Bortezomib

Generic Name: Bortezomib

Brand Names: Velcade, Bortezomib Accord, Bortezomib Hospira, Bortezomib Fresenius Kabi, Bortezomib Sun

Drug Type: Small Molecule

Chemical Formula: C_₁₉H_₂₅BN_₄O_₄

CAS Number: 179324-69-7

Unique Ingredient Identifier: 69G8BD63PP

Background: Bortezomib is a dipeptide boronic acid derivative and proteasome inhibitor used to treat multiple myeloma and mantle cell lymphoma. The 26S proteasome is a protein complex that degrades ubiquitinated proteins in the ubiquitin-proteasome pathway: reversible inhibition of the 26S proteasome, leading to cell cycle arrest and apoptosis of cancer cells, is thought to be the main mechanism of action of bortezomib. However, multiple mechanisms may be involved in the anticancer activity of bortezomib.

Bortezomib was first synthesized in 1995. In May 2003, bortezomib became the first anticancer proteasome inhibitor that was approved by the FDA under the trade name VELCADE. Phase I, II, III, and IV clinical trials are undergoing to investigate the therapeutic efficacy of bortezomib in leukemia, myasthenia gravis, systemic lupus erythematosus, rheumatoid arthritis, and solid tumours.

Indication: Bortezomib is indicated for the treatment of adults with multiple myeloma or mantle cell lymphoma.

Associated Conditions: Mantle Cell Lymphoma (MCL), Multiple Myeloma (MM)

Associated Therapies: -

Clinical Trials

PS-341 in Treating Patients With Refractory or Relapsed Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia, Chronic Myeloid Leukemia in Blast Phase, or Myelodysplastic Syndrome

Phase 1

Completed

Conditions: Adult Acute Promyelocytic Leukemia (M3)
Blastic Phase Chronic Myelogenous Leukemia
Previously Treated Myelodysplastic Syndromes
Recurrent Adult Acute Lymphoblastic Leukemia
Recurrent Adult Acute Myeloid Leukemia
Refractory Anemia With Excess Blasts
Refractory Anemia With Excess Blasts in Transformation
Relapsing Chronic Myelogenous Leukemia

Interventions: Drug: bortezomib

First Posted Date: 2004-02-02

Last Posted Date: 2013-01-23

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 30

Registration Number: NCT00005064

Locations: 🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States

Gemcitabine, Carboplatin, and Bortezomib in Advanced or Recurrent Non-Small Cell Lung Cancer

Phase 2

Completed

Conditions: Recurrent Non-small Cell Lung Cancer
Stage IIIB Non-small Cell Lung Cancer
Stage IV Non-small Cell Lung Cancer

Interventions: Drug: gemcitabine hydrochloride
Drug: carboplatin
Drug: bortezomib

First Posted Date: 2004-01-13

Last Posted Date: 2013-02-28

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 99

Registration Number: NCT00075751

Locations: 🇺🇸
Southwest Oncology Group, San Antonio, Texas, United States

Bortezomib in Treating Patients With Newly Diagnosed Multiple Myeloma

Phase 2

Completed

Conditions: Stage I Multiple Myeloma
Stage II Multiple Myeloma
Stage III Multiple Myeloma

Interventions: Drug: bortezomib
Other: laboratory biomarker analysis

First Posted Date: 2004-01-13

Last Posted Date: 2014-06-02

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 44

Registration Number: NCT00075881

Locations: 🇺🇸
Eastern Cooperative Oncology Group, Boston, Massachusetts, United States

Bortezomib in Treating Patients With Unresectable or Metastatic Gastric Cancer or Gastroesophageal Junction Adenocarcinoma

Phase 2

Completed

Conditions: Gastric Cancer

First Posted Date: 2003-12-11

Last Posted Date: 2012-02-14

Lead Sponsor: Memorial Sloan Kettering Cancer Center

Registration Number: NCT00074009

Locations: 🇺🇸
Queens Cancer Center of Queens Hospital, Jamaica, New York, United States
🇺🇸
University of Chicago Cancer Research Center, Chicago, Illinois, United States
🇺🇸
University of Wisconsin Comprehensive Cancer Center, Madison, Wisconsin, United States

and more 1 locations

Phase II Trial Of PS-341 (Bortezomib) In Patients With Previously Treated Advanced Urothelial Tract Transitional Cell Carcinoma

Phase 2

Completed

Conditions: Metastatic Transitional Cell Cancer of the Renal Pelvis and Ureter
Recurrent Bladder Cancer
Recurrent Transitional Cell Cancer of the Renal Pelvis and Ureter
Recurrent Urethral Cancer
Stage III Bladder Cancer
Stage III Urethral Cancer
Stage IV Bladder Cancer
Stage IV Urethral Cancer
Transitional Cell Carcinoma of the Bladder
Ureter Cancer

Interventions: Drug: bortezomib

First Posted Date: 2003-11-06

Last Posted Date: 2013-06-05

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 40

Registration Number: NCT00072150

Locations: 🇺🇸
UCSF-Mount Zion, San Francisco, California, United States

Bortezomib in Treating Patients With Recurrent or Refractory Extensive-Stage Small Cell Lung Cancer Previously Treated With Platinum-Based Chemotherapy

Phase 2

Completed

Conditions: Lung Cancer

First Posted Date: 2003-09-11

Last Posted Date: 2013-06-24

Lead Sponsor: SWOG Cancer Research Network

Registration Number: NCT00068289

Locations: 🇺🇸
Cardinal Bernardin Cancer Center at Loyola University Medical Center, Maywood, Illinois, United States
🇺🇸
CCOP - Central Illinois, Decatur, Illinois, United States
🇺🇸
Providence Cancer Institute at Providence Hospital, Southfield, Michigan, United States

and more 88 locations

A Dose Finding Phase I Trial of the Combination of Topotecan and PS-341, a Novel Proteasome Inhibitor, in Advanced Malignancies

Phase 1

Completed

Conditions: Unspecified Adult Solid Tumor, Protocol Specific

Interventions: Drug: topotecan hydrochloride
Drug: bortezomib
Other: pharmacological study
Other: laboratory biomarker analysis

First Posted Date: 2003-09-11

Last Posted Date: 2013-02-01

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 25

Registration Number: NCT00068484

Locations: 🇺🇸
Yale University, New Haven, Connecticut, United States

Bortezomib and Fludarabine With or Without Rituximab in Treating Patients With Relapsed or Refractory Indolent Non-Hodgkin's Lymphoma or Chronic Lymphocytic Leukemia

Phase 1

Completed

Conditions: Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue
Hematopoietic/Lymphoid Cancer
Nodal Marginal Zone B-cell Lymphoma
Recurrent Adult Diffuse Small Cleaved Cell Lymphoma
Recurrent Grade 1 Follicular Lymphoma
Recurrent Grade 2 Follicular Lymphoma
Recurrent Mantle Cell Lymphoma
Recurrent Marginal Zone Lymphoma
Recurrent Small Lymphocytic Lymphoma
Refractory Chronic Lymphocytic Leukemia

Interventions: Drug: bortezomib
Drug: fludarabine phosphate
Biological: rituximab

First Posted Date: 2003-09-11

Last Posted Date: 2013-09-30

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 18

Registration Number: NCT00068315

Locations: 🇺🇸
Mercy Medical Center, Canton, Ohio, United States
🇺🇸
Case Western Reserve University, Cleveland, Ohio, United States
🇺🇸
Seidman Cancer Center at University Hospitals Case Medical Center, Case Comprehensive Cancer Center, Cleveland, Ohio, United States

and more 4 locations