Evidence Grade A — Regulatory approved. 11566 published studies. 1000 registered clinical trials.
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Bortezomib (sold as Velcade) is a cancer treatment that fundamentally changed how multiple myeloma — a blood cancer of the bone marrow — is managed. It was the first drug in an entirely new class that works by blocking the cell's internal protein recycling system, causing cancer cells to essentially choke on their own waste. Before treatments like bortezomib, most myeloma patients survived about three years; many now live a decade or more.
Bortezomib is also known by these brand and alternate names:
11,566 published studies: 9090 human, 486 animal, 1735 in-vitro, 2076 reviews
Bortezomib is marketed as Velcade (approved May 2003) for multiple myeloma and mantle cell lymphoma. Generic versions are available. Originally given intravenously, subcutaneous injection is now preferred as it causes significantly less nerve damage.
The VISTA trial established bortezomib-based combination therapy as standard for newly diagnosed myeloma patients ineligible for transplant, with median time to disease progression of 24 months versus 16.6 months with older chemotherapy. Peripheral neuropathy (numbness and tingling in hands and feet) is the main dose-limiting side effect, affecting up to 30% of patients. Bortezomib transformed myeloma from a disease with a median survival of approximately 3 years to one where many patients live a decade or more with sequential treatments.
Like carfilzomib, bortezomib disables the proteasome — the cell's protein recycling system. Myeloma cells produce vast quantities of antibody proteins and rely heavily on the proteasome to dispose of defective copies. When bortezomib blocks the proteasome, these waste proteins accumulate rapidly, triggering a stress response that overwhelms the cancer cell. Bortezomib also blocks the NF-kappaB pathway, which myeloma cells use to resist self-destruction. Unlike carfilzomib's permanent bond, bortezomib's attachment is reversible, which may contribute to its different side effect profile.
Bortezomib has over 20 years of clinical data from dozens of large trials. The VISTA trial established bortezomib-based combination therapy as the standard approach for newly diagnosed myeloma patients, extending the time before disease worsened from about 17 months (with older chemotherapy) to 24 months. Both intravenous and subcutaneous injection routes are available, with subcutaneous now preferred because it significantly reduces the main dose-limiting side effect: peripheral neuropathy (numbness and tingling in hands and feet, affecting up to 30-40% of patients). While bortezomib remains a backbone of myeloma treatment worldwide, second-generation drugs in the same class (such as carfilzomib and ixazomib) offer different side effect profiles and are increasingly used alongside or instead of bortezomib for certain patient groups. Generic versions are now available, making it more accessible globally.
PeptideTrace tracks 1000 registered clinical trials for Bortezomib sourced from ClinicalTrials.gov.
A Study to Assess Two Different Strategies of Combining Dexamethasone and VELCADE
An Expanded Treatment Protocol of Panobinostat in Combination Therapy for Relapsed, and Relapsed and Refractory Multiple Myeloma
Technology Platform and System Construction of Clinical Evaluation Studies on New Drugs of Hematological Malignancy
GO-203-2C + Bortezomib For Relapsed Or Refractory MM
Early Patient Access Single Named Patient Program for the Use of Ulocuplumab for the Treatment of Multiple Myeloma
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Bortezomib is a modified dipeptidyl boronic acid, MW 384.24 Da. Pyrazinyl-Phe-Leu backbone with boronic acid pharmacophore forming reversible tetrahedral adduct with proteasome Thr-1. First proteasome inhibitor approved for cancer. IV push or SC at 1.3 mg/m2 Days 1,4,8,11 of 21-day cycles. Half-life 9-15 hours. SC produces equivalent efficacy with reduced neuropathy.
Boronic acid forms reversible tetrahedral covalent bond with Thr-1 hydroxyl of beta-5 catalytic subunit. Blocks IkappaBalpha degradation, preventing NF-kappaB nuclear translocation. Stabilizes pro-apoptotic proteins (Bax, Noxa, p53), inhibits UPR, disrupts myeloma-stroma interactions, and inhibits osteoclast differentiation. Reversibility allows proteasome recovery between doses.
Marketed as Velcade. Approved May 13, 2003. VISTA (N=682): VMP vs. MP, TTP 24.0 vs. 16.6 months (HR 0.48, P<0.001); OS 56.4 vs. 43.1 months. Multiple Phase III trials established bortezomib-based induction as standard for transplant-eligible MM. Indications: multiple myeloma (all lines), mantle cell lymphoma. Generics available.
Vancomycin is marketed as Vancocin and Firvanq (approved 1958, with oral solution Firvanq approved 2018). It is the standard treatment for serious MRSA infections (bloodstream infections, endocarditis, pneumonia, bone infections) and is first-line for severe C. difficile colitis. Vancomycin requires therapeutic drug monitoring — blood levels must be checked regularly to ensure the dose is effective without causing kidney damage or hearing loss. The rise of vancomycin-resistant enterococci (VRE) and occasional vancomycin-intermediate S. aureus (VISA) strains represent ongoing challenges. Despite being nearly 70 years old, vancomycin remains irreplaceable for many serious infections, though newer alternatives like daptomycin and the lipoglycopeptides offer advantages in specific settings.
Zilucoplan is marketed as Zilbrysq (approved October 2023) for anti-acetylcholine receptor antibody-positive generalised myasthenia gravis in adults. Administered as a daily subcutaneous self-injection. In the RAISE trial, zilucoplan showed statistically significant improvements in both activities of daily living and quantitative muscle strength scores compared to placebo, with improvements evident from week one. Its key differentiator from existing complement inhibitors (eculizumab, ravulizumab) is the self-injectable format — those alternatives require hospital-based intravenous infusions. As with all complement inhibitors, patients require meningococcal vaccination before starting treatment due to increased susceptibility to meningococcal infection.
Daptomycin is marketed as Cubicin (approved September 2003). It is indicated for complicated skin and soft tissue infections and S. aureus bloodstream infections including right-sided endocarditis. Administered as a once-daily intravenous infusion. A key limitation is that daptomycin cannot be used for pneumonia — lung surfactant inactivates the drug. In the bacteraemia trial, daptomycin was non-inferior to vancomycin with significantly lower rates of kidney problems (11% versus 26%). Creatine kinase (CK) levels must be monitored during treatment, as daptomycin can cause muscle toxicity. Generics became available after patent expiry, significantly reducing cost.
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