| Drug General Information |
| Drug ID |
D01EUF
|
| Former ID |
DCL000003
|
| Drug Name |
BMS 275291
|
| Synonyms |
D 2163; N-((2S)-2-Mercapto-1-oxo-4-(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)butyl)-L-leucyl-N,3-dimethyl-L-valinamide; (2S)-N-[(2S)-3,3-dimethyl-2-(methylamino)butanoyl]-4-methyl-2-[[(2S)-2-sulfanyl-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butanoyl]amino]pentanamide
|
| Drug Type |
Small molecular drug
|
| Indication |
Non-small-cell lung cancer; Hormone-refractory prostate cancer; Kaposi's sarcoma [ICD9: 140-229, 162, 176, 185, 204.0; ICD10:C33, C33-C34, C34, C46, C61, C91.0]
|
Discontinued in Phase 3 |
[1]
|
|---|
| Therapeutic Class |
Anticancer Agents
|
| Company |
Bristol Myers Squibb; Celltech Group
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C23H41N5O5S
|
| Canonical SMILES |
CC(C)CC(C(=O)NC(=O)C(C(C)(C)C)NC)NC(=O)C(CCN1C(=O)C(N(C<br />1=O)C)(C)C)S
|
| InChI |
1S/C23H41N5O5S/c1-13(2)12-14(17(29)26-19(31)16(24-8)22(3,4)5)25-18(30)15(34)10-11-28-20(32)23(6,7)27(9)21(28)33/h13-16,24,34H,10-12H2,1-9H3,(H,25,30)(H,26,29,31)/t14-,15-,16+/m0/s1
|
| InChIKey |
BWLOJMZLTBBDHA-HRCADAONSA-N
|
| CAS Number |
CAS 259188-38-0
|
| PubChem Compound ID |
|
| PubChem Substance ID |
|
| Target and Pathway |
| Target(s) |
72 kDa type IV collagenase |
Target Info |
Inhibitor |
[2],
[3],
[4],
[1]
|
|---|
| Interstitial collagenase |
Target Info |
Inhibitor |
[2],
[3],
[4],
[1]
|
| Matrilysin |
Target Info |
Inhibitor |
[2],
[3],
[4],
[1]
|
|
KEGG Pathway
|
Leukocyte transendothelial migration
|
|
GnRH signaling pathway
|
|
Estrogen signaling pathway
|
|
Pathways in cancer
|
|
Proteoglycans in cancer
|
|
Bladder cancerhsa03320:PPAR signaling pathway
|
|
Bladder cancer
|
|
Rheumatoid arthritishsa04310:Wnt signaling pathway
|
|
NetPath Pathway
|
Leptin Signaling Pathway
|
|
TCR Signaling Pathway
|
|
ID Signaling PathwayNetPath_13:IL1 Signaling Pathway
|
|
EGFR1 Signaling Pathway
|
|
TWEAK Signaling Pathway
|
|
Wnt Signaling PathwayNetPath_8:Wnt Signaling Pathway
|
|
PANTHER Pathway
|
Alzheimer disease-presenilin pathwayP00004:Alzheimer disease-presenilin pathway
|
|
Plasminogen activating cascadeP00004:Alzheimer disease-presenilin pathway
|
|
Wnt signaling pathway
|
|
CCKR signaling map ST
|
|
Pathway Interaction Database
|
LPA receptor mediated events
|
|
Plasma membrane estrogen receptor signaling
|
|
Osteopontin-mediated events
|
|
Validated transcriptional targets of AP1 family members Fra1 and Fra2
|
|
Angiopoietin receptor Tie2-mediated signaling
|
|
Direct p53 effectors
|
|
amb2 Integrin signaling
|
|
ATF-2 transcription factor network
|
|
FOXM1 transcription factor network
|
|
Regulation of nuclear beta catenin signaling and target gene transcription
|
|
Syndecan-2-mediated signaling eventsendothelinpathway:Endothelins
|
|
Glucocorticoid receptor regulatory network
|
|
AP-1 transcription factor network
|
|
Syndecan-1-mediated signaling eventsajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly
|
|
p75(NTR)-mediated signaling
|
|
Syndecan-1-mediated signaling events
|
|
Reactome
|
Collagen degradation
|
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Degradation of the extracellular matrix
|
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Activation of Matrix Metalloproteinases
|
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Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
|
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EPH-ephrin mediated repulsion of cellsR-HSA-1442490:Collagen degradation
|
|
Basigin interactions
|
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Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)R-HSA-1442490:Collagen degradation
|
|
Assembly of collagen fibrils and other multimeric structures
|
|
WikiPathways
|
Activation of Matrix Metalloproteinases
|
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AGE/RAGE pathway
|
|
Matrix MetalloproteinasesWP366:TGF beta Signaling Pathway
|
|
Bladder Cancer
|
|
Degradation of collagen
|
|
Quercetin and Nf-kB/ AP-1 Induced Cell Apoptosis
|
|
Oncostatin M Signaling Pathway
|
|
Prostate Cancer
|
|
Integrated Breast Cancer Pathway
|
|
Integrated Cancer pathway
|
|
Cell surface interactions at the vascular wall
|
|
Matrix MetalloproteinasesWP399:Wnt Signaling Pathway and Pluripotency
|
|
Matrix Metalloproteinases
|
| References |
| REF 1 | Phase 1/2 trial of BMS-275291 in patients with human immunodeficiency virus-related Kaposi sarcoma: a multicenter trial of the AIDS Malignancy Consortium. Cancer. 2008 Mar 1;112(5):1083-8. |
|---|
| REF 2 | Tumour microenvironment - opinion: validating matrix metalloproteinases as drug targets and anti-targets for cancer therapy. Nat Rev Cancer. 2006 Mar;6(3):227-39. |
|---|
| REF 3 | Randomized phase II feasibility study of combining the matrix metalloproteinase inhibitor BMS-275291 with paclitaxel plus carboplatin in advanced non-small cell lung cancer. Lung Cancer. 2004 Dec;46(3):361-8. |
|---|
| REF 4 | Randomized phase III study of matrix metalloproteinase inhibitor BMS-275291 in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: National Cancer Institute of Canada-Clinical Trials Group Study BR.18. J Clin Oncol. 2005 Apr 20;23(12):2831-9. |
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