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Details

Stereochemistry ABSOLUTE
Molecular Formula C14H19BCl2N2O4
Molecular Weight 361.0291
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])(B(O)O)N=C(CN=C(c1cc(ccc1Cl)Cl)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

Molecular Formula C14H19BCl2N2O4
Molecular Weight 361.0291
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: 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 (trade name Ninlaro) is a drug for the treatment of multiple myeloma in adults after at least one prior therapy, in combination with lenalidomide and dexamethasone. It is taken by mouth in form of capsules. Common side effects include diarrhea, constipation and low platelet count. Like the older bortezomib (which can only be given by injection), it acts as a proteasome inhibitor, has orphan drug status in the US and Europe. At therapeutic concentrations, ixazomib selectively and reversibly inhibits the protein proteasome subunit beta type-5 (PSMB5) with a dissociation half-life of 18 minutes. This mechanism is the same as of bortezomib, which has a much longer dissociation half-life of 110 minutes; the related drug carfilzomib, by contrast, blocks PSMB5 irreversibly. Proteasome subunits beta type-1 and type-2 are only inhibited at high concentrations reached in cell culture models. PSMB5 is part of the 20S proteasome complex and has enzymatic activity similar to chymotrypsin. It induces apoptosis, a type of programmed cell death, in various cancer cell lines. A synergistic effect of ixazomib and lenalidomide has been found in a large number of myeloma cell lines. The medication is taken orally as a prodrug, ixazomib citrate, which is a boronic ester; this ester rapidly hydrolyzes under physiological conditions to its biologically active form, ixazomib, a boronic acid. Absolute bioavailability is 58%, and highest blood plasma concentrations of ixazomib are reached after one hour. Plasma protein binding is 99%.

CNS Activity

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P28074|||Q86T01
Gene ID: 5693
Gene Symbol: PSMB5
Target Organism: Homo sapiens (Human)
0.930000000000000049 nM [Ki]
Target ID: P28074|||Q86T01
Gene ID: 5693
Gene Symbol: PSMB5
Target Organism: Homo sapiens (Human)
3.39999999999999991 nM [IC50]
Target ID: P49721
Gene ID: 5690
Gene Symbol: PSMB2
Target Organism: Homo sapiens (Human)
3500 nM [IC50]
Target ID: P20618
Gene ID: 5689
Gene Symbol: PSMB1
Target Organism: Homo sapiens (Human)
31 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

1447977600000
Primary
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

1447977600000
Primary
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

1447977600000
Primary
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

1447977600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
77 ng/mL
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
multiple, oral
IXAZOMIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
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%
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:
unhealthy, 45 years (range: 23–73 years)
Health Status: unhealthy
Age Group: 45 years (range: 23–73 years)
Sex: M+F
Sources:
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 1 patient)
Sources:
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:
unhealthy, 56 years (range: 27–72 years)
Health Status: unhealthy
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 3, 1 patient)
Sources:
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:
unhealthy, 69.5 years (range: 47–75 years)
Health Status: unhealthy
Age Group: 69.5 years (range: 47–75 years)
Sex: M+F
Sources:
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 3, 1 patient)
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
DLT: Nausea, Vomiting...
Dose limiting toxicities:
Nausea (grade 3, 1 patient)
Vomiting (grade 3, 1 patient)
Diarrhea (grade 3, 1 patient)
Sources:
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 3, 1 patient)
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
DLT: Diarrhea, Renal failure...
Dose limiting toxicities:
Diarrhea (grade 3, 1 patient)
Renal failure (grade 2, 1 patient)
Dyspnea (grade 2, 1 patient)
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Sources:
unhealthy
Disc. AE: Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (8.6%)
Sources:
4 mg 1 times / week multiple, oral
Recommended
Dose: 4 mg, 1 times / week
Route: oral
Route: multiple
Dose: 4 mg, 1 times / week
Sources:
unhealthy
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:
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:
unhealthy, 45 years (range: 23–73 years)
Health Status: unhealthy
Age Group: 45 years (range: 23–73 years)
Sex: M+F
Sources:
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:
unhealthy, 56 years (range: 27–72 years)
Health Status: unhealthy
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Sources:
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:
unhealthy, 56 years (range: 27–72 years)
Health Status: unhealthy
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Sources:
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:
unhealthy, 56 years (range: 27–72 years)
Health Status: unhealthy
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Sources:
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:
unhealthy, 56 years (range: 27–72 years)
Health Status: unhealthy
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Sources:
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:
unhealthy, 56 years (range: 27–72 years)
Health Status: unhealthy
Age Group: 56 years (range: 27–72 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 69.5 years (range: 47–75 years)
Health Status: unhealthy
Age Group: 69.5 years (range: 47–75 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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:
unhealthy, 64.0 years (range: 40-76 years)
Health Status: unhealthy
Age Group: 64.0 years (range: 40-76 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, 66 years (range: 38 - 91 years)
Health Status: unhealthy
Age Group: 66 years (range: 38 - 91 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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:
unhealthy, 66.0 years (range: 54–77 years)
Health Status: unhealthy
Age Group: 66.0 years (range: 54–77 years)
Sex: M+F
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Sources:
unhealthy
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
Sources:
unhealthy
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
Sources:
unhealthy
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
Sources:
unhealthy
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
Sources:
unhealthy
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
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
minor
minor
minor
minor
no
weak
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
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
Tox targets

Tox targets

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
An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma.
2014
Patents

Sample Use Guides

Recommended starting dose of 4 mg taken orally on Days 1, 8, and 15 of a 28-day cycle.
Route of Administration: Oral
In a cell viability assay, MM.1S {Dexamethasone-(Dex) sensitive}, MM.1R (Dex-resistant), RPMI-8226, OPM1, OPM2, H929 and INA-6 (IL-6-dependent) human multiple myeloma cell lines were treated with various concentrations of ixazomib (6.25, 12.5, 25, 50 nM) for 48h. The anti-myeloma activity of the drug was observed in MM cell lines sensitive and resistant to conventional therapies, as well as representing distinct cytogenetic profiles.
Substance Class Chemical
Created
by admin
on Sat Jun 26 07:45:12 UTC 2021
Edited
by admin
on Sat Jun 26 07:45:12 UTC 2021
Record UNII
71050168A2
Record Status Validated (UNII)
Record Version
  • Download
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
IXAZOMIB [WHO-DD]
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 [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 Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
WHO-ATC L01XX50
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
NDF-RT N0000175604
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
EU-Orphan Drug EU/3/12/1060
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
Code System Code Type Description
DRUG CENTRAL
5067
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
PUBCHEM
25183872
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
CAS
1072833-77-2
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
LACTMED
Ixazomib
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
RXCUI
1723735
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY RxNorm
NCI_THESAURUS
C97940
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
DRUG BANK
DB09570
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
EVMPD
SUB121332
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
FDA UNII
71050168A2
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
WIKIPEDIA
Ixazomib
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
INN
9411
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
MERCK INDEX
M11904
Created by admin on Sat Jun 26 07:45:12 UTC 2021 , Edited by admin on Sat Jun 26 07:45:12 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
CYP 1A2 CONTRIBUTES FOR 26% OF IXAZOMIB METABOLISM
METABOLIC ENZYME -> SUBSTRATE
At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (< 1%).
EXCRETED UNCHANGED
62% of the 4.1 MG dose recovered in the urine (3.3% as unchanged drug)
AMOUNT EXCRETED
URINE
METABOLIC ENZYME -> SUBSTRATE
At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (< 1%).
METABOLIC ENZYME -> SUBSTRATE
At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (< 1%).
METABOLIC ENZYME -> SUBSTRATE
At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (< 1%).
METABOLIC ENZYME -> SUBSTRATE
CYP 3A CONTRIBUTES FOR 42% OF IXAZOMIB METABOLISM
MAJOR
METABOLIC ENZYME -> SUBSTRATE
CYP 2B6 CONTRIBUTES FOR 16% OF IXAZOMIB METABOLISM
BINDER->LIGAND
BINDING
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC