Ixazomib citrate - CAS 1239908-20-3
Catalog number: 1239908-20-3
Category: Inhibitor
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The citrate salt form of Ixazomib which is a proteasome inhibitor. It is considered a rollover Phase II trial against multiple myeloma, amyloidosis and lymphoma in sorts of countries. IC50: 3.4 nM.
Related CAS:
1201902-80-8; 1072833-77-2 (free base)
White to off-white solid powder
4-(carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid; MLN9708; MLN-9708; MLN 9708; ixazomib citrate MMLN-2238-prodrug Ixazomib-prodrug; Ninlaro
DMSO 103 mg/mL; Water <1 mg/mL
-20ºC Freeze
HDAC-IN-1, an analogue of MC 1568, is a Iia HDACs inhibitor that could probably influence myogenesis and adipogenesis.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
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Current Developer:
Millennium Pharmaceuticals
1.An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma.
Offidani M;Corvatta L;Caraffa P;Gentili S;Maracci L;Leoni P Onco Targets Ther. 2014 Sep 29;7:1793-800. doi: 10.2147/OTT.S49187. eCollection 2014.
Proteasome inhibition represents one of the more important therapeutic targets in the treatment of multiple myeloma (MM), since by suppressing nuclear factor-κB activity, which promotes myelomagenesis, it makes plasma cells susceptible to proapoptotic signals. Bortezomib, the first proteasome inhibitor approved for MM therapy, has been shown to increase response rate and improve outcome in patients with relapsed/refractory disease and in the frontline setting, particularly when combined with immunomodulatory drugs and alkylating agents. Among second-generation proteasome inhibitors, ixazomib (MLN9708) is the first oral compound to be evaluated for the treatment of MM. Ixazomib has shown improved pharmacokinetic and pharmacodynamic parameters compared with bortezomib, in addition to similar efficacy in the control of myeloma growth and prevention of bone loss. Ixazomib was found to overcome bortezomib resistance and to trigger synergistic antimyeloma activity with dexamethasone, lenalidomide, and histone deacetylase inhibitors. Phase I/II studies using ixazomib weekly or twice weekly in relapsed/refractory MM patients suggested antitumor activity of the single agent, but more promising results have been obtained with the combination of ixazomib, lenalidomide, and dexamethasone in newly diagnosed MM.
2.Syntheses of C-13 and C-14-labeled versions of the investigational proteasome inhibitor MLN9708.
Plesescu M;Elliott EL;Li Y;Prakash SR J Labelled Comp Radiopharm. 2013 Jul-Aug;56(9-10):464-70. doi: 10.1002/jlcr.3079. Epub 2013 Jul 9.
MLN9708 (ixazomib citrate) is an investigational, orally bioavailable proteasome inhibitor that is under development by Millennium in clinical studies in both hematologic and nonhematologic malignancies. The stable isotope-labeled MLN9708 was required for bio-analytical studies. [(13) C9 ]-MLN9708 (11) was synthesized in seven steps from the uniformly labeled [(13) C6 ]-1,4-dichlorobenzene (3) and [1-(13) C]-acetyl chloride. Because of the presence of two chlorine atoms and a boron atom, compound 6 was further reacted with [(13) C2 ]-glycine to provide an internal standard that is well separated from the parent compound during mass spectrometric analysis. The radiolabeled version was prepared to support metabolite profiling and whole body autoradiography studies in experimental animals. [(14) C]-MLN9708 (19) was synthesized in six steps from commercially available [(14) C]-barium carbonate. The key intermediate, [carboxyl-(14) C]-2,5-dichlorobenzoic acid (14), was prepared by selective lithiation of 1-bromo-2,5-dichlorobenzene (12) followed by carbonation with [(14) C]-barium carbonate. In preparation for a one-time human absorption, distribution, metabolism and excretion (ADME) study, the stability of [(14) C]-MLN9708 and its precursors were also evaluated.
3.Pharmacokinetic drug evaluation of ixazomib citrate for the treatment of multiple myeloma.
Salvini M;Troia R;Giudice D;Pautasso C;Boccadoro M;Larocca A Expert Opin Drug Metab Toxicol. 2018 Jan;14(1):91-99. doi: 10.1080/17425255.2018.1417388. Epub 2017 Dec 19.
multiple myeloma (MM) is a plasma cell disorder that represents the second most frequent hematologic cancer. Although MM is still an incurable disease, prognosis has improved in the last decades thanks to the introduction of novel agents such as proteasome inhibitors (PIs), immunomodulatory drugs, monoclonal antibodies, and histone deacetylase inhibitors. Areas covered: ixazomib is the first oral PI recently approved by Food and Drug Administration (FDA) and European Medicine Agency (EMA) in combination with lenalidomide and dexamethasone as salvage therapy in MM patients. In this paper, we focus on its pharmacokinetics features, as well as its safety and efficacy in clinical studies. Expert opinion: ixazomib can be considered an oral analogue of bortezomib, with 9.5-day half-life, 58% of oral bioavailability, and a large distribution volume of 543L. These features make it a versatile molecule, potentially useful both in combination and as single agent. Oral route of administration and good efficacy/safety profile are its winning characteristics, providing the rationale for a future role also in the maintenance setting.
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