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
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
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 |
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 Date2003 |
|||
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 Date2003 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
127.02 ng/mL CLINICAL TRIAL https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20306195 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
349.62 ng*h/mL CLINICAL TRIAL https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20306195 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
51.55 h CLINICAL TRIAL https://clinicaltrials.gov/ct2/show/NCT01801436 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20306195 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
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) 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) 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) 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) 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 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%) 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 Health Status: unhealthy Sex: M+F 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%) |
1.3 mg/m2 2 times / 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 Health Status: unhealthy Sex: M+F Sources: |
Disc. AE: Hypotension, Pyrexia... AEs leading to discontinuation/dose reduction: Hypotension (1%) Sources: Pyrexia (< 1%) Weakness (< 1%) Asthenia (< 1%) |
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) 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F Sources: |
Hypotension | 1% Disc. AE |
1.3 mg/m2 2 times / week steady, intravenous Recommended Dose: 1.3 mg/m2, 2 times / week Route: intravenous Route: steady Dose: 1.3 mg/m2, 2 times / week Sources: |
unhealthy Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 |
---|---|---|
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 |
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
Created
by
admin
on
Edited
Mon Mar 31 18:11:16 GMT 2025
by
admin
on
Mon Mar 31 18:11:16 GMT 2025
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Record UNII |
69G8BD63PP
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
---|---|---|---|---|
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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
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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
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||
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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Code System | Code | Type | Description | ||
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179324-69-7
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PRIMARY | |||
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8331
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PRIMARY | |||
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387447
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PRIMARY | |||
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69G8BD63PP
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PRIMARY | |||
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1610526-91-4
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ALTERNATIVE | |||
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C400082
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PRIMARY | |||
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BORTEZOMIB
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PRIMARY | |||
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C1851
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PRIMARY | |||
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100000091450
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PRIMARY | |||
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6391
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PRIMARY | |||
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DTXSID3040980
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PRIMARY | |||
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391
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admin on Mon Mar 31 18:11:16 GMT 2025 , Edited by admin on Mon Mar 31 18:11:16 GMT 2025
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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
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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
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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
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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
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PRIMARY | RxNorm | ||
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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
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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
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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
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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
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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
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PRIMARY | Merck Index | ||
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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
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
REVERSIBLE
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
caspase-like
REVERSIBLE
IC50
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR |
trypsin-like.
REVERSIBLE
IC50
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TARGET -> INHIBITOR |
REVERSIBLE
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
chymotrypsin-like
IC50
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
MINOR
PLASMA
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METABOLITE -> PARENT |
MINOR
PLASMA
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METABOLITE -> PARENT |
MINOR
PLASMA
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PRODRUG -> METABOLITE ACTIVE | |||
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METABOLITE -> PARENT |
MINOR
PLASMA
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METABOLITE -> PARENT |
MINOR
PLASMA
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METABOLITE -> PARENT |
MAJOR
PLASMA
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METABOLITE -> PARENT |
MAJOR
PLASMA
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METABOLITE -> PARENT |
MINOR
PLASMA
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PRODRUG -> METABOLITE ACTIVE | |||
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METABOLITE -> PARENT |
MINOR
PLASMA
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METABOLITE -> PARENT |
MINOR
PLASMA
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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