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
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.
