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Details

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

SHOW SMILES / InChI
Structure of Bortezomib

SMILES

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

InChI

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

HIDE SMILES / InChI

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

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

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

CNS Activity

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

Originator

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.6 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VELCADE

Approved Use

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

Launch Date

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
127.02 ng/mL
1.3 mg/m² 2 times / week multiple, intravenous
dose: 1.3 mg/m²
route of administration: intravenous
experiment type: MULTIPLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
106.2 ng/mL
1 mg/m² 2 times / week multiple, intravenous
dose: 1 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
BORTEZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
112 ng/mL
1.3 mg/m² single, intravenous
dose: 1.3 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
349.62 ng*h/mL
1.3 mg/m² 2 times / week multiple, intravenous
dose: 1.3 mg/m²
route of administration: intravenous
experiment type: MULTIPLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
82.8 ng × h/mL
1 mg/m² 2 times / week multiple, intravenous
dose: 1 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
BORTEZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
51.55 h
1.3 mg/m² 2 times / week multiple, intravenous
dose: 1.3 mg/m²
route of administration: intravenous
experiment type: MULTIPLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
78.9 h
1 mg/m² 2 times / week multiple, intravenous
dose: 1 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
BORTEZOMIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
17%
1.3 mg/m² single, intravenous
dose: 1.3 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
BORTEZOMIB plasma
Homo sapiens
population: UNHEALTHY
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: 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:
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:
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:
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
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
Overview

OverviewOther

Drug as perpetrator​Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Development of the proteasome inhibitor Velcade (Bortezomib).
2004
Treatment of human chronic lymphocytic leukemia cells with the proteasome inhibitor bortezomib promotes apoptosis.
2004 Aug
Synergistic effect of histone deacetylase inhibitors FK228 and m-carboxycinnamic acid bis-hydroxamide with proteasome inhibitors PSI and PS-341 against gastrointestinal adenocarcinoma cells.
2004 Jun 1
Proteasome inhibition sensitizes non-small cell lung cancer to histone deacetylase inhibitor-induced apoptosis through the generation of reactive oxygen species.
2004 Nov
Proteasome inhibitor PS-341 induces apoptosis through induction of endoplasmic reticulum stress-reactive oxygen species in head and neck squamous cell carcinoma cells.
2004 Nov
Tumour lysis syndrome in multiple myeloma after bortezomib (VELCADE) administration.
2004 Oct
Antitumor effects of bortezomib (PS-341) on primary effusion lymphomas.
2004 Oct
Novel biological therapies for the treatment of multiple myeloma.
2005
Reduction in BCL-2 levels by 26S proteasome inhibition with bortezomib is associated with induction of apoptosis in small cell lung cancer.
2005 Aug
Perspectives for combination therapy to overcome drug-resistant multiple myeloma.
2005 Aug
A phase II trial with pharmacodynamic endpoints of the proteasome inhibitor bortezomib in patients with metastatic colorectal cancer.
2005 Aug 1
New treatments for multiple myeloma.
2005 Dec
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
Bortezomib-induced severe hepatitis in multiple myeloma: a case report.
2005 Feb 28
Efficacy and mechanism of action of the proteasome inhibitor PS-341 in T-cell lymphomas and HTLV-I associated adult T-cell leukemia/lymphoma.
2005 Jan 13
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
Human metabolism of the proteasome inhibitor bortezomib: identification of circulating metabolites.
2005 Jun
Bortezomib abolishes tumor necrosis factor-related apoptosis-inducing ligand resistance via a p21-dependent mechanism in human bladder and prostate cancer cells.
2005 Jun 1
Serum amyloid A-luciferase transgenic mice: response to sepsis, acute arthritis, and contact hypersensitivity and the effects of proteasome inhibition.
2005 Jun 15
NF-kappaB and not the MAPK signaling pathway regulates GADD45beta expression during acute inflammation.
2005 Jun 3
Predominant Bcl-XL knockdown disables antiapoptotic mechanisms: tumor necrosis factor-related apoptosis-inducing ligand-based triple chemotherapy overcomes chemoresistance in pancreatic cancer cells in vitro.
2005 Mar 15
Severe irreversible bilateral hearing loss after bortezomib (VELCADE) therapy in a multiple myeloma (MM) patient.
2005 May
PS-341 (bortezomib) induces lysosomal cathepsin B release and a caspase-2-dependent mitochondrial permeabilization and apoptosis in human pancreatic cancer cells.
2006 Apr 28
Bortezomib inhibits docetaxel-induced apoptosis via a p21-dependent mechanism in human prostate cancer cells.
2006 Aug
Bortezomib 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
Activation of sterile20-like kinase 1 in proteasome inhibitor bortezomib-induced apoptosis in oncogenic K-ras-transformed cells.
2006 Jun 15
Bortezomib induces selective depletion of alloreactive T lymphocytes and decreases the production of Th1 cytokines.
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
Proteasome inhibitor PS-341 induces apoptosis in cisplatin-resistant squamous cell carcinoma cells by induction of Noxa.
2006 Oct 20
Cytotoxic synergy between the multikinase inhibitor sorafenib and the proteasome inhibitor bortezomib in vitro: induction of apoptosis through Akt and c-Jun NH2-terminal kinase pathways.
2006 Sep
[Apoptosis of myeloid leukemia cell line HL60 induced by Bortezomib, a proteasome inhibitor].
2006 Sep 12
A novel bioluminescent mouse model and effective therapy for adult T-cell leukemia/lymphoma.
2007 Dec 15
SAHA induces apoptosis in hepatoma cells and synergistically interacts with the proteasome inhibitor Bortezomib.
2007 Jul
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
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
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 Mon Mar 31 18:11:16 GMT 2025
Edited
by admin
on Mon Mar 31 18:11:16 GMT 2025
Record UNII
69G8BD63PP
Record Status Validated (UNII)
Record Version
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Name Type Language
BORTEZOMIB ACCORD
Preferred Name English
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 [WHO-DD]
Common Name English
BORTEZOMIB [ORANGE BOOK]
Common Name English
BORTEZOMIB [MART.]
Common Name English
NSC-681239
Code English
LDP-341
Code English
BORTEZOMIB [HSDB]
Common Name English
BORTEZOMIB [MI]
Common Name English
VELCADE
Brand Name English
BORONIC ACID, ((1R)-3-METHYL-1-(((2S)-1-OXO-3-PHENYL-2-((PYRAZINYLCARBONYL)AMINO)PROPYL)AMINO)BUTYL)-
Common Name English
[(1R)-3-Methyl-1-[[(2S)-3-phenyl-2-[(pyrazinylcarbonyl)amino]propanoyl]amino]butyl]boronic acid
Systematic Name English
N-((1S)-1-BENZYL-2-(((1R)-1-(DIHYDROXYBORANYL)-3-METHYLBUTYL)AMINO)-2-OXOETHYL)PYRAZINECARBOXAMIDE
Systematic Name English
BORTEZOMIB HYDRATE [JAN]
Common Name English
BORTEZOMIB [JAN]
Common Name English
bortezomib [INN]
Common Name English
BORTEZOMIB [EMA EPAR]
Common Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS VELCADE (AUTHORIZED: MULTIPLE MYELOMA)
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
FDA ORPHAN DRUG 525816
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
NCI_THESAURUS C2160
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
NDF-RT N0000175604
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
FDA ORPHAN DRUG 464014
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
WHO-VATC QL01XX32
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
FDA ORPHAN DRUG 226106
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
WHO-ATC L01XX32
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
FDA ORPHAN DRUG 328610
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
LIVERTOX NBK548027
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
EMA ASSESSMENT REPORTS BORTEZOMIB ACCORD (AUTHORIZED: MULTIPLE MYELOMA)
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
NDF-RT N0000175075
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
FDA ORPHAN DRUG 163002
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
Code System Code Type Description
CAS
179324-69-7
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
INN
8331
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
PUBCHEM
387447
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
DAILYMED
69G8BD63PP
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
CAS
1610526-91-4
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
ALTERNATIVE
MESH
C400082
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
WIKIPEDIA
BORTEZOMIB
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
NCI_THESAURUS
C1851
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
SMS_ID
100000091450
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
IUPHAR
6391
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
EPA CompTox
DTXSID3040980
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
DRUG CENTRAL
391
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
FDA UNII
69G8BD63PP
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
CHEBI
52717
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
ChEMBL
CHEMBL325041
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
RXCUI
358258
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY RxNorm
USAN
OO-13
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
DRUG BANK
DB00188
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
EVMPD
SUB20020
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
HSDB
7666
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
MERCK INDEX
m2623
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY Merck Index
NSC
681239
Created by admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
caspase-like
REVERSIBLE
IC50
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
trypsin-like.
REVERSIBLE
IC50
TARGET -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
chymotrypsin-like
IC50
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
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METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
PRODRUG -> METABOLITE ACTIVE
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
PRODRUG -> METABOLITE ACTIVE
METABOLITE -> PARENT
MINOR
PLASMA
METABOLITE -> PARENT
MINOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC