Ixazomib

DRACPC ID  DRACPC0107

Active Ingredients   Ixazomib

Description  An active metabolite of MLN9708, a second generation, boron containing peptide proteasome inhibitor (PI) with potential antineoplastic activity. Ixazomib binds to and inhibits the 20S catalytic core of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome, which results in an accumulation of unwanted or misfolded proteins; disruption of various cell signaling pathways may follow, resulting in the induction of apoptosis. Compared to first generation PIs, second generation PIs may have an improved pharmacokinetic profile with increased potency and less toxicity. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquinated.

Synonyms  Ninlaro; MLN-2238; MLN2238; {(1R)-1-[(2,5-dichlorobenzamido)acetamido]-3-methylbutyl}boronic Acid

Type  Small Molecule

Disease  Multiple Myeloma

Classification

  

Amino acid and derivative Proteasome inhibitor

Structure Information


Molecular Formula  C14H19BCl2N2O4

Molecular Weight  361

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  [(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid

InChI  InChI=1S/C14H19BCl2N2O4/c1-8(2)5-12(15(22)23)19-13(20)7-18-14(21)10-6-9(16)3-4-11(10)17/h3-4,6,8,12,22-23H,5,7H2,1-2H3,(H,18,21)(H,19,20)/t12-/m0/s1

InChI_Key MXAYKZJJDUDWDS-LBPRGKRZSA-N

SMILES  CC(C)C[C@@H](B(O)O)NC(CNC(C1=CC(Cl)=CC=C1Cl)=O)=O

External Codes


PubChem CID  25183872

DrugBank Accession Number  DB09570

NCI Thesaurus Code  C97940  

UNII  71050168A2   GSRS

CAS  1072833-77-2



Drug approval


Drug indication
    Ixazomib is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

Drug Name Strength Dosage Form/Route Company Marketing Status Drug ID Approval year
Ninlaro 2.3, 3 and 4 mg Capsules; Oral Takeda Pharma A/S Prescription EMEA/H/C/003844 2016
NINLARO EQ 2.3/3/4MG BASE CAPSULE; ORAL TAKEDA PHARMS USA Prescription NDA: 208462 2015

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT02924272 An Open-Label, Rollover Protocol for Patients Previously Enrolled in Millennium-Sponsored Ixazomib Studies Multiple Myeloma; Lymphoma; Amyloidosis Phase 2 Treatment
NCT03616782 Multicenter Phase II Study of Ixazomib Maintenance in Patients With Newly Diagnosed Mantle Cell Lymphoma Mantle Cell Lymphoma Phase 2 Treatment
NCT02302846 Phase II Study Of Ixazomib As Maintenance Therapy For Patients With Acute Myeloid Leukemia (AML) And High Risk Myelodysplastic Syndrome (MDS) In Remission Leukemia Phase 2 Treatment
NCT02993094 Ixazomib (MLN9708) in Combination With Carboplatin in Pretreated Women With Advanced Triple Negative Breast Cancer Triple-Negative Breast Cancer Phase 1/2 Treatment
NCT02181413 A Phase 3, Randomized, Placebo-Controlled, Double-Blind Study of Oral Ixazomib Citrate (MLN9708) Maintenance Therapy in Patients With Multiple Myeloma Following Autologous Stem Cell Transplant Multiple Myeloma; Autologous Stem Cell Transplant Phase 3 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





DRACP is developed by Dr.Zheng's team.