Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM48K0X)

Drug Name
Carfilzomib Drug Info
Synonyms
Carfilzomib; 868540-17-4; Kyprolis; Carfilzomib (PR-171); PR-171; UNII-72X6E3J5AR; 72X6E3J5AR; CHEMBL451887; CHEBI:65347; NCGC00249613-01; DSSTox_RID_82886; DSSTox_CID_28616; DSSTox_GSID_48690; (S)-4-methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide; N-{(2S)-2-[(morpholin-4-ylacetyl)amino]-4-phenylbutanoyl}-L-leucyl-N-{(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl}-L-phenylalaninamide
Indication
Disease Entry ICD 11 Status REF
Multiple myeloma 2A83 Approved [1]
Plasma cell myeloma 2A83.1 Approved [2]
Small-cell lung cancer 2C25.Y Phase 1/2 [3]
Cross-matching ID
PubChem CID
11556711
ChEBI ID
CHEMBL451887
CAS Number
CAS 868540-17-4
TTD Drug ID
DM48K0X
VARIDT Drug ID
DR01324
ACDINA Drug ID
D00915

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Proteasome (PS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bortezomib DMNO38U Leukemia Approved [10]
MLN9708 DMCMETN Amyloidosis 5D00 Approved [11]
Marizomib DME9QGW Glioblastoma of brain 2A00.00 Phase 3 [12]
Oprozomib DM16RIC Hodgkin lymphoma 2B30 Phase 2 [13]
Delanzomib DMX4DQH Multiple myeloma 2A83 Phase 2 [14]
GSK3494245 DMSMQGL Visceral leishmaniasis 1F54.0 Phase 1 [15]
PS-519 DMI0WHC Ischemia-reperfusion injury DB98.B Terminated [16]
MG-101 DM3RUT8 Discovery agent N.A. Investigative [17]
⏷ Show the Full List of 8 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [18]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [19]
Methotrexate DM2TEOL Anterior urethra cancer Approved [20]
Folic Acid DMEMBJC Colorectal carcinoma Approved [21]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [20]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [20]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [22]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [20]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [23]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [24]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Transforming growth factor beta-1 proprotein (TGFB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [25]
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [26]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [27]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [28]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [29]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [30]
Prednisone DM2HG4X Acute asthma CA23 Approved [31]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [32]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [33]
Methotrexate DM2TEOL Anterior urethra cancer Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome c oxidase subunit 8A, mitochondrial (COX8A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [35]
Bortezomib DMNO38U Leukemia Approved [8]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [36]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [37]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [38]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [39]
3R14S-OCHRATOXIN A DM2KEW6 Discovery agent N.A. Investigative [40]
bisphenol A DM2ZLD7 Discovery agent N.A. Investigative [41]
Milchsaure DM462BT Pruritus EC90 Investigative [42]
chloropicrin DMSGBQA Discovery agent N.A. Investigative [43]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Breast cancer type 1 susceptibility protein (BRCA1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [44]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [45]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [46]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [47]
Methotrexate DM2TEOL Anterior urethra cancer Approved [48]
Quercetin DM3NC4M Obesity 5B81 Approved [49]
Furazolidone DM3P6V7 Diarrhea ME05.1 Approved [50]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [51]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [52]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [53]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Proteasome (PS) TTU7ZMG NOUNIPROTAC Modulator [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
AN1-type zinc finger protein 2A OTTG7P8R ZFN2A_HUMAN Gene/Protein Processing [6]
Breast cancer type 1 susceptibility protein (BRCA1) OT5BN6VH BRCA1_HUMAN Drug Response [7]
Cytochrome c oxidase subunit 8A, mitochondrial (COX8A) OTU0NR39 COX8A_HUMAN Gene/Protein Processing [8]
Transforming growth factor beta-1 proprotein (TGFB1) OTV5XHVH TGFB1_HUMAN Gene/Protein Processing [9]

References

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2 Carfilzomib FDA Label
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
5 Identification of an ABCB1 (P-glycoprotein)-positive carfilzomib-resistant myeloma subpopulation by the pluripotent stem cell fluorescent dye CDy1. Am J Hematol. 2013 Apr;88(4):265-72.
6 The Zinc-Finger AN1-Type Domain 2a Gene Acts as a Regulator of Cell Survival in Human Melanoma: Role of E3-Ligase cIAP2. Mol Cancer Res. 2019 Dec;17(12):2444-2456. doi: 10.1158/1541-7786.MCR-19-0243. Epub 2019 Sep 20.
7 Suppression of BRCA1 sensitizes cells to proteasome inhibitors. Cell Death Dis. 2014 Dec 18;5(12):e1580. doi: 10.1038/cddis.2014.537.
8 Identification of Compounds That Inhibit Estrogen-Related Receptor Alpha Signaling Using High-Throughput Screening Assays. Molecules. 2019 Feb 27;24(5):841. doi: 10.3390/molecules24050841.
9 Identification and Profiling of Environmental Chemicals That Inhibit the TGF/SMAD Signaling Pathway. Chem Res Toxicol. 2019 Dec 16;32(12):2433-2444. doi: 10.1021/acs.chemrestox.9b00228. Epub 2019 Nov 11.
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11 Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010 Mar 1;70(5):1970-80.
12 Marizomib, a proteasome inhibitor for all seasons: preclinical profile and a framework for clinical trials. Curr Cancer Drug Targets. 2011 Mar;11(3):254-84.
13 A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood. 2010 Dec 2;116(23):4906-15.
14 Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE. Int Immunopharmacol. 2012 Jan;12(1):257-70.
15 Clinical pipeline report, company report or official report of GlaxoSmithKline
16 Effect of the proteasome inhibitor MLN519 on the expression of inflammatory molecules following middle cerebral artery occlusion and reperfusion in... Neurotox Res. 2003;5(7):505-14.
17 Covalent complexes of proteasome model with peptide aldehyde inhibitors MG132 and MG101: docking and molecular dynamics study.J Mol Model.2009 Dec;15(12):1481-90.
18 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
19 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
20 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
21 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
22 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
23 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
24 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
25 Oxidative stress in kidney transplant patients with calcineurin inhibitor-induced hypertension: effect of ramipril. J Cardiovasc Pharmacol. 2002 Oct;40(4):625-31.
26 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
27 Transcriptomic Analysis of Stem Cells Treated with Moringin or Cannabidiol: Analogies and Differences in Inflammation Pathways. Int J Mol Sci. 2019 Nov 30;20(23):6039. doi: 10.3390/ijms20236039.
28 Antiestrogens induce transforming growth factor beta-mediated immunosuppression in breast cancer. Cancer Res. 2010 Feb 15;70(4):1314-22. doi: 10.1158/0008-5472.CAN-09-3292. Epub 2010 Feb 9.
29 PPAR-alpha ligands inhibit H2O2-mediated activation of transforming growth factor-beta1 in human mesangial cells. Antioxid Redox Signal. 2002 Dec;4(6):877-84. doi: 10.1089/152308602762197416.
30 Cannabidiol selectively modulates interleukin (IL)-1 and IL-6 production in toll-like receptor activated human peripheral blood monocytes. Toxicology. 2021 Dec;464:153016. doi: 10.1016/j.tox.2021.153016. Epub 2021 Nov 2.
31 Cytokine abnormalities in a patient with eosinophilic fasciitis. Ann Allergy Asthma Immunol. 2003 Apr;90(4):452-5. doi: 10.1016/S1081-1206(10)61832-7.
32 Ciprofloxacin decreases survival in HT-29 cells via the induction of TGF-beta1 secretion and enhances the anti-proliferative effect of 5-fluorouracil. Br J Pharmacol. 2009 Jun;157(3):362-70. doi: 10.1111/j.1476-5381.2009.00161.x. Epub 2009 Apr 9.
33 Enhanced apoptosis and transforming growth factor-beta1 expression in colorectal adenomas and carcinomas after Sulindac therapy. Dis Colon Rectum. 2001 Jul;44(7):1008-15. doi: 10.1007/BF02235490.
34 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
35 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
36 Low doses of cisplatin induce gene alterations, cell cycle arrest, and apoptosis in human promyelocytic leukemia cells. Biomark Insights. 2016 Aug 24;11:113-21.
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38 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
39 Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells. J Biol Chem. 2012 Dec 14;287(51):43137-55.
40 In vitro gene expression data supporting a DNA non-reactive genotoxic mechanism for ochratoxin A. Toxicol Appl Pharmacol. 2007 Apr 15;220(2):216-24.
41 Comprehensive analysis of transcriptomic changes induced by low and high doses of bisphenol A in HepG2 spheroids in vitro and rat liver in vivo. Environ Res. 2019 Jun;173:124-134. doi: 10.1016/j.envres.2019.03.035. Epub 2019 Mar 18.
42 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.
43 Transcriptomic analysis of human primary bronchial epithelial cells after chloropicrin treatment. Chem Res Toxicol. 2015 Oct 19;28(10):1926-35.
44 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
45 Cross-talk between non-genomic and genomic signalling pathways--distinct effect profiles of environmental estrogens. Toxicol Appl Pharmacol. 2010 Jun 1;245(2):160-70. doi: 10.1016/j.taap.2010.02.015. Epub 2010 Mar 4.
46 Pro-oxidant induced DNA damage in human lymphoblastoid cells: homeostatic mechanisms of genotoxic tolerance. Toxicol Sci. 2012 Aug;128(2):387-97. doi: 10.1093/toxsci/kfs152. Epub 2012 Apr 26.
47 Differential gene expression of sulindac-treated human breast epithelial cells. Int J Oncol. 2005 Dec;27(6):1727-36.
48 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
49 Quercetin and Its Fermented Extract as a Potential Inhibitor of Bisphenol A-Exposed HT-29 Colon Cancer Cells' Viability. Int J Mol Sci. 2023 Mar 15;24(6):5604. doi: 10.3390/ijms24065604.
50 Involvement of the activation of Nrf2/HO-1, p38 MAPK signaling pathways and endoplasmic reticulum stress in furazolidone induced cytotoxicity and S phase arrest in human hepatocyte L02 cells: modulation of curcumin. Toxicol Mech Methods. 2017 Mar;27(3):165-172. doi: 10.1080/15376516.2016.1273424. Epub 2017 Jan 8.
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53 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.