| dbo:abstract |
Oprozomib (codenamed ONX 0912 and PR-047) is an orally active second-generation proteasome inhibitor developed by Proteolix, which was acquired by Onyx Pharmaceuticals, an Amgen subsidiary, in 2009. It selectively inhibits chymotrypsin-like activity of both the constitutive proteasome (PSMB5) and immunoproteasome (LMP7). It is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase 1b studies ongoing (as of February 16, 2016). Being an epoxyketone derivative, oprozomib is structurally related to carfilzomib and has the added benefit of being orally bioavailable. Like carfilzomib, it is active against bortezomib-resistant multiple myeloma cells. Oprozomib was granted orphan drug status for the treatment of Waldenström's macroglobulinaemia and multiple myeloma in 2014. (en) |
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935888-69-0 |
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2103884 |
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D10318 |
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25067547 |
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dbr:Carfilzomib dbr:Proteasome_inhibitor dbr:Bortezomib dbc:Proteasome_inhibitors dbr:Tumors_of_the_hematopoietic_and_lymphoid_tissues dbc:Epoxides dbr:Onyx_Pharmaceuticals dbr:Orphan_drug dbr:Multiple_myeloma dbc:Experimental_cancer_drugs dbc:Proteins dbr:Amgen dbc:Thiazoles dbr:Chymotrypsin dbr:Ixazomib dbr:PSMB8 dbr:Bioavailability dbr:Phases_of_clinical_research dbr:PSMB5 dbr:Waldenström's_macroglobulinaemia |
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N-[-3-methoxy-1-[[-3-methoxy-1-[[-1-[-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-methyl-1,3-thiazole-5-carboxamide (en) |
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Investigational drug (en) |
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Oral (en) |
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COC[C@H]CN[C@@H]C[C@@]3CO3 (en) |
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SWZXEVABPLUDIO-WSZYKNRRSA-N (en) |
| dbp:synonyms |
O-methyl-N--(L)-seryl-O-methyl-N-{-1-[-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl}-(L)-serinamide (en) |
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dbc:Proteasome_inhibitors dbc:Epoxides dbc:Experimental_cancer_drugs dbc:Proteins dbc:Thiazoles |
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owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment |
Oprozomib (codenamed ONX 0912 and PR-047) is an orally active second-generation proteasome inhibitor developed by Proteolix, which was acquired by Onyx Pharmaceuticals, an Amgen subsidiary, in 2009. It selectively inhibits chymotrypsin-like activity of both the constitutive proteasome (PSMB5) and immunoproteasome (LMP7). Oprozomib was granted orphan drug status for the treatment of Waldenström's macroglobulinaemia and multiple myeloma in 2014. (en) |
| rdfs:label |
Oprozomib (en) |
| owl:sameAs |
yago-res:Oprozomib wikidata:Oprozomib https://global.dbpedia.org/id/2Mp6Z |
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wikipedia-en:Oprozomib?oldid=981902702&ns=0 |
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wikipedia-en:Oprozomib |
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dbr:Proteasome_inhibitor |
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wikipedia-en:Oprozomib |
