Movatterモバイル変換

[0]ホーム
URL:

Jump to content
WikipediaThe Free Encyclopedia
Search

Oprozomib

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Oprozomib
Clinical data
Pronunciation/oʊˈprɒzoʊmɪb/oh-PROZ-oh-mib
Other namesO-methyl-N-(2-methyl-1,3-thiazol-5-carbonyl)-L-seryl-O-methyl-N-{(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl}-L-serinamide
Routes of
administration		Oral
ATC code
  • None
Legal status
Legal status
  • Investigational drug
Identifiers
  • N-[(2S)-3-methoxy-1-[[(2S)-3-methoxy-1-[[(2S)-1-[(2R)-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
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC25H32N4O7S
Molar mass532.61 g·mol−1
3D model (JSmol)
  • COC[C@H](NC(=O)[C@H](COC)NC(=O)c1cnc(C)s1)C(=O)N[C@@H](Cc2ccccc2)C(=O)[C@@]3(C)CO3
  • InChI=1S/C25H32N4O7S/c1-15-26-11-20(37-15)24(33)29-19(13-35-4)23(32)28-18(12-34-3)22(31)27-17(21(30)25(2)14-36-25)10-16-8-6-5-7-9-16/h5-9,11,17-19H,10,12-14H2,1-4H3,(H,27,31)(H,28,32)(H,29,33)/t17-,18-,19-,25+/m0/s1
  • Key:SWZXEVABPLUDIO-WSZYKNRRSA-N

Oprozomib[1] (codenamedONX 0912 andPR-047) is an orally active second-generationproteasome inhibitor developed by Proteolix, which was acquired byOnyx Pharmaceuticals, anAmgen subsidiary, in 2009. It selectively inhibitschymotrypsin-like activity of both the constitutive proteasome (PSMB5) and immunoproteasome (LMP7).[2]

It is being investigated for the treatment ofhematologic malignancies, specifically,multiple myeloma, withPhase 1b studies ongoing (as of February 16, 2016).[3] Being an epoxyketone derivative, oprozomib is structurally related tocarfilzomib and has the added benefit of being orallybioavailable. Like carfilzomib, it is active againstbortezomib-resistant multiple myeloma cells.[4]

Oprozomib was grantedorphan drug status for the treatment ofWaldenström's macroglobulinaemia andmultiple myeloma in 2014.[5]

See also

[edit]
  • Ixazomib (trade nameNinlaro) — an orally available boronic acid-derived proteasome inhibitor approved for the treatment of multiple myeloma

References

[edit]
  1. ^"International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 107"(PDF). World Health Organization. p. 193. Retrieved24 April 2016.
  2. ^Zhou HJ, Aujay MA, Bennett MK, Dajee M, Demo SD, Fang Y, et al. (May 2009). "Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047)".Journal of Medicinal Chemistry.52 (9):3028–38.doi:10.1021/jm801329v.PMID 19348473.
  3. ^"Amgen Pipeline Chart". Amgen Inc. February 16, 2016. p. 3. Retrieved24 April 2016.
  4. ^Chauhan D, Singh AV, Aujay M, Kirk CJ, Bandi M, Ciccarelli B, et al. (December 2010)."A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma".Blood.116 (23):4906–15.doi:10.1182/blood-2010-04-276626.PMC 3321748.PMID 20805366.
  5. ^"Oprozomib - Onyx Pharmaceuticals".Adis Insight. Springer Nature Switzerland AG.
SPs/MIs
(M phase)
Blockmicrotubule assembly
Block microtubule disassembly
DNA replication
inhibitor
DNA precursors/
antimetabolites
(S phase)
Folic acid
Purine
Pyrimidine
Deoxyribonucleotide
Topoisomerase inhibitors
(S phase)
I
II
II+Intercalation
Crosslinking of DNA
(CCNS)
Alkylating
Platinum-based
Nonclassical
Intercalation
Photosensitizers/PDT
Other
Enzyme inhibitors
Receptor antagonists
Other/ungrouped
Stub icon

Thisantineoplastic orimmunomodulatorydrug article is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Oprozomib&oldid=1138278448"
Categories:
Hidden categories:
[8]ページ先頭
©2009-2025 Movatter.jp