U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C14H19BCl2N2O4
Molecular Weight 361.029
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IXAZOMIB

SMILES

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

InChI

InChIKey=MXAYKZJJDUDWDS-LBPRGKRZSA-N
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

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including https://clinicaltrials.gov/ct2/show/NCT02630030 | https://www.ncbi.nlm.nih.gov/pubmed/24486586 | https://www.ncbi.nlm.nih.gov/pubmed/25016815 | https://www.ncbi.nlm.nih.gov/pubmed/25605842

Ixazomib (MLN2238) is an active metabolite of orally bioavailable proteasome inhibitor ixazomib citrate (MLN9708), which hydrolyzes upon administration. Ixazomib citrate was approved under the name Ninlaro for the treatment of multiple myeloma in patients who have received at least one prior therapy. In vitro studies has shown that ixazomib preferentially binds and inhibits the chymotrypsin-like activity of the beta 5 subunit of the 20S proteasome.

CNS Activity

CNS Penetrant
2432
Curator's Comment: Following oral administration, a tissue distribution study in rats revealed that the brain and spinal cord were amongst the tissues with the lowest levels, suggesting that the penetration of ixazomib through the blood-brain barrier appears to be limited. However, the relevance to humans is unknown.

Originator

Approval Year

2015
462
Targets

Targets

Primary TargetPharmacologyConditionPotency
Proteasome subunit beta type-5
6
Target ID: P28074|||Q86T01
Gene ID: 5693.0
Gene Symbol: PSMB5
Target Organism: Homo sapiens (Human)
Inhibitor
8146
 0.93 nM [Ki]
Proteasome subunit beta type-5
6
Target ID: P28074|||Q86T01
Gene ID: 5693.0
Gene Symbol: PSMB5
Target Organism: Homo sapiens (Human)
Inhibitor
8146
 3.4 nM [IC50]
Proteasome subunit beta type-2
3
Target ID: P49721
Gene ID: 5690.0
Gene Symbol: PSMB2
Target Organism: Homo sapiens (Human)
Inhibitor
8146
 3500.0 nM [IC50]
Proteasome subunit beta type-1
3
Target ID: P20618
Gene ID: 5689.0
Gene Symbol: PSMB1
Target Organism: Homo sapiens (Human)
Inhibitor
8146
 31.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8307
NINLARO

Approved Use

NINLARO is a proteasome inhibitor indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

Launch Date

1.44797755E12
Primary
Approved
8307
NINLARO

Approved Use

INDICATIONS AND USAGE. NINLARO is a proteasome inhibitor indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

Launch Date

1.44797755E12
Primary
Phase I
422
NINLARO

Approved Use

INDICATIONS AND USAGE. NINLARO is a proteasome inhibitor indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

Launch Date

1.44797755E12
Primary
Phase II
1133
NINLARO

Approved Use

INDICATIONS AND USAGE. NINLARO is a proteasome inhibitor indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

Launch Date

1.44797755E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
77 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/26872892
4 mg single, oral
dose: 4 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
22.8 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/26872892
4 mg single, oral
dose: 4 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
77 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26872892/
4 mg 3 times / 2 weeks multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
25.8 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27196567/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
22.8 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26872892/
4 mg 3 times / 2 weeks multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1470 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/26872892
4 mg single, oral
dose: 4 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
999 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/26872892
4 mg single, oral
dose: 4 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
1470 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26872892/
4 mg 3 times / 2 weeks multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
575 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27196567/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
999 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26872892/
4 mg 3 times / 2 weeks multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
1161.92 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1.33 mg/m^2 1 times / 3 days multiple, intravenous
dose: 1.33 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
1542.63999999999 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1.76 mg/m^2 1 times / 3 days multiple, intravenous
dose: 1.76 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
191.87 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1 mg/m^2 single, intravenous
dose: 1 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
301 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
0.5 mg/m^2 1 times / 3 days multiple, intravenous
dose: 0.5 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
3800 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
2.34 mg/m^2 1 times / 3 days multiple, intravenous
dose: 2.34 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
391.46 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1.33 mg/m^2 single, intravenous
dose: 1.33 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
522.74 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1.76 mg/m^2 single, intravenous
dose: 1.76 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
579.91 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1 mg/m^2 1 times / 3 days multiple, intravenous
dose: 1 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
60.9 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
0.25 mg/m^2 1 times / 3 days multiple, intravenous
dose: 0.25 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
620 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
2.34 mg/m^2 single, intravenous
dose: 2.34 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
91.6 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
0.5 mg/m^2 single, intravenous
dose: 0.5 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
144.69 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1.33 mg/m^2 1 times / 3 days multiple, intravenous
dose: 1.33 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
104.84 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1.76 mg/m^2 1 times / 3 days multiple, intravenous
dose: 1.76 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
90.8 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
2.34 mg/m^2 1 times / 3 days multiple, intravenous
dose: 2.34 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
171.9 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT00830869
1 mg/m^2 1 times / 3 days multiple, intravenous
dose: 1 mg/m^2
route of administration: intravenous
experiment type: multiple
co-administered:
IXAZOMIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status:
9.5 day
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28290121/
multiple, oral
 IXAZOMIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27196567/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IXAZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
IXAZOMIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1.76 mg/m2 3 times / month multiple, intravenous
Dose: 1.76 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 1.76 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 45 years (range: 23–73 years)
n = 7
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 45 years (range: 23–73 years)
Sex: M+F
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
3.11 mg/m2 3 times / month multiple, intravenous
Highest studied dose
Dose: 3.11 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 3.11 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 56 years (range: 27–72 years)
n = 5
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
DLT: Acute renal failure, Diarrhea...
Dose limiting toxicities:
Acute renal failure (grade 3, 1 patient)
Diarrhea (grade 2-3, 2 patients)
Vomiting (grade 2-3, 2 patients)
Fatigue (grade 2, 1 patient)
Nausea (grade 2, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
5.5 mg 3 times / month multiple, oral
Highest studied dose
Dose: 5.5 mg, 3 times / month
Route: oral
Route: multiple
Dose: 5.5 mg, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed or refractory light-chain (AL) amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
DLT: Diarrhea, Renal failure...
Dose limiting toxicities:
Diarrhea (grade 3, 1 patient)
Renal failure (grade 2, 1 patient)
Failure respiratory (grade 2, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
4 mg 3 times / month multiple, oral
MTD|RP2D|Recommended
Dose: 4 mg, 3 times / month
Route: oral
Route: multiple
Dose: 4 mg, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 6
Health Status: unhealthy
Condition: relapsed or refractory light-chain (AL) amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
2.34 mg/m2 3 times / month multiple, intravenous
MTD
Dose: 2.34 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 2.34 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 69.5 years (range: 47–75 years)
n = 10
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 69.5 years (range: 47–75 years)
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
3.95 mg/m2 1 times / week multiple, oral
Highest studied dose
Dose: 3.95 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 3.95 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
n = 4
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
DLT: Nausea, Vomiting...
Dose limiting toxicities:
Nausea (grade 3, 1 patient)
Vomiting (grade 3, 1 patient)
Diarrhea (grade 3, 1 patient)
Erythema multiforme (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
2.97 mg/m2 1 times / week multiple, oral
MTD
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
DLT: Nausea, Vomiting...
Dose limiting toxicities:
Nausea (grade 3, 1 patient)
Vomiting (grade 3, 1 patient)
Diarrhea (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Other AEs: Upper respiratory tract infection, Upper respiratory tract infection...
Other AEs:
Upper respiratory tract infection (grade 1-2, 19%)
Upper respiratory tract infection (grade 3, <1%)
Peripheral neuropathies (grade 1-2, 28%)
Peripheral neuropathies (grade 3, 2%)
Diarrhea (grade 1-2, 42%)
Diarrhea (grade 3, 6%)
Constipation (grade 1-2, 34%)
Constipation (grade 3, <1%)
Nausea (grade 1-2, 26%)
Nausea (grade 3, 2%)
Vomiting (grade 1-2, 22%)
Vomiting (grade 3, 1%)
Rash (grade 1-2, 19%)
Rash (grade 3, 3%)
Back pain (grade 1-2, 21%)
Back pain (grade 3, <1%)
Edema peripheral (grade 1-2, 25%)
Edema peripheral (grade 3, 2%)
Thrombocytopenia (grade 1-2, 78%)
Thrombocytopenia (grade 3, 26%)
Neutropenia (grade 1-2, 67%)
Neutropenia (grade 3, 26%)
Blurred vision (all grades, 3%)
Dry eye (5%)
Conjunctivitis (6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
4 mg 1 times / week multiple, oral
MTD
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 6
Health Status: unhealthy
Condition: relapsed/refractory AL amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
5.5 mg 1 times / week multiple, oral
Dose: 5.5 mg, 1 times / week
Route: oral
Route: multiple
Dose: 5.5 mg, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed/refractory AL amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
DLT: Diarrhea, Renal failure...
Dose limiting toxicities:
Diarrhea (grade 3, 1 patient)
Renal failure (grade 2, 1 patient)
Dyspnea (grade 2, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Disc. AE: Thrombocytopenia, Diarrhea...
Other AEs: Renal failure...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (1 patient)
Diarrhea (1 patient)
Nausea and vomiting (1 patient)
Hypercalcemia (1 patient)
Dyspnea (1 patient)
Other AEs:
Renal failure (2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
Disc. AE: Diarrhea, Fatigue...
AEs leading to
discontinuation/dose reduction:
Diarrhea
Fatigue (0.8%)
Asthenia (0.8%)
Peripheral sensory neuropathy (0.6%)
Septic shock (0.6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 56
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 56
Disc. AE: Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (8.6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 56
AEs

AEs

AESignificanceDosePopulation
Neutropenia grade 4, 1 patient
DLT
1.76 mg/m2 3 times / month multiple, intravenous
Dose: 1.76 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 1.76 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 45 years (range: 23–73 years)
n = 7
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 45 years (range: 23–73 years)
Sex: M+F
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Fatigue grade 2, 1 patient
DLT
3.11 mg/m2 3 times / month multiple, intravenous
Highest studied dose
Dose: 3.11 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 3.11 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 56 years (range: 27–72 years)
n = 5
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Nausea grade 2, 1 patient
DLT
3.11 mg/m2 3 times / month multiple, intravenous
Highest studied dose
Dose: 3.11 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 3.11 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 56 years (range: 27–72 years)
n = 5
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Diarrhea grade 2-3, 2 patients
DLT
3.11 mg/m2 3 times / month multiple, intravenous
Highest studied dose
Dose: 3.11 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 3.11 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 56 years (range: 27–72 years)
n = 5
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Vomiting grade 2-3, 2 patients
DLT
3.11 mg/m2 3 times / month multiple, intravenous
Highest studied dose
Dose: 3.11 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 3.11 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 56 years (range: 27–72 years)
n = 5
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Acute renal failure grade 3, 1 patient
DLT
3.11 mg/m2 3 times / month multiple, intravenous
Highest studied dose
Dose: 3.11 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 3.11 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 56 years (range: 27–72 years)
n = 5
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Failure respiratory grade 2, 1 patient
DLT, Disc. AE
5.5 mg 3 times / month multiple, oral
Highest studied dose
Dose: 5.5 mg, 3 times / month
Route: oral
Route: multiple
Dose: 5.5 mg, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed or refractory light-chain (AL) amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Renal failure grade 2, 1 patient
DLT, Disc. AE
5.5 mg 3 times / month multiple, oral
Highest studied dose
Dose: 5.5 mg, 3 times / month
Route: oral
Route: multiple
Dose: 5.5 mg, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed or refractory light-chain (AL) amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Diarrhea grade 3, 1 patient
DLT
5.5 mg 3 times / month multiple, oral
Highest studied dose
Dose: 5.5 mg, 3 times / month
Route: oral
Route: multiple
Dose: 5.5 mg, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed or refractory light-chain (AL) amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Thrombocytopenia grade 3, 1 patient
DLT, Disc. AE
4 mg 3 times / month multiple, oral
MTD|RP2D|Recommended
Dose: 4 mg, 3 times / month
Route: oral
Route: multiple
Dose: 4 mg, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 6
Health Status: unhealthy
Condition: relapsed or refractory light-chain (AL) amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Neutropenia grade 3, 1 patient
DLT
2.34 mg/m2 3 times / month multiple, intravenous
MTD
Dose: 2.34 mg/m2, 3 times / month
Route: intravenous
Route: multiple
Dose: 2.34 mg/m2, 3 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
unhealthy, 69.5 years (range: 47–75 years)
n = 10
Health Status: unhealthy
Condition: non-hematologic malignancies
Age Group: 69.5 years (range: 47–75 years)
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/25325301
Diarrhea grade 3, 1 patient
DLT, Disc. AE
3.95 mg/m2 1 times / week multiple, oral
Highest studied dose
Dose: 3.95 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 3.95 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
n = 4
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Erythema multiforme grade 3, 1 patient
DLT, Disc. AE
3.95 mg/m2 1 times / week multiple, oral
Highest studied dose
Dose: 3.95 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 3.95 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
n = 4
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Nausea grade 3, 1 patient
DLT, Disc. AE
3.95 mg/m2 1 times / week multiple, oral
Highest studied dose
Dose: 3.95 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 3.95 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
n = 4
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Vomiting grade 3, 1 patient
DLT, Disc. AE
3.95 mg/m2 1 times / week multiple, oral
Highest studied dose
Dose: 3.95 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 3.95 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
n = 4
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Diarrhea grade 3, 1 patient
DLT, Disc. AE
2.97 mg/m2 1 times / week multiple, oral
MTD
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Nausea grade 3, 1 patient
DLT, Disc. AE
2.97 mg/m2 1 times / week multiple, oral
MTD
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Vomiting grade 3, 1 patient
DLT, Disc. AE
2.97 mg/m2 1 times / week multiple, oral
MTD
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Condition: relapsed/refractory multiple myeloma
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24904120
Dry eye 5%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Conjunctivitis 6%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Blurred vision all grades, 3%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Rash grade 1-2, 19%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Upper respiratory tract infection grade 1-2, 19%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Back pain grade 1-2, 21%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Vomiting grade 1-2, 22%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Edema peripheral grade 1-2, 25%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Nausea grade 1-2, 26%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Peripheral neuropathies grade 1-2, 28%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Constipation grade 1-2, 34%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Diarrhea grade 1-2, 42%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Neutropenia grade 1-2, 67%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Thrombocytopenia grade 1-2, 78%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Vomiting grade 3, 1%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Edema peripheral grade 3, 2%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Nausea grade 3, 2%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Peripheral neuropathies grade 3, 2%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Neutropenia grade 3, 26%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Thrombocytopenia grade 3, 26%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Rash grade 3, 3%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Diarrhea grade 3, 6%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Back pain grade 3, <1%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Constipation grade 3, <1%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Upper respiratory tract infection grade 3, <1%
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
unhealthy, 66 years (range: 38 - 91 years)
n = 360
Health Status: unhealthy
Condition: relapsed and/or refractory multiple myeloma
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf
Thrombocytopenia grade 3, 1 patient
DLT, Disc. AE
4 mg 1 times / week multiple, oral
MTD
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 6
Health Status: unhealthy
Condition: relapsed/refractory AL amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Dyspnea grade 2, 1 patient
DLT
5.5 mg 1 times / week multiple, oral
Dose: 5.5 mg, 1 times / week
Route: oral
Route: multiple
Dose: 5.5 mg, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed/refractory AL amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Renal failure grade 2, 1 patient
DLT
5.5 mg 1 times / week multiple, oral
Dose: 5.5 mg, 1 times / week
Route: oral
Route: multiple
Dose: 5.5 mg, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed/refractory AL amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Diarrhea grade 3, 1 patient
DLT, Disc. AE
5.5 mg 1 times / week multiple, oral
Dose: 5.5 mg, 1 times / week
Route: oral
Route: multiple
Dose: 5.5 mg, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
unhealthy, 66.0 years (range: 54–77 years)
n = 5
Health Status: unhealthy
Condition: relapsed/refractory AL amyloidosis
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/28550039
Diarrhea 1 patient
Disc. AE
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Dyspnea 1 patient
Disc. AE
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Hypercalcemia 1 patient
Disc. AE
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Nausea and vomiting 1 patient
Disc. AE
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Thrombocytopenia 1 patient
Disc. AE
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Renal failure 2 patients
2.97 mg/m2 1 times / week multiple, oral
Recommended
Dose: 2.97 mg/m2, 1 times / week
Route: oral
Route: multiple
Dose: 2.97 mg/m2, 1 times / week
Co-administed with::
lenalidomide(25mg, PO, 1-21 day)
dexamethasone(40mg, PO, 1-21 day, Days 1, 8, 15, 22)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: cancer
Age Group: adult
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000ClinPharmR.pdf
Page: C16005
Peripheral sensory neuropathy 0.6%
Disc. AE
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
Septic shock 0.6%
Disc. AE
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
Asthenia 0.8%
Disc. AE
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
Fatigue 0.8%
Disc. AE
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
Diarrhea Disc. AE
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 55
Thrombocytopenia 8.6%
Disc. AE
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Co-administed with::
lenalidomide(25 mg on Days 1 throughn21)
dexamethasone(40 mg on Days 1, 8, 15, and 22 of a 28-day cycle)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 56
unhealthy
n = 360
Health Status: unhealthy
Population Size: 360
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208462Orig1s000MedR.pdf
Page: p. 56
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1670

inhibitor
1532

inducer
753
substrate
985
substrate
1168

inhibitor
1789
inhibitor
1570

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1463

CYP2B6
770

CYP2C8
869

CYP2C19
1410

P-gp
1401

BCRP
678

MRP2
363

OATP1B1
770

OATP1B3
691

OAT1
584

OAT3
625

OCT2
630

MATE1
302

MATE2
259
esterase
68

CYP1A2
1013

CYP2B6
648

CYP2C8
670

CYP2C19
955

P-gp
1491
CYP1A2
671

CYP2B6
521
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1620
 no [IC50 >30 uM]
CYP2B6
946
 no [IC50 >30 uM]
CYP2C19
1484
 no [IC50 >30 uM]
CYP2C8
923
 no [IC50 >30 uM]
CYP2D6
1826
 no [IC50 >30 uM]
CYP3A4
1857
 no [IC50 >30 uM]
BCRP
751
 no
CYP1A2
1620
 no
CYP2B6
946
 no
CYP3A4
1857
 no
MATE1
304
 no
MATE2
259
 no
MRP2
452
 no
OAT1
588
 no
OAT3
627
 no
OATP1B1
785
 no
OATP1B3
700
 no
OCT2
631
 no
P-gp
1588
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
esterase
68
 major
CYP2B6
648
 minor
CYP2C19
955
 minor
CYP2C8
670
 minor
CYP2D6
1168
 minor
CYP2C9
985
 no
P-gp
1491
 weak
CYP1A2
1013
 yes
unlikely
Comment: Smoking is known to be a moderate CYP1A2 inducer. Based on population PK analyses of smokers in the Phase 3 Study C16010, smoking status (n=33 current smokers) was not found to be a significant covariate affecting ixazomib PK
Page: 8.0
CYP3A4
1670
 yes
yes (co-administration study)
Comment: Clinical DDI studies with strong CYP3A4 inhibitors ketoconazole and clarithromycin did not show clinically meaningful effects on ixazomib systemic exposure. On the other hand, clinical study with the strong CYP3A4 inducer rifampin showed significant decrease in ixazomib exposure (AUC v74%, CMAX |54%).
Page: 5.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1603
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:90942
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:90942
ChemicalBook
CB62521080
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62521080
MolPort
MolPort-016-633-297
https://www.molport.com/shop/molecule-link/MolPort-016-633-297
Selleck Chemicals
MLN-2238
http://www.selleckchem.com/products/MLN-2238.html
ZINC
ZINC000169946773
http://zinc15.docking.org/substances/ZINC000169946773
eMolecules
32278221
https://www.emolecules.com/cgi-bin/more?vid=32278221
PubMed

PubMed

TitleDatePubMed
Intracellular protein degradation: from a vague idea, through the lysosome and the ubiquitin-proteasome system, and onto human diseases and drug targeting (Nobel lecture).
2005 Sep 19
Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma.
2007 Apr
Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.
2010 Mar 1
An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma.
2014
Ixazomib for the treatment of multiple myeloma.
2015
The investigational proteasome inhibitor ixazomib for the treatment of multiple myeloma.
2015
Therapeutic landscape of carfilzomib and other modulators of the ubiquitin-proteasome pathway.
2015 Mar 1
Patents

Patents

US7442830 B1
2
WO2009154737
2

Sample Use Guides

In Vivo Use Guide
Recommended starting dose of 4 mg taken orally on Days 1, 8, and 15 of a 28-day cycle. Dose should be taken at least one hour before or at least two hours after food.
Route of Administration: Oral
In Vitro Use Guide
Osteoblasts were generated from mesenchymal osteoprogenitors by culture in osteogenic medium (containing 5 mmol/L b-glycerophosphate, 50 mkg/mL ascorbic acid, and 80 nmol/L dexamethasone). Mesenchymal stem cell (MSC, passage 2–3) or the hMSC–TERT cell line were exposed to different MLN2238 or bortezomib concentrations and cultured in osteogenic medium for 11 or 21 days for alkaline phosphatase (ALP) activity and matrix mineralization assays, respectively. ALP activity was quantified by hydrolysis of p-nitrophenylphosphate into p-nitrophenol (Sigma-Aldrich), whereas mineralization was assessed by quantitative measurement of Alizarin Red staining.
Name Type Language
IXAZOMIB
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
IXAZOMIB [MI]
Common Name English
MLN2238
Code English
IXAZOMIB [USAN]
Common Name English
MLN-9708 FREE BASE
Code English
MLN-2238
Code English
((1R)-1-((2,5-DICHLOROBENZAMIDO)ACETAMIDO)-3-METHYLBUTYL)BORONIC ACID
Systematic Name English
Ixazomib [WHO-DD]
Common Name English
ixazomib [INN]
Common Name English
BORONIC ACID, B-((1R)-1-((2-((2,5-DICHLOROBENZOYL)AMINO)ACETYL)AMINO)-3-METHYLBUTYL)-
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C2160
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
WHO-ATC L01XX50
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
NDF-RT N0000175604
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
EU-Orphan Drug EU/3/12/1060
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
Code System Code Type Description
DRUG CENTRAL
5067
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
PUBCHEM
25183872
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
CAS
1072833-77-2
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
LACTMED
Ixazomib
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
RXCUI
1723735
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY RxNorm
NCI_THESAURUS
C97940
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
DRUG BANK
DB09570
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
EVMPD
SUB121332
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
FDA UNII
71050168A2
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
DAILYMED
71050168A2
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
CHEBI
90942
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
WIKIPEDIA
Ixazomib
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
INN
9411
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
EPA CompTox
DTXSID701025662
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
PRIMARY
MERCK INDEX
M11904
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
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USAN
YY-46
Created by admin on Sat Dec 17 00:07:08 UTC 2022 , Edited by admin on Sat Dec 17 00:07:08 UTC 2022
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ACTIVE MOIETY
Structure of IXAZOMIB
METABOLITE (PARENT)
Structure of 2,5-DICHLOROBENZAMIDE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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