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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

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
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
The bortezomib/proteasome inhibitor PS-341 and triterpenoid CDDO-Im induce synergistic anti-multiple myeloma (MM) activity and overcome bortezomib resistance.
2004 Apr 15
Treatment of human chronic lymphocytic leukemia cells with the proteasome inhibitor bortezomib promotes apoptosis.
2004 Aug
Synergistic induction of oxidative injury and apoptosis in human multiple myeloma cells by the proteasome inhibitor bortezomib and histone deacetylase inhibitors.
2004 Jun 1
Induction of cell cycle arrest and apoptosis by the proteasome inhibitor PS-341 in Hodgkin disease cell lines is independent of inhibitor of nuclear factor-kappaB mutations or activation of the CD30, CD40, and RANK receptors.
2004 May 1
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
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
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
Sustained remission including marked regression of a paravertebral plasmacytoma in a patient with heavily pretreated, relapsed multiple myeloma after treatment with bortezomib.
2005 Dec
Bortezomib-induced severe hepatitis in multiple myeloma: a case report.
2005 Feb 28
Sulindac enhances the proteasome inhibitor bortezomib-mediated oxidative stress and anticancer activity.
2005 Jul 15
Differential regulation of noxa in normal melanocytes and melanoma cells by proteasome inhibition: therapeutic implications.
2005 Jul 15
Bortezomib therapy alone and in combination with dexamethasone for previously untreated symptomatic multiple myeloma.
2005 Jun
PAD combination therapy (PS-341/bortezomib, doxorubicin and dexamethasone) for previously untreated patients with multiple myeloma.
2005 Jun
Serum amyloid A-luciferase transgenic mice: response to sepsis, acute arthritis, and contact hypersensitivity and the effects of proteasome inhibition.
2005 Jun 15
Severe irreversible bilateral hearing loss after bortezomib (VELCADE) therapy in a multiple myeloma (MM) patient.
2005 May
Modulation of uridine phosphorylase gene expression by tumor necrosis factor-alpha enhances the antiproliferative activity of the capecitabine intermediate 5'-deoxy-5-fluorouridine in breast cancer cells.
2006 Apr
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 inhibits docetaxel-induced apoptosis via a p21-dependent mechanism in human prostate cancer cells.
2006 Aug
Bortezomib (PS-341, Velcade) increases the efficacy of trastuzumab (Herceptin) in HER-2-positive breast cancer cells in a synergistic manner.
2006 Dec
Anti-cancer effects of bortezomib against chemoresistant neuroblastoma cell lines in vitro and in vivo.
2006 Feb
Vitamin C inactivates the proteasome inhibitor PS-341 in human cancer cells.
2006 Jan 1
Bortezomib and depsipeptide sensitize tumors to tumor necrosis factor-related apoptosis-inducing ligand: a novel method to potentiate natural killer cell tumor cytotoxicity.
2006 Jul 15
The combination of the proteasome inhibitor bortezomib and the bcl-2 antisense molecule oblimersen sensitizes human B-cell lymphomas to cyclophosphamide.
2006 May 1
Bortezomib induces selective depletion of alloreactive T lymphocytes and decreases the production of Th1 cytokines.
2006 May 1
Severe reversible cardiac failure after bortezomib treatment combined with chemotherapy in a non-small cell lung cancer patient: a case report.
2006 May 11
Adaphostin and bortezomib induce oxidative injury and apoptosis in imatinib mesylate-resistant hematopoietic cells expressing mutant forms of Bcr/Abl.
2006 Oct
Histone deacetylase inhibitor trichostatin A and proteasome inhibitor PS-341 synergistically induce apoptosis in pancreatic cancer cells.
2006 Oct 6
Cytotoxic synergy between the multikinase inhibitor sorafenib and the proteasome inhibitor bortezomib in vitro: induction of apoptosis through Akt and c-Jun NH2-terminal kinase pathways.
2006 Sep
[Apoptosis of myeloid leukemia cell line HL60 induced by Bortezomib, a proteasome inhibitor].
2006 Sep 12
Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma.
2007 Apr
Quantitative sensory findings in patients with bortezomib-induced pain.
2007 Apr
A novel bioluminescent mouse model and effective therapy for adult T-cell leukemia/lymphoma.
2007 Dec 15
TRAIL/bortezomib cotreatment is potentially hepatotoxic but induces cancer-specific apoptosis within a therapeutic window.
2007 Mar
Bortezomib-induced peripheral neurotoxicity: a neurophysiological and pathological study in the rat.
2007 Mar
Proteasome inhibitors synergize with tumor necrosis factor-related apoptosis-induced ligand to induce anaplastic thyroid carcinoma cell death.
2007 May
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
Induction of heme oxygenase-1 by cobalt protoporphyrin enhances the antitumour effect of bortezomib in adult T-cell leukaemia cells.
2007 Oct 22
Predictive value of alkaline phosphatase for response and time to progression in bortezomib-treated multiple myeloma patients.
2007 Sep
Bortezomib sensitizes non-Hodgkin's lymphoma cells to apoptosis induced by antibodies to tumor necrosis factor related apoptosis-inducing ligand (TRAIL) receptors TRAIL-R1 and TRAIL-R2.
2007 Sep 15
Topoisomerase IIbeta mediated DNA double-strand breaks: implications in doxorubicin cardiotoxicity and prevention by dexrazoxane.
2007 Sep 15
Synergistic interaction of the histone deacetylase inhibitor SAHA with the proteasome inhibitor bortezomib in mantle cell lymphoma.
2008 Feb
CHOP transcription factor mediates IL-8 signaling in cystic fibrosis bronchial epithelial cells.
2008 Feb
Bortezomib is synergistic with rituximab and cyclophosphamide in inducing apoptosis of mantle cell lymphoma cells in vitro and in vivo.
2008 Jan
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.
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