue: 3), pp. 432–45, DOI: 10.1016/j.cell.2010.03.030, PMID: 20434984, PMC: 2864022,</ref>
The compound is a synthetic analog of natural product rohitukine which was initially extracted from Amoora rohituka [syn. Aphanamixis polystachya] and later from Dysoxylum binectariferum.<ref>,
The structure of rohitukine, the main alkaloid of Amoora rohituka (syn.Aphanamixis polystachya) (Meliaceae), Tetrahedron Lett., Vol. 20(Issue: 1), pp. 721–724, DOI: 10.1016/S0040-4039(01)93556-7,</ref><ref>, Immunopharmacological potential of rohitukine: a novel compound isolated from the plant Dysoxylum binectariferum, Asia Pac J Pharmcol., Vol. 3(Issue: 1), pp. 91–98,</ref>
Orphan drug
Tolero Pharmaceuticals Inc. announced that the FDA has granted orphan drug designation for Alvocidib, its cyclin-dependent kinase small molecule inhibitor, for the treatment of patients with acute myeloid leukemia.<ref>http://www.healio.com/hematology-oncology/hematologic-malignancies/news/online/%7B74c6a69e-4529-400d-98e9-d5ee6c602122%7D/fda-grants-orphan-drug-status-to-alvocidib-for-aml</ref>
References
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