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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H25BN4O4
Molecular Weight 384.237
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BORTEZOMIB

SMILES

CC(C)C[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)B(O)O

InChI

InChIKey=GXJABQQUPOEUTA-RDJZCZTQSA-N
InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1

HIDE SMILES / InChI

Molecular Formula C19H25BN4O4
Molecular Weight 384.237
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/11854543 http://www.drugbank.ca/drugs/DB00188 https://www.drugs.com/mtm/bortezomib.html https://en.wikipedia.org/wiki/Bortezomib

Bortezomib is the therapeutic proteasome inhibitor. First, which is tested in humans. The boron atom in bortezomib binds the catalytic site of the 26S proteasome with high affinity and specificity. Bortezomib is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. The 26S proteasome degrades various proteins critical to cancer cell survival, such as cyclins, tumor suppressors, BCL-2, and cyclin-dependent kinase inhibitors. Inhibition of these degradations sensitizes cells to apoptosis. Bortezomib is a potent inhibitor of 26S proteasome, which sensitizes activity in dividing multiple myeloma and leukemic cells, thus inducing apoptosis. Most commonly reported adverse reactions (incidence ≥30%) in clinical studies include asthenic conditions, diarrhea, nausea, constipation, peripheral neuropathy, vomiting, pyrexia, thrombocytopenia, psychiatric disorders, anorexia and decreased appetite, neutropenia, neuralgia, leukopenia and anemia. Co-administration of ketoconazole, a potent CYP3A inhibitor, increased the exposure of bortezomib. Co-administration of melphalan-prednisone increased the exposure of bortezomib. However, this increase is unlikely to be clinically relevant.

CNS Activity

Curator's Comment: Based on animal studies, the penetration of bortezomib through the blood-brain barrier appears to be limited, if any and the relevance to humans is unknown. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000539/WC500048467.pdf http://meeting.ascopubs.org/cgi/content/short/24/18_suppl/12036 https://www.ncbi.nlm.nih.gov/pubmed/26792401

Originator

Curator's Comment: ProScript was acquired in 1999 by Millennium Pharmaceuticals Inc., which eventually funded studies of PS-341. http://archive.boston.com/business/healthcare/articles/2007/05/06/the_velcade_story/

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.6 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VELCADE

Approved Use

VELCADE is a proteasome inhibitor indicated for: treatment of patients with multiple myeloma (1.1) treatment of patients with mantle cell lymphoma (1.2) 1.1 Multiple Myeloma VELCADE® (bortezomib) is indicated for the treatment of patients with multiple myeloma. 1.2 Mantle Cell Lymphoma VELCADE is indicated for the treatment of patients with mantle cell lymphoma.

Launch Date

1.052784E12
Primary
VELCADE

Approved Use

VELCADE is a proteasome inhibitor indicated for: treatment of patients with multiple myeloma (1.1) treatment of patients with mantle cell lymphoma (1.2) 1.1 Multiple Myeloma VELCADE® (bortezomib) is indicated for the treatment of patients with multiple myeloma. 1.2 Mantle Cell Lymphoma VELCADE is indicated for the treatment of patients with mantle cell lymphoma.

Launch Date

1.052784E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
106.2 ng/mL
1 mg/m² 1 times / 4 days multiple, oral
dose: 1 mg/m²
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
127.02 ng/mL
1.3 mg/m^2 1 times / 4 day steady, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: steady
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
76.43 ng/mL
1.3 mg/m^2 single, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
82.8 ng × h/mL
1 mg/m² 1 times / 4 days multiple, oral
dose: 1 mg/m²
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
190.39 ng*h/mL
1.3 mg/m^2 1 times / 4 day steady, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: steady
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
51.86 ng*h/mL
1.3 mg/m^2 single, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
106.99 ng*h/mL
1.3 mg/m^2 single, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
349.62 ng*h/mL
1.3 mg/m^2 1 times / 4 day steady, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: steady
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
78.9 h
1 mg/m² 1 times / 4 days multiple, oral
dose: 1 mg/m²
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.08 h
1.3 mg/m^2 single, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: single
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
51.55 h
1.3 mg/m^2 1 times / 4 day steady, intravenous
dose: 1.3 mg/m^2
route of administration: intravenous
experiment type: steady
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
17%
BORTEZOMIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
DLT: Thrombocytopenia, Sensory neuropathy...
Other AEs: Diarrhea, Hypotension...
Dose limiting toxicities:
Thrombocytopenia (grade 3, 1 patient)
Sensory neuropathy (grade 3, 1 patient)
Fatigue (grade 3, 1 patient)
Other AEs:
Diarrhea (grade 3-4, 1 patient)
Hypotension (grade 3-4, 1 patient)
Hypoxia (grade 3-4, 1 patient)
Infection (grade 3-4, 1 patient)
Acidosis (grade 3-4)
CPK increased (grade 3-4)
Blood bicarbonate low (grade 3-4)
Hypokalemia (grade 3-4)
Alanine aminotransferase increase (grade 3-4)
Sources:
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Other AEs: Thrombocytopenia, Sensory neuropathy...
Other AEs:
Thrombocytopenia (all grades, 5 patients)
Sensory neuropathy (grade 3, 3 patients)
Abdominal pain (grade 3, 1 patient)
Constipation (grade 3, 1 patient)
Depressed level of consciousness (grade 3, 1 patient)
Fatigue (grade 3, 1 patient)
Headache (grade 3, 1 patient)
Pain (grade 3, 1 patient)
Hypokalemia (grade 3, 1 patient)
Sources:
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Other AEs: Thrombocytopenia, Thrombocytopenia...
Other AEs:
Thrombocytopenia (grade 3, 18%)
Thrombocytopenia (grade 4-5, 17%)
Neutropenia (grade 3, 30%)
Neutropenia (grade 4-5, 10%)
Anemia (grade 3, 12%)
Anemia (grade 4-5, 1%)
Leukopenia (grade 3, 19%)
Leukopenia (grade 4-5, 2%)
Lymphopenia (grade 3, 14%)
Lymphopenia (grade 4-5, 5%)
Nausea (grade 3, 3%)
Diarrhea (grade 3, 6%)
Diarrhea (grade 4-5, 1%)
Vomiting (grade 3, 4%)
Constipation (grade 3, 1%)
Abdominal pain upper (grade 3, <1%)
Peripheral neuropathy (grade 3, 12%)
Peripheral neuropathy (grade 4-5, 1%)
Neuralgia (grade 3, 8%)
Neuralgia (grade 4-5, 1%)
Paresthesia (grade 3, 2%)
Fatigue (grade 3, 6%)
Fatigue (grade 4-5, 1%)
Asthenia (grade 3, 5%)
Pyrexia (grade 3, 1%)
Herpes zoster (grade 3, 3%)
Anorexia (grade 3, 2%)
Rash (grade 3, 1%)
Insomnia (grade 3, < 1%)
Sources:
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: multiple myeloma |mantle cell lymphoma
Sex: M+F
Population Size: 331
Sources:
Disc. AE: Hypotension, Pyrexia...
AEs leading to
discontinuation/dose reduction:
Hypotension (1%)
Pyrexia (< 1%)
Weakness (< 1%)
Asthenia (< 1%)
Sources:
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Disc. AE: Peripheral neuropathy, Cardiogenic shock...
Other AEs: Diarrhea, Dehydration...
AEs leading to
discontinuation/dose reduction:
Peripheral neuropathy (8%)
Cardiogenic shock (grade 5, 1 patient)
Respiratory insufficiency (grade 5, 1 patient)
Congestive heart failure (grade 5, 1 patient)
Cardiac arrest (grade 5, 1 patient)
Fatigue (2%)
Thrombocytopenia (2%)
Diarrhea (2%)
Other AEs:
Diarrhea (serious, 3%)
Dehydration (serious, 2%)
Herpes zoster (serious, 2%)
Pyrexia (serious, 2%)
Nausea (serious, 2%)
Vomiting (serious, 2%)
Dyspnea (serious, 2%)
Thrombocytopenia (serious, 2%)
Constipation (grade 3, 2%)
Anorexia (grade 3, 2%)
Paresthesia (grade 3, 2%)
Anaemia NOS (grade 3, 6%)
Anaemia NOS (grade 4, <1%)
Headache (grade 3, <1%)
Neutropenia (grade 3, 11%)
Neutropenia (grade 4, 2%)
Rash NOS (grade 3, <1%)
Abdominal pain (grade 3, 2%)
Weakness (grade 3, 3%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Fatigue grade 3, 1 patient
DLT
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Sensory neuropathy grade 3, 1 patient
DLT
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Thrombocytopenia grade 3, 1 patient
DLT
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Acidosis grade 3-4
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Alanine aminotransferase increase grade 3-4
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Blood bicarbonate low grade 3-4
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
CPK increased grade 3-4
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Hypokalemia grade 3-4
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Diarrhea grade 3-4, 1 patient
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Hypotension grade 3-4, 1 patient
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Hypoxia grade 3-4, 1 patient
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Infection grade 3-4, 1 patient
1.9 mg/m2 2 times / week steady, intravenous
Highest studied dose
Dose: 1.9 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.9 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Thrombocytopenia all grades, 5 patients
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Abdominal pain grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Constipation grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Depressed level of consciousness grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Fatigue grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Headache grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Hypokalemia grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Pain grade 3, 1 patient
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Sensory neuropathy grade 3, 3 patients
1.7 mg/m2 2 times / week steady, intravenous
MTD
Dose: 1.7 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.7 mg/m2, 2 times / week
Sources:
unhealthy, 52 years (range: 26–85 years)
n = 33
Health Status: unhealthy
Condition: recurrent malignant glioma
Age Group: 52 years (range: 26–85 years)
Sex: M+F
Population Size: 33
Sources:
Constipation grade 3, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Pyrexia grade 3, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Rash grade 3, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Anemia grade 3, 12%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Peripheral neuropathy grade 3, 12%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Lymphopenia grade 3, 14%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Thrombocytopenia grade 3, 18%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Leukopenia grade 3, 19%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Anorexia grade 3, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Paresthesia grade 3, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Herpes zoster grade 3, 3%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Nausea grade 3, 3%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Neutropenia grade 3, 30%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Vomiting grade 3, 4%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Asthenia grade 3, 5%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Diarrhea grade 3, 6%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Fatigue grade 3, 6%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Neuralgia grade 3, 8%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Insomnia grade 3, < 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Abdominal pain upper grade 3, <1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Anemia grade 4-5, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Diarrhea grade 4-5, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Fatigue grade 4-5, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Neuralgia grade 4-5, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Peripheral neuropathy grade 4-5, 1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Neutropenia grade 4-5, 10%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Thrombocytopenia grade 4-5, 17%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Leukopenia grade 4-5, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Lymphopenia grade 4-5, 5%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Co-administed with::
melphalan(9 mg/m2)
prednisone(60 mg/m2)
Sources:
unhealthy, 71 years (range: 48 - 91 years)
n = 340
Health Status: unhealthy
Condition: multiple myeloma
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
Population Size: 340
Sources:
Hypotension 1%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: multiple myeloma |mantle cell lymphoma
Sex: M+F
Population Size: 331
Sources:
Asthenia < 1%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: multiple myeloma |mantle cell lymphoma
Sex: M+F
Population Size: 331
Sources:
Pyrexia < 1%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: multiple myeloma |mantle cell lymphoma
Sex: M+F
Population Size: 331
Sources:
Weakness < 1%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: multiple myeloma |mantle cell lymphoma
Sex: M+F
Population Size: 331
Sources:
Diarrhea 2%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Fatigue 2%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Thrombocytopenia 2%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Peripheral neuropathy 8%
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Neutropenia grade 3, 11%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Abdominal pain grade 3, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Anorexia grade 3, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Constipation grade 3, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Paresthesia grade 3, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Weakness grade 3, 3%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Anaemia NOS grade 3, 6%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Headache grade 3, <1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Rash NOS grade 3, <1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Neutropenia grade 4, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Anaemia NOS grade 4, <1%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Cardiac arrest grade 5, 1 patient
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Cardiogenic shock grade 5, 1 patient
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Congestive heart failure grade 5, 1 patient
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Respiratory insufficiency grade 5, 1 patient
Disc. AE
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Dehydration serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Dyspnea serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Herpes zoster serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Nausea serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Pyrexia serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Thrombocytopenia serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Vomiting serious, 2%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Diarrhea serious, 3%
1.3 mg/m2 2 times / week steady, intravenous
Recommended
Dose: 1.3 mg/m2, 2 times / week
Route: intravenous
Route: steady
Dose: 1.3 mg/m2, 2 times / week
Sources:
unhealthy
n = 331
Health Status: unhealthy
Condition: relapsed multiple myeloma
Sex: M+F
Population Size: 331
Sources:
Overview

OverviewOther

Drug as perpetrator​Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
The proteasome inhibitor PS-341 overcomes TRAIL resistance in Bax and caspase 9-negative or Bcl-xL overexpressing cells.
2003 Aug 7
Molecular mechanisms mediating antimyeloma activity of proteasome inhibitor PS-341.
2003 Feb 15
The proteasome inhibitor bortezomib interacts synergistically with histone deacetylase inhibitors to induce apoptosis in Bcr/Abl+ cells sensitive and resistant to STI571.
2003 Nov 15
[Treatment with a proteasome inhibitor, bortezomib, for thalidomide-resistant multiple myeloma].
2004 Feb
Proteasome inhibition sensitizes non-small cell lung cancer to histone deacetylase inhibitor-induced apoptosis through the generation of reactive oxygen species.
2004 Nov
Proteasome inhibitor PS-341 induces apoptosis through induction of endoplasmic reticulum stress-reactive oxygen species in head and neck squamous cell carcinoma cells.
2004 Nov
Antitumor effects of bortezomib (PS-341) on primary effusion lymphomas.
2004 Oct
Novel biological therapies for the treatment of multiple myeloma.
2005
Reduction in BCL-2 levels by 26S proteasome inhibition with bortezomib is associated with induction of apoptosis in small cell lung cancer.
2005 Aug
A phase II trial with pharmacodynamic endpoints of the proteasome inhibitor bortezomib in patients with metastatic colorectal cancer.
2005 Aug 1
New treatments for multiple myeloma.
2005 Dec
Sensitization of DNA damage-induced apoptosis by the proteasome inhibitor PS-341 is p53 dependent and involves target proteins 14-3-3sigma and survivin.
2005 Dec
Bortezomib, a novel proteasome inhibitor, in the treatment of hematologic malignancies.
2005 Dec
Bortezomib sensitizes pancreatic cancer cells to endoplasmic reticulum stress-mediated apoptosis.
2005 Dec 15
Bortezomib-induced severe hepatitis in multiple myeloma: a case report.
2005 Feb 28
Efficacy and mechanism of action of the proteasome inhibitor PS-341 in T-cell lymphomas and HTLV-I associated adult T-cell leukemia/lymphoma.
2005 Jan 13
Sulindac enhances the proteasome inhibitor bortezomib-mediated oxidative stress and anticancer activity.
2005 Jul 15
New biological agents in the treatment of advanced non-small cell lung cancer.
2005 Jun
Human metabolism of the proteasome inhibitor bortezomib: identification of circulating metabolites.
2005 Jun
Bortezomib abolishes tumor necrosis factor-related apoptosis-inducing ligand resistance via a p21-dependent mechanism in human bladder and prostate cancer cells.
2005 Jun 1
Serum amyloid A-luciferase transgenic mice: response to sepsis, acute arthritis, and contact hypersensitivity and the effects of proteasome inhibition.
2005 Jun 15
NF-kappaB and not the MAPK signaling pathway regulates GADD45beta expression during acute inflammation.
2005 Jun 3
Predominant Bcl-XL knockdown disables antiapoptotic mechanisms: tumor necrosis factor-related apoptosis-inducing ligand-based triple chemotherapy overcomes chemoresistance in pancreatic cancer cells in vitro.
2005 Mar 15
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
PS-341 (bortezomib) induces lysosomal cathepsin B release and a caspase-2-dependent mitochondrial permeabilization and apoptosis in human pancreatic cancer cells.
2006 Apr 28
Bortezomib (PS-341, Velcade) increases the efficacy of trastuzumab (Herceptin) in HER-2-positive breast cancer cells in a synergistic manner.
2006 Dec
Bortezomib-dexamethasone combination in a patient with refractory multiple myeloma and impaired renal function.
2006 Jun
Proteasome inhibitor PS-341 induces apoptosis in cisplatin-resistant squamous cell carcinoma cells by induction of Noxa.
2006 Oct 20
A novel bioluminescent mouse model and effective therapy for adult T-cell leukemia/lymphoma.
2007 Dec 15
A phase I and pharmacologic study of sequences of the proteasome inhibitor, bortezomib (PS-341, Velcade), in combination with paclitaxel and carboplatin in patients with advanced malignancies.
2007 Feb
Arsenic trioxide and proteasome inhibitor bortezomib synergistically induce apoptosis in leukemic cells: the role of protein kinase Cdelta.
2007 Jul
The proteasome inhibitor PS-341 (bortezomib) up-regulates DR5 expression leading to induction of apoptosis and enhancement of TRAIL-induced apoptosis despite up-regulation of c-FLIP and survivin expression in human NSCLC cells.
2007 May 15
Bortezomib induces apoptosis in T-cell prolymphocytic leukemia (T-PLL).
2007 Nov
Novel therapies in myeloma.
2007 Nov
The proteasome inhibitor bortezomib induces apoptosis in human retinoblastoma cell lines in vitro.
2007 Oct
Predictive value of alkaline phosphatase for response and time to progression in bortezomib-treated multiple myeloma patients.
2007 Sep
Synergistic interaction of the histone deacetylase inhibitor SAHA with the proteasome inhibitor bortezomib in mantle cell lymphoma.
2008 Feb
Bortezomib induces caspase-dependent apoptosis in Hodgkin lymphoma cell lines and is associated with reduced c-FLIP expression: a gene expression profiling study with implications for potential combination therapies.
2008 Feb
Patents

Sample Use Guides

1.3 mg/m2 administered as a 3 to 5 second bolus.
Route of Administration: Intravenous
Fifty % growth inhibition (IC50) in U266, IM-9, and Hs Sultan (multiple myeloma) cells was noted at concentrations of 0.003, 0.006, or 0.02 × 10−6 M, respectively.
Substance Class Chemical
Created
by admin
on Wed Jul 05 23:20:09 UTC 2023
Edited
by admin
on Wed Jul 05 23:20:09 UTC 2023
Record UNII
69G8BD63PP
Record Status Validated (UNII)
Record Version
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Name Type Language
BORTEZOMIB
EMA EPAR   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
BORTEZOMIB [USAN]
Common Name English
PS-341
Code English
BORTEZOMIB [VANDF]
Common Name English
BORTEZOMIB ACCORD
Brand Name English
Bortezomib [WHO-DD]
Common Name English
BORTEZOMIB [ORANGE BOOK]
Common Name English
BORTEZOMIB [MART.]
Common Name English
NSC-681239
Code English
LDP-341
Code English
BORTEZOMIB [HSDB]
Common Name English
BORTEZOMIB [MI]
Common Name English
VELCADE
Brand Name English
BORONIC ACID, ((1R)-3-METHYL-1-(((2S)-1-OXO-3-PHENYL-2-((PYRAZINYLCARBONYL)AMINO)PROPYL)AMINO)BUTYL)-
Common Name English
[(1R)-3-Methyl-1-[[(2S)-3-phenyl-2-[(pyrazinylcarbonyl)amino]propanoyl]amino]butyl]boronic acid
Systematic Name English
N-((1S)-1-BENZYL-2-(((1R)-1-(DIHYDROXYBORANYL)-3-METHYLBUTYL)AMINO)-2-OXOETHYL)PYRAZINECARBOXAMIDE
Systematic Name English
BORTEZOMIB HYDRATE [JAN]
Common Name English
BORTEZOMIB [JAN]
Common Name English
bortezomib [INN]
Common Name English
BORTEZOMIB [EMA EPAR]
Common Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS VELCADE (AUTHORIZED: MULTIPLE MYELOMA)
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
FDA ORPHAN DRUG 525816
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
NCI_THESAURUS C2160
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
NDF-RT N0000175604
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
FDA ORPHAN DRUG 464014
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
WHO-VATC QL01XX32
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
FDA ORPHAN DRUG 226106
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
WHO-ATC L01XX32
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
FDA ORPHAN DRUG 328610
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
LIVERTOX NBK548027
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
EMA ASSESSMENT REPORTS BORTEZOMIB ACCORD (AUTHORIZED: MULTIPLE MYELOMA)
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
NDF-RT N0000175075
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
FDA ORPHAN DRUG 163002
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
Code System Code Type Description
CAS
179324-69-7
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
INN
8331
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
PUBCHEM
387447
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
DAILYMED
69G8BD63PP
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
CAS
1610526-91-4
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
ALTERNATIVE
MESH
C400082
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
WIKIPEDIA
BORTEZOMIB
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
NCI_THESAURUS
C1851
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
SMS_ID
100000091450
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
IUPHAR
6391
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
EPA CompTox
DTXSID3040980
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
DRUG CENTRAL
391
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
FDA UNII
69G8BD63PP
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
CHEBI
52717
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
ChEMBL
CHEMBL325041
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
RXCUI
358258
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY RxNorm
USAN
OO-13
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
DRUG BANK
DB00188
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
EVMPD
SUB20020
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
HSDB
7666
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
MERCK INDEX
M2623
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY Merck Index
NSC
681239
Created by admin on Wed Jul 05 23:20:09 UTC 2023 , Edited by admin on Wed Jul 05 23:20:09 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
caspase-like
REVERSIBLE
IC50
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
trypsin-like.
REVERSIBLE
IC50
TARGET -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
chymotrypsin-like
IC50
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
PRODRUG -> METABOLITE ACTIVE
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
PRODRUG -> METABOLITE ACTIVE
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC