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Details

Stereochemistry ABSOLUTE
Molecular Formula C25H35BN4O8
Molecular Weight 530.378
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BORTEZOMIB D-MANNITOL

SMILES

[H][C@@]1(OB(O[C@]1([H])[C@H](O)CO)[C@H](CC(C)C)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)C3=NC=CN=C3)[C@H](O)CO

InChI

InChIKey=QDMRNLRJDHCHLB-DNNBANOASA-N
InChI=1S/C25H35BN4O8/c1-15(2)10-21(26-37-22(19(33)13-31)23(38-26)20(34)14-32)30-24(35)17(11-16-6-4-3-5-7-16)29-25(36)18-12-27-8-9-28-18/h3-9,12,15,17,19-23,31-34H,10-11,13-14H2,1-2H3,(H,29,36)(H,30,35)/t17-,19+,20+,21-,22+,23+/m0/s1

HIDE SMILES / InChI

Molecular Formula C25H35BN4O8
Molecular Weight 530.378
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
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

2003
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

2003
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
Novel biological therapies for the treatment of multiple myeloma.
2005
Perspectives for combination therapy to overcome drug-resistant multiple myeloma.
2005 Aug
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 sensitizes pancreatic cancer cells to endoplasmic reticulum stress-mediated apoptosis.
2005 Dec 15
The combination of the farnesyl transferase inhibitor lonafarnib and the proteasome inhibitor bortezomib induces synergistic apoptosis in human myeloma cells that is associated with down-regulation of p-AKT.
2005 Dec 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
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
Mammalian target of rapamycin inhibitors activate the AKT kinase in multiple myeloma cells by up-regulating the insulin-like growth factor receptor/insulin receptor substrate-1/phosphatidylinositol 3-kinase cascade.
2005 Oct
N-(4-hydroxyphenyl)retinamide inhibits invasion, suppresses osteoclastogenesis, and potentiates apoptosis through down-regulation of I(kappa)B(alpha) kinase and nuclear factor-kappaB-regulated gene products.
2005 Oct 15
Aggresome disruption: a novel strategy to enhance bortezomib-induced apoptosis in pancreatic cancer cells.
2006 Apr 1
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
[Salvage therapy with proteasome inhibitor bortezomib for relapsed and refractory multiple myeloma].
2006 Dec
Combination therapy with IFN-alpha plus bortezomib induces apoptosis and inhibits angiogenesis in human bladder cancer cells.
2006 Dec
The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status.
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
Bortezomib-dexamethasone combination in a patient with refractory multiple myeloma and impaired renal function.
2006 Jun
Activation of sterile20-like kinase 1 in proteasome inhibitor bortezomib-induced apoptosis in oncogenic K-ras-transformed cells.
2006 Jun 15
Crystal structure of the boronic acid-based proteasome inhibitor bortezomib in complex with the yeast 20S proteasome.
2006 Mar
Gallium-induced cell death in lymphoma: role of transferrin receptor cycling, involvement of Bax and the mitochondria, and effects of proteasome inhibition.
2006 Nov
Adaphostin and bortezomib induce oxidative injury and apoptosis in imatinib mesylate-resistant hematopoietic cells expressing mutant forms of Bcr/Abl.
2006 Oct
Proteasome inhibitor PS-341 induces apoptosis in cisplatin-resistant squamous cell carcinoma cells by induction of Noxa.
2006 Oct 20
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
Phase II study of single-agent bortezomib for the treatment of patients with fludarabine-refractory B-cell chronic lymphocytic leukemia.
2006 Sep 1
Complete remission and early relapse of refractory plasma cell leukemia after bortezomib induction and consolidation by HLA-mismatched unrelated allogeneic stem cell transplantation.
2007 Apr
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
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
SAHA induces apoptosis in hepatoma cells and synergistically interacts with the proteasome inhibitor Bortezomib.
2007 Jul
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
Resveratrol inhibits proliferation, induces apoptosis, and overcomes chemoresistance through down-regulation of STAT3 and nuclear factor-kappaB-regulated antiapoptotic and cell survival gene products in human multiple myeloma cells.
2007 Mar 15
Proteasome inhibitors synergize with tumor necrosis factor-related apoptosis-induced ligand to induce anaplastic thyroid carcinoma cell death.
2007 May
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
Capsaicin is a novel blocker of constitutive and interleukin-6-inducible STAT3 activation.
2007 May 15
The proteasome inhibitor bortezomib induces apoptosis in human retinoblastoma cell lines in vitro.
2007 Oct
Bortezomib induces apoptosis of Epstein-Barr virus (EBV)-transformed B cells and prolongs survival of mice inoculated with EBV-transformed B cells.
2007 Sep
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
Synergistic interaction of the histone deacetylase inhibitor SAHA with the proteasome inhibitor bortezomib in mantle cell lymphoma.
2008 Feb
Bortezomib is synergistic with rituximab and cyclophosphamide in inducing apoptosis of mantle cell lymphoma cells in vitro and in vivo.
2008 Jan
PS-341 (Bortezomib) inhibits proliferation and induces apoptosis of megakaryoblastic MO7-e cells.
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.
Substance Class Chemical
Created
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on Sat Dec 16 13:58:45 GMT 2023
Edited
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on Sat Dec 16 13:58:45 GMT 2023
Record UNII
P2AWN9VSQ6
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Name Type Language
BORTEZOMIB D-MANNITOL
Common Name English
BORTEZOMIB D-MANNITOL SYMMETRICAL ESTER
Common Name English
BORTEZOMIB D-MANNITOL ESTER
Common Name English
D-MANNITOL, CYCLIC 3,4-(B-((1R)-3-METHYL-1-(((2S)-1-OXO-3-PHENYL-2-((2-PYRAZINYLCARBONYL)AMINO)PROPYL)AMINO)BUTYL)BORONATE)
Common Name English
BORTEZOMIB MANNITOL BORONIC ESTER
Common Name English
Code System Code Type Description
SMS_ID
300000027876
Created by admin on Sat Dec 16 13:58:45 GMT 2023 , Edited by admin on Sat Dec 16 13:58:45 GMT 2023
PRIMARY
PUBCHEM
12990536
Created by admin on Sat Dec 16 13:58:45 GMT 2023 , Edited by admin on Sat Dec 16 13:58:45 GMT 2023
PRIMARY
FDA UNII
P2AWN9VSQ6
Created by admin on Sat Dec 16 13:58:45 GMT 2023 , Edited by admin on Sat Dec 16 13:58:45 GMT 2023
PRIMARY
CAS
444576-08-3
Created by admin on Sat Dec 16 13:58:45 GMT 2023 , Edited by admin on Sat Dec 16 13:58:45 GMT 2023
PRIMARY
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METABOLITE ACTIVE -> PRODRUG
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