Bortezomib
drugOn this page
Also known as Bortezomib hydrateLDP-341NSC-681239PS-341Dipeptidyl boronic acid derivativePeptidyl boronic acid derivativeSID518755SID124950705SID144206183SID144206225SID170465087Velcade
Summary
Bortezomib (CHEMBL325041) is an approved small-molecule antineoplastic agent (ATC L01XG01) targeting PSMB5; indicated across 107 conditions including neoplasm and leukemia; with CIViC clinical evidence for 3 variant-indication associations (e.g. CCND1 Overexpression in multiple myeloma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01XG01
- Targets: 1 (PSMB5)
- Indications: 107 conditions
- Clinical trials: 866
- Precision-oncology evidence (CIViC): 3 variant–indication associations
- Chemistry: 384.2 Da · C19H25BN4O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL325041 |
| Name | Bortezomib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 387447 |
| ChEBI | CHEBI:52717 |
| ATC | L01XG01 |
| Molecular formula | C19H25BN4O4 |
| Molecular weight | 384.2 |
| InChIKey | GXJABQQUPOEUTA-RDJZCZTQSA-N |
SMILES: B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
IUPAC name: [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
ChEBI definition: L-Phenylalaninamide substituted at the amide nitrogen by a 1-(dihydroxyboranyl)-3-methylbutyl group and at Nα by a pyrazin-2-ylcarbonyl group. It is a dipeptidyl boronic acid that reversibly inhibits the 26S proteasome.
Pharmacological roles (ChEBI): antineoplastic agent, proteasome inhibitor, protease inhibitor, antiprotozoal drug.
Also known as: Bortezomib, Bortezomib hydrate, LDP-341, NSC-681239, PS-341, Dipeptidyl boronic acid derivative, Peptidyl boronic acid derivative, bortezomib, SID518755, BORTEZOMIB, SID124950705, SID144206183
Parent form; salt/anhydrous children: CHEMBL5315122
Patent coverage: 3,917 distinct patent families (13,120 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 12,876 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| PSMB5 | proteasome 20S subunit beta 5 | Inhibition | 7.7 | 95% (common-essential) | P28074 |
| Plasmodium falciparum proteasome subunit beta type-5 | 7.51 |
Broader ChEMBL bioactivity targets: 41 (assay-derived). Sample: Histone deacetylase 3, Protein deacetylase HDAC6, ATP-dependent Clp protease proteolytic subunit, Histone deacetylase 2, Proteasome subunit beta type-8, Proteasome subunit beta type-9, Proteasome subunit beta type-6, Prothrombin, Carbonic anhydrase 2, Nuclear factor NF-kappa-B complex.
Bioactivity
ChEMBL activities: 122 potent at pChembl ≥ 5 of 126 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PSMB5 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_18537720 |
| PSMB5 | 9.26 | Ki | 0.55 | nM | CHEMBL_ACT_14528999 |
| PSMB5 | 9.22 | Ki | 0.6 | nM | CHEMBL_ACT_13322909 |
| PSMB11 | 9.22 | Ki | 0.6 | nM | CHEMBL_ACT_29064079 |
| PSMB11 | 9.22 | Ki | 0.6 | nM | CHEMBL_ACT_29278081 |
| PSMB8 | 8.89 | IC50 | 1.3 | nM | CHEMBL_ACT_24866178 |
| PSMB5 | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_16532743 |
| PSMB5 | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_16548365 |
| PSMB5 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_14526779 |
| PSMB8 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_22456283 |
| PSMB5 | 8.62 | IC50 | 2.4 | nM | CHEMBL_ACT_24972784 |
| PSMB11 | 8.62 | IC50 | 2.4 | nM | CHEMBL_ACT_25524559 |
| PSMB11 | 8.59 | IC50 | 2.56 | nM | CHEMBL_ACT_14550610 |
| PSMB5 | 8.55 | IC50 | 2.8 | nM | CHEMBL_ACT_24746484 |
| PSMB5 | 8.55 | IC50 | 2.82 | nM | CHEMBL_ACT_24746486 |
| PSMB9 | 8.54 | IC50 | 2.9 | nM | CHEMBL_ACT_24866168 |
| PSMB9 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_19300208 |
| PSMB11 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25918282 |
| PSMB5 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25999750 |
| PSMB5 | 8.49 | IC50 | 3.2 | nM | CHEMBL_ACT_24866230 |
| PSMB8 | 8.48 | IC50 | 3.3 | nM | CHEMBL_ACT_19258360 |
| PSMB5 | 8.47 | Ki | 3.4 | nM | CHEMBL_ACT_25995183 |
| PSMB5 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_14526811 |
| PSMB5 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_18195674 |
| PSMB5 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_18249143 |
| PSMB5 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_18259017 |
| PSMB8 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_19300202 |
| PSMB8 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_25999712 |
| PSMB9 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_25999731 |
| PSMB5 | 8.35 | IC50 | 4.5 | nM | CHEMBL_ACT_12699996 |
Target pathways
Aggregated over 1 target gene(s): PSMB5.
Top Reactome pathways
68 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Activation of NF-kappaB in B cells | 1 | PSMB5 |
| Oxygen-dependent proline hydroxylation of Hypoxia-inducible Factor Alpha | 1 | PSMB5 |
| ER-Phagosome pathway | 1 | PSMB5 |
| Cross-presentation of soluble exogenous antigens (endosomes) | 1 | PSMB5 |
| Autodegradation of Cdh1 by Cdh1:APC/C | 1 | PSMB5 |
| SCF-beta-TrCP mediated degradation of Emi1 | 1 | PSMB5 |
| APC/C:Cdc20 mediated degradation of Securin | 1 | PSMB5 |
| APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1 | 1 | PSMB5 |
| Cdc20:Phospho-APC/C mediated degradation of Cyclin A | 1 | PSMB5 |
| Vpu mediated degradation of CD4 | 1 | PSMB5 |
| Vif-mediated degradation of APOBEC3G | 1 | PSMB5 |
| SCF(Skp2)-mediated degradation of p27/p21 | 1 | PSMB5 |
| Degradation of beta-catenin by the destruction complex | 1 | PSMB5 |
| Downstream TCR signaling | 1 | PSMB5 |
| Regulation of activated PAK-2p34 by proteasome mediated degradation | 1 | PSMB5 |
| Separation of Sister Chromatids | 1 | PSMB5 |
| FCERI mediated NF-kB activation | 1 | PSMB5 |
| Autodegradation of the E3 ubiquitin ligase COP1 | 1 | PSMB5 |
| Regulation of ornithine decarboxylase (ODC) | 1 | PSMB5 |
| ABC-family protein mediated transport | 1 | PSMB5 |
| AUF1 (hnRNP D0) binds and destabilizes mRNA | 1 | PSMB5 |
| Asymmetric localization of PCP proteins | 1 | PSMB5 |
| Degradation of AXIN | 1 | PSMB5 |
| Degradation of DVL | 1 | PSMB5 |
| Hedgehog ligand biogenesis | 1 | PSMB5 |
| Hh mutants are degraded by ERAD | 1 | PSMB5 |
| Dectin-1 mediated noncanonical NF-kB signaling | 1 | PSMB5 |
| CLEC7A (Dectin-1) signaling | 1 | PSMB5 |
| Degradation of GLI1 by the proteasome | 1 | PSMB5 |
| Degradation of GLI2 by the proteasome | 1 | PSMB5 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| proteolysis | 1 |
| response to oxidative stress | 1 |
| proteasomal ubiquitin-independent protein catabolic process | 1 |
| proteasome-mediated ubiquitin-dependent protein catabolic process | 1 |
| proteasome assembly | 1 |
| obsolete proteolysis involved in protein catabolic process | 1 |
Indications & clinical
Indications
107 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| leukemia | 3 | MONDO:0005059 | EFO:0000565 |
| plasma cell myeloma | 3 | MONDO:0009693 | EFO:0001378 |
| lymphoma | 3 | MONDO:0005062 | EFO:0000574 |
| acute myeloid leukemia | 3 | MONDO:0018874 | EFO:0000222 |
| mantle cell lymphoma | 3 | MONDO:0018876 | EFO:1001469 |
| diffuse large B-cell lymphoma | 3 | MONDO:0018905 | EFO:0000403 |
| acute lymphoblastic leukemia | 3 | MONDO:0004967 | EFO:0000220 |
| chronic kidney disease | 3 | MONDO:0005300 | EFO:0003884 |
| non-Hodgkin lymphoma | 3 | MONDO:0018908 | EFO:0005952 |
| plasmacytoma | 3 | MONDO:0005615 | EFO:0006738 |
| autoimmune thrombocytopenic purpura | 3 | MONDO:0008558 | EFO:0007160 |
| myeloid sarcoma | 3 | MONDO:0006861 | EFO:1001052 |
| amyloidosis | 3 | MONDO:0019065 | EFO:1001875 |
| intrahepatic cholangiocarcinoma | 3 | MONDO:0003210 | EFO:1001961 |
| Waldenstrom macroglobulinemia | 3 | MONDO:0100280 | EFO:0009441 |
| hereditary amyloidosis | 3 | MONDO:0018634 | MONDO:0019438 |
| graft versus host disease | 2 | MONDO:0013730 | EFO:0004599 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| acute promyelocytic leukemia | 2 | MONDO:0012883 | EFO:0000224 |
| myelodysplastic syndrome | 2 | MONDO:0018881 | EFO:0000198 |
| neoplasm of mature B-cells | 2 | MONDO:0004949 | EFO:0000096 |
| mesothelioma | 2 | MONDO:0005065 | EFO:0000588 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| neuromyelitis optica | 2 | MONDO:0019100 | EFO:0004256 |
| bronchiolitis obliterans syndrome | 2 | MONDO:0015265 | EFO:0007183 |
| B-cell acute lymphoblastic leukemia | 2 | MONDO:0004947 | EFO:0000094 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| Hodgkins lymphoma | 2 | MONDO:0004952 | EFO:0000183 |
| MALT lymphoma | 2 | MONDO:0007650 | EFO:0000191 |
| T-cell acute lymphoblastic leukemia | 2 | MONDO:0004963 | EFO:0000209 |
| peripheral T-cell lymphoma, not otherwise specified | 2 | MONDO:0004964 | EFO:0000211 |
| adenoid cystic carcinoma | 2 | MONDO:0004971 | EFO:0000231 |
| chronic myeloid leukemia | 2 | MONDO:0011996 | EFO:0000339 |
| thyroid gland follicular carcinoma | 2 | MONDO:0005034 | EFO:0000501 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| immune system disorder | 2 | MONDO:0005046 | EFO:0000540 |
| thyroid gland papillary carcinoma | 2 | MONDO:0005075 | EFO:0000641 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| prostate carcinoma | 2 | MONDO:0005159 | EFO:0001663 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| nasopharyngeal neoplasm | 2 | MONDO:0005375 | EFO:0004252 |
| plasma cell leukemia | 2 | MONDO:0018689 | EFO:0006475 |
| head and neck cancer | 2 | MONDO:0005627 | EFO:0006859 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| lung adenocarcinoma | 2 | MONDO:0005061 | EFO:0000571 |
| central nervous system neoplasm | 2 | MONDO:0006130 | EFO:1000158 |
| soft tissue sarcoma | 2 | MONDO:0018078 | EFO:1001968 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| kidney cancer | 2 | MONDO:0002367 | MONDO:0002367 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| ureter cancer | 2 | MONDO:0008627 | MONDO:0008627 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| Castleman disease | 2 | MONDO:0015564 | MONDO:0015564 |
| follicular lymphoma | 2 | MONDO:0018906 | MONDO:0018906 |
| acute biphenotypic leukemia | 2 | MONDO:0020322 | MONDO:0019460 |
| hematopoietic and lymphoid system neoplasm | 2 | MONDO:0002334 | MONDO:0044881 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
| pure red-cell aplasia | 2 | MONDO:0001705 | MONDO:0001705 |
| lymphoproliferative syndrome | 2 | MONDO:0016537 | MONDO:0016537 |
| autoimmune hemolytic anemia | 2 | MONDO:0020108 | MONDO:0018922 |
| plasma cell neoplasm | 2 | MONDO:0004959 | EFO:0000200 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
| pancreatic ductal adenocarcinoma | 2 | MONDO:0005184 | MONDO:0005184 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| autoimmune disorder of the nervous system | 2 | MONDO:0002977 | MONDO:0020640 |
| neuroblastoma | 1 | MONDO:0005072 | EFO:0000621 |
| renal cell carcinoma | 1 | MONDO:0005086 | EFO:0000681 |
| squamous cell carcinoma | 1 | MONDO:0005096 | EFO:0000707 |
| anaplastic astrocytoma | 1 | MONDO:0016684 | EFO:0002499 |
| anaplastic oligodendroglioma | 1 | MONDO:0016696 | EFO:0002501 |
| smoldering plasma cell myeloma | 1 | MONDO:0005235 | EFO:0003073 |
| myelodysplastic syndrome with excess blasts | 1 | MONDO:0019454 | EFO:0003811 |
| angioimmunoblastic T-cell lymphoma | 1 | MONDO:0004977 | EFO:0000255 |
| Burkitt lymphoma | 1 | MONDO:0007243 | EFO:0000309 |
| anaplastic large cell lymphoma | 1 | MONDO:0020325 | EFO:0003032 |
| Sezary syndrome | 1 | MONDO:0017844 | EFO:1000785 |
| mycosis fungoides | 1 | MONDO:0009691 | EFO:1001051 |
| uremia | 1 | MONDO:0007008 | EFO:1001226 |
| peritoneal neoplasm | 1 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 1 | MONDO:0021092 | MONDO:0002158 |
| lymphoid leukemia | 1 | MONDO:0005402 | EFO:0004289 |
| muscular dystrophy | 1 | MONDO:0020121 | MONDO:0016145 |
| myeloproliferative neoplasm | 0 | MONDO:0020076 | EFO:0002428 |
21 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 866.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 409 |
| PHASE1 | 169 |
| PHASE3 | 108 |
| PHASE1/PHASE2 | 103 |
| Not specified | 40 |
| PHASE4 | 22 |
| PHASE2/PHASE3 | 8 |
| EARLY_PHASE1 | 7 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03829371 | PHASE4 | ACTIVE_NOT_RECRUITING | STUDY COMPARING TWO STANDARD TREATMENTS IN AUTOLOGOUS STEM CELL TRANSPLANTATION INELIGIBLE POPULATION AFFECTED BY MULTIPLE MYELOMA |
| NCT03844360 | PHASE4 | RECRUITING | Dose Individualization of Antineoplastic Drugs and Anti-Infective Drug in Children With Hematoplastic Disease |
| NCT07025005 | PHASE4 | RECRUITING | Fenofibrate Role in the Prophylaxis From Peripheral Neuropathy Induced by Bortezomib, Lenalidomide and Dexamethasone (VRd) Protocol in the Treatment of Patients With Multiple Myeloma (MM) |
| NCT07334535 | PHASE4 | NOT_YET_RECRUITING | Isa-VRD in TIE HRMM |
| NCT00257114 | PHASE4 | COMPLETED | Evaluation of VELCADE Given as Retreatment to Multiple Myeloma Patients for Efficacy, Safety and Tolerability |
| NCT00652041 | PHASE4 | COMPLETED | Bortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma |
| NCT00782821 | PHASE4 | COMPLETED | Randomized Trial of Induction Therapies in High Immunological Risk Kidney Transplant Recipients |
| NCT00908583 | PHASE4 | COMPLETED | Desensitization in Kidney Transplantation |
| NCT01103778 | PHASE4 | COMPLETED | Pilot Study of Velcade® in IgA Nephropathy |
| NCT01169857 | PHASE4 | WITHDRAWN | Velcade for Proliferative Lupus Nephritis |
| NCT01249690 | PHASE4 | UNKNOWN | Efficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma |
| NCT01842074 | PHASE4 | UNKNOWN | Desensitization With Bortezomib Before a Living Kidney Donation |
| NCT02268890 | PHASE4 | COMPLETED | A Pharmacokinetic Study of Bortezomib in Taiwanese Participants With Multiple Myeloma |
| NCT02525172 | PHASE4 | UNKNOWN | Immune Modulation Therapy for Pompe Disease |
| NCT02559154 | PHASE4 | UNKNOWN | Modified Bortezomib-based Combination Therapy for Multiple Myeloma |
| NCT02773550 | PHASE4 | TERMINATED | Treatment With a Scheme With Low Doses of Bortezomib / Melphalan / Prednisone (MPV) in Patients With Multiple Myeloma |
| NCT02844322 | PHASE4 | COMPLETED | The Comparison of RCD Versus BCD in Newly Diagnosed Waldenström Macroglobulinemia |
| NCT03416374 | PHASE4 | COMPLETED | A Study to Evaluate the Efficacy and Safety of Ixazomib in Combination With Lenalidomide and Dexamethasone in Patients With Relapsed and/or Refractory Multiple Myeloma Initially Treated With an Injection of Proteasome Inhibitor-Based Therapy |
| NCT04348006 | PHASE4 | WITHDRAWN | Assessment of Bortezomib (Alvocade ®) Efficacy and Safety in Newly Diagnosed Multiple Myeloma Patients |
| NCT05135442 | PHASE4 | UNKNOWN | Efficacy and Safety of Bortezomib as First-line Treatment of Acquired TTP |
| NCT05137860 | PHASE4 | UNKNOWN | Efficacy of the Use of Bortezomib for the Treatment of Relapsed Leukemia or Positive MRD |
| NCT06015750 | PHASE4 | WITHDRAWN | Mitigate Immune-Mediated Loss of Therapeutic Response to Asfotase Alfa (STRENSIQ®) for Hypophosphatasia |
| NCT00572169 | PHASE3 | ACTIVE_NOT_RECRUITING | UARK 2006-66, Total Therapy 3B: An Extension of UARK 2003-33 Total Therapy |
| NCT00644228 | PHASE3 | ACTIVE_NOT_RECRUITING | Lenalidomide and Dexamethasone With or Without Bortezomib in Treating Patients With Previously Untreated Multiple Myeloma |
| NCT01208662 | PHASE3 | ACTIVE_NOT_RECRUITING | Randomized Trial of Lenalidomide, Bortezomib, Dexamethasone vs High-Dose Treatment With SCT in MM Patients up to Age 65 |
| NCT01863550 | PHASE3 | ACTIVE_NOT_RECRUITING | Bortezomib or Carfilzomib With Lenalidomide and Dexamethasone in Treating Patients With Newly Diagnosed Multiple Myeloma |
| NCT02112916 | PHASE3 | ACTIVE_NOT_RECRUITING | Combination Chemotherapy With or Without Bortezomib in Treating Younger Patients With Newly Diagnosed T-Cell Acute Lymphoblastic Leukemia or Stage II-IV T-Cell Lymphoblastic Lymphoma |
| NCT03117751 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Total Therapy XVII for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia and Lymphoma |
| NCT03319667 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Investigate the Clinical Benefit of Isatuximab in Combination With Bortezomib, Lenalidomide and Dexamethasone in Adults With Newly Diagnosed Multiple Myeloma Not Eligible for Transplant |
| NCT03617731 | PHASE3 | ACTIVE_NOT_RECRUITING | Trial on the Effect of Isatuximab to Lenalidomide/Bortezomib/Dexamethasone (RVd) Induction and Lenalidomide Maintenance in Patients With Newly Diagnosed Myeloma (GMMG HD7) |
| NCT03643276 | PHASE3 | RECRUITING | Treatment Protocol for Children and Adolescents With Acute Lymphoblastic Leukemia - AIEOP-BFM ALL 2017 |
| NCT03651128 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety Study of bb2121 Versus Standard Regimens in Subjects With Relapsed and Refractory Multiple Myeloma (RRMM) |
| NCT03652064 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Comparing Daratumumab, VELCADE (Bortezomib), Lenalidomide, and Dexamethasone (D-VRd) With VELCADE, Lenalidomide, and Dexamethasone (VRd) in Participants With Untreated Multiple Myeloma and for Whom Hematopoietic Stem Cell Transplant is Not Planned as Initial Therapy |
| NCT03710603 | PHASE3 | ACTIVE_NOT_RECRUITING | Daratumumab, VELCADE (Bortezomib), Lenalidomide and Dexamethasone Compared to VELCADE, Lenalidomide and Dexamethasone in Subjects With Previously Untreated Multiple Myeloma |
| NCT03729804 | PHASE3 | ACTIVE_NOT_RECRUITING | Carfilzomib, Lenalidomide, and Dexamethasone Versus Bortezomib, Lenalidomide and Dexamethasone (KRd vs. VRd) in Patients With Newly Diagnosed Multiple Myeloma (COBRA) |
| NCT03742297 | PHASE3 | ACTIVE_NOT_RECRUITING | Treatment for Elderly Fit Newly Diagnosed Multiple Myeloma Patients Aged Between 65 and 80 Years |
| NCT04181827 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Comparing JNJ-68284528, a CAR-T Therapy Directed Against B-cell Maturation Antigen (BCMA), Versus Pomalidomide, Bortezomib and Dexamethasone (PVd) or Daratumumab, Pomalidomide and Dexamethasone (DPd) in Participants With Relapsed and Lenalidomide-Refractory Multiple Myeloma |
| NCT04246047 | PHASE3 | ACTIVE_NOT_RECRUITING | Evaluation of Efficacy and Safety of Belantamab Mafodotin, Bortezomib and Dexamethasone Versus Daratumumab, Bortezomib and Dexamethasone in Participants With Relapsed/Refractory Multiple Myeloma |
| NCT04484623 | PHASE3 | ACTIVE_NOT_RECRUITING | Belantamab Mafodotin Plus Pomalidomide and Dexamethasone (Pd) Versus Bortezomib Plus Pd in Relapsed/Refractory Multiple Myeloma |
| NCT04566328 | PHASE3 | RECRUITING | Testing the Use of Combination Therapy in Adult Patients With Newly Diagnosed Multiple Myeloma, the EQUATE Trial |
Clinical evidence (CIViC)
Variant × indication × effect (3 predictive associations from 3 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| CCND1 Overexpression | Multiple Myeloma | Sensitivity/Response | Bortezomib | CIViC C | EID7788 |
| TP53 Y220C | Breast Cancer | Sensitivity/Response | Bortezomib | CIViC C | EID6172 |
| GATA2 EXPRESSION | Lung Adenocarcinoma | Sensitivity/Response | Bortezomib + Fasudil | CIViC D | EID301 |
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
12 molecules share ≥1 primary target. Top 12 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CARFILZOMIB | ChEMBL + PubChem | Phase 4 (approved) | PSMB5 |
| IXAZOMIB | ChEMBL | Phase 4 (approved) | PSMB5 |
| VINBLASTINE | ChEMBL | Phase 4 (approved) | PSMB5 |
| CURCUMIN | ChEMBL | Phase 3 | PSMB5 |
| EPIGALOCATECHIN GALLATE | ChEMBL | Phase 3 | PSMB5 |
| MARIZOMIB | ChEMBL | Phase 3 | PSMB5 |
| QUERCETIN | ChEMBL | Phase 3 | PSMB5 |
| DELANZOMIB | ChEMBL | Phase 2 | PSMB5 |
| GENISTEIN | ChEMBL | Phase 2 | PSMB5 |
| LUTEOLIN | ChEMBL | Phase 2 | PSMB5 |
| OPROZOMIB | ChEMBL | Phase 2 | PSMB5 |
| ZETOMIPZOMIB | ChEMBL | Phase 2 | PSMB5 |
Related Atlas pages
- Genes: PSMB5
- Diseases: neoplasm, leukemia, plasma cell myeloma, lymphoma, acute myeloid leukemia, mantle cell lymphoma, diffuse large B-cell lymphoma, acute lymphoblastic leukemia, chronic kidney disease, non-Hodgkin lymphoma, plasmacytoma, autoimmune thrombocytopenic purpura, myeloid sarcoma, amyloidosis, intrahepatic cholangiocarcinoma, Waldenstrom macroglobulinemia, hereditary amyloidosis, breast carcinoma, lung adenocarcinoma
- Drugs: Carfilzomib, Ixazomib, Vinblastine, Curcumin, Epigalocatechin Gallate, Marizomib, Quercetin
- Biomarker genes: CCND1