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

Details

Stereochemistry ABSOLUTE
Molecular Formula C19H25BN4O4
Molecular Weight 384.238
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])(B(O)O)N=C([C@]([H])(Cc1ccccc1)N=C(c2cnccn2)O)O

InChI

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

HIDE SMILES / InChI

Molecular Formula C19H25BN4O4
Molecular Weight 384.238
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: 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.

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
0.599999999999999978 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

1052784000000
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

1052784000000
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
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
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 52 years (range: 26–85 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
Sources:
unhealthy, 71 years (range: 48 - 91 years)
Health Status: unhealthy
Age Group: 71 years (range: 48 - 91 years)
Sex: M+F
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Overview

OverviewOther

Drug as perpetrator​Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
New treatments for multiple myeloma.
2005 Dec
Sensitization of DNA damage-induced apoptosis by the proteasome inhibitor PS-341 is p53 dependent and involves target proteins 14-3-3sigma and survivin.
2005 Dec
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
[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
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
Bortezomib-dexamethasone combination in a patient with refractory multiple myeloma and impaired renal function.
2006 Jun
Inhibition of p38alpha MAPK enhances proteasome inhibitor-induced apoptosis of myeloma cells by modulating Hsp27, Bcl-X(L), Mcl-1 and p53 levels in vitro and inhibits tumor growth in vivo.
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
The combination of the proteasome inhibitor bortezomib and the bcl-2 antisense molecule oblimersen sensitizes human B-cell lymphomas to cyclophosphamide.
2006 May 1
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
[Apoptosis of myeloid leukemia cell line HL60 induced by Bortezomib, a proteasome inhibitor].
2006 Sep 12
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
TRAIL therapy in non-small cell lung cancer cells: sensitization to death receptor-mediated apoptosis by proteasome inhibitor bortezomib.
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
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
Bortezomib-associated cutaneous vasculitis.
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
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
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 induces caspase-dependent apoptosis in Hodgkin lymphoma cell lines and is associated with reduced c-FLIP expression: a gene expression profiling study with implications for potential combination therapies.
2008 Feb
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
by admin
on Sat Jun 26 12:20:31 UTC 2021
Edited
by admin
on Sat Jun 26 12:20:31 UTC 2021
Record UNII
69G8BD63PP
Record Status Validated (UNII)
Record Version
  • Download
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 [ORANGE BOOK]
Common Name English
BORTEZOMIB [WHO-DD]
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 Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
FDA ORPHAN DRUG 525816
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
NCI_THESAURUS C2160
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
NDF-RT N0000175604
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
WHO-VATC QL01XX32
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
FDA ORPHAN DRUG 328610
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
FDA ORPHAN DRUG 226106
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
WHO-ATC L01XX32
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
FDA ORPHAN DRUG 464014
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
LIVERTOX 118
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
EMA ASSESSMENT REPORTS BORTEZOMIB ACCORD (AUTHORIZED: MULTIPLE MYELOMA)
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
NDF-RT N0000175075
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
FDA ORPHAN DRUG 163002
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
Code System Code Type Description
CAS
179324-69-7
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
INN
8331
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
PUBCHEM
387447
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
CAS
1610526-91-4
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
ALTERNATIVE
MESH
C400082
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
WIKIPEDIA
BORTEZOMIB
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
NCI_THESAURUS
C1851
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
IUPHAR
6391
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
EPA CompTox
179324-69-7
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
DRUG CENTRAL
391
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
FDA UNII
69G8BD63PP
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
ChEMBL
CHEMBL325041
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
RXCUI
358258
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY RxNorm
DRUG BANK
DB00188
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
EVMPD
SUB20020
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
HSDB
7666
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY
MERCK INDEX
M2623
Created by admin on Sat Jun 26 12:20:32 UTC 2021 , Edited by admin on Sat Jun 26 12:20:32 UTC 2021
PRIMARY Merck Index
Related Record Type Details
TARGET -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
caspase-like
REVERSIBLE
IC50
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
trypsin-like.
REVERSIBLE
IC50
TARGET -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
chymotrypsin-like
IC50
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
PRODRUG -> METABOLITE ACTIVE
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC