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
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
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 |
DescriptionCurator'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
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
Sources: https://www.google.com/patents/US5780454
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2364701 |
0.6 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | VELCADE Approved UseVELCADE 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 Date1.052784E12 |
|||
Primary | VELCADE Approved UseVELCADE 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 Date1.052784E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
106.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20306195 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
82.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20306195 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
78.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20306195 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01801436 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17% |
BORTEZOMIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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) Other AEs:Sensory neuropathy (grade 3, 1 patient) Fatigue (grade 3, 1 patient) Diarrhea (grade 3-4, 1 patient) Sources: 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) |
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) Sources: 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) |
1.3 mg/m2 2 times / 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) Sources: prednisone(60 mg/m2) |
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%) Sources: 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%) |
1.3 mg/m2 2 times / 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%) Sources: Pyrexia (< 1%) Weakness (< 1%) Asthenia (< 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: |
Disc. AE: Peripheral neuropathy, Cardiogenic shock... Other AEs: Diarrhea, Dehydration... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (8%) Other AEs: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%) Diarrhea (serious, 3%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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) Sources: prednisone(60 mg/m2) |
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
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/23589314/ Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/29107984/ Page: - |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=11 Page: 11.0 |
weak [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=11 Page: 11.0 |
weak [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=11 Page: 11.0 |
weak [IC50 >30 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=11 Page: 11.0 |
weak [IC50 >30 uM] | |||
Page: - |
yes [IC50 18 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/29107984/ Page: - |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | yes (co-administration study) Comment: Co-administration of ketoconazole, a potent CYP3A inhibitor, increased theexposure of bortezomib. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=2 Page: 2.0 |
|||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=12 Page: 12.0 |
no | |||
yes | ||||
yes | ||||
yes | ||||
yes | no (co-administration study) Comment: Co-administration of omeprazole, a potent inhibitor of CYP2C19, had noeffect on the exposure of bortezomib. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21602_Velcade_biopharmr_P1.pdf#page=9 Page: 9.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
PubMed
Title | Date | PubMed |
---|---|---|
The proteasome inhibitor bortezomib interacts synergistically with histone deacetylase inhibitors to induce apoptosis in Bcr/Abl+ cells sensitive and resistant to STI571. | 2003 Nov 15 |
|
The bortezomib/proteasome inhibitor PS-341 and triterpenoid CDDO-Im induce synergistic anti-multiple myeloma (MM) activity and overcome bortezomib resistance. | 2004 Apr 15 |
|
The proteasome inhibitor bortezomib enhances the activity of docetaxel in orthotopic human pancreatic tumor xenografts. | 2004 Jan |
|
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 |
|
Antitumor effects of bortezomib (PS-341) on primary effusion lymphomas. | 2004 Oct |
|
Reduction in BCL-2 levels by 26S proteasome inhibition with bortezomib is associated with induction of apoptosis in small cell lung cancer. | 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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
Vitamin C inactivates the proteasome inhibitor PS-341 in human cancer cells. | 2006 Jan 1 |
|
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 |
|
[Apoptosis of myeloid leukemia cell line HL60 induced by Bortezomib, a proteasome inhibitor]. | 2006 Sep 12 |
|
Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma. | 2007 Apr |
|
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 |
|
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 |
|
Bortezomib-induced peripheral neurotoxicity: a neurophysiological and pathological study in the rat. | 2007 Mar |
|
Proteasome inhibitors synergize with tumor necrosis factor-related apoptosis-induced ligand to induce anaplastic thyroid carcinoma cell death. | 2007 May |
|
Bortezomib induces apoptosis in T-cell prolymphocytic leukemia (T-PLL). | 2007 Nov |
|
Novel therapies in myeloma. | 2007 Nov |
|
The proteasome inhibitor bortezomib induces apoptosis in human retinoblastoma cell lines in vitro. | 2007 Oct |
|
Bortezomib-associated cutaneous vasculitis. | 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 |
|
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 |
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PS-341 (Bortezomib) inhibits proliferation and induces apoptosis of megakaryoblastic MO7-e cells. | 2008 Jan |
Sample Use Guides
1.3 mg/m2 administered as a 3 to 5 second bolus.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11306489
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
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P2AWN9VSQ6
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Validated (UNII)
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12990536
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P2AWN9VSQ6
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444576-08-3
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METABOLITE ACTIVE -> PRODRUG |
Related Record | Type | Details | ||
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ACTIVE MOIETY |