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

General Information of Drug (ID: DMJ3ZT8)

Drug Name
Lexacalcitol Drug Info
Synonyms KH-106; KH-1060; MC-1357; Vitamin D3 agonist, Leo
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
5288670
CAS Number
CAS 131875-08-6
TTD Drug ID
DMJ3ZT8

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Vitamin D3 receptor (VDR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergocalciferol DMHO0AR Hypoparathyroidism 5A50 Approved [7]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [8]
Calcidiol DMN4CV5 Hypophosphatemia Approved [7]
Doxercalciferol DM6FG1P Chronic kidney disease GB61 Approved [9]
Calcipotriol DM03CP7 Psoriasis EA90 Approved [10]
Falecalcitrol DMBI9ZJ Hyperparathyroidism 5A51 Approved [11]
Dihydrotachysterol DMFB97P Hypocalcemia 5B5K.1 Approved [12]
Cholecalciferol DMGU74E Adult acute monocytic leukemia Approved [13]
Paricalcitol DMYBV3G Hyperparathyroidism 5A51 Approved [14]
Seocalcitol DMKL9QO Rickets 5B57 Phase 3 [15]
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Drug(s) Affected By Osteocalcin (BGLAP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [16]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [17]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [18]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [19]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [21]
Pamidronate DMB4AVP Bone Paget disease Approved [22]
Falecalcitrol DMBI9ZJ Hyperparathyroidism 5A51 Approved [23]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [24]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [25]
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Drug(s) Affected By Retinoblastoma-associated protein (RB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [26]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [27]
Gefitinib DM15F0X Colon adenocarcinoma Approved [28]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [30]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [31]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [32]
Methotrexate DM2TEOL Anterior urethra cancer Approved [33]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [34]
Quercetin DM3NC4M Obesity 5B81 Approved [35]
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Drug(s) Affected By G1/S-specific cyclin-E1 (CCNE1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [36]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [37]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [38]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [39]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [32]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
Fluoxetine DM3PD2C Bipolar depression Approved [40]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [41]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [42]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [43]
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Drug(s) Affected By Cyclin-dependent kinase 2 (CDK2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [44]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [45]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [37]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [46]
Selenium DM25CGV N. A. N. A. Approved [47]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [39]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [48]
Methotrexate DM2TEOL Anterior urethra cancer Approved [49]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [50]
Quercetin DM3NC4M Obesity 5B81 Approved [35]
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Drug(s) Affected By Cyclin-dependent kinase inhibitor 1 (CDKN1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [51]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [52]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [53]
Gefitinib DM15F0X Colon adenocarcinoma Approved [54]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [55]
Etretinate DM2CZFA Keratosis ED56 Approved [56]
Prednisone DM2HG4X Acute asthma CA23 Approved [57]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [39]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [58]
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Drug(s) Affected By Cyclin-dependent kinase inhibitor 1B (CDKN1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [27]
Gefitinib DM15F0X Colon adenocarcinoma Approved [59]
Prednisone DM2HG4X Acute asthma CA23 Approved [57]
Methotrexate DM2TEOL Anterior urethra cancer Approved [60]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [61]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [62]
Quercetin DM3NC4M Obesity 5B81 Approved [63]
Fluoxetine DM3PD2C Bipolar depression Approved [40]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [64]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [65]
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Drug(s) Affected By Cathelicidin antimicrobial peptide (CAMP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [66]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [67]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [3]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [68]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [69]
Mifepristone DMGZQEF Cushing disease 5A70 Approved [70]
Arsenic DMTL2Y1 N. A. N. A. Approved [71]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [72]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [70]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [73]
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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
Vitamin D3 receptor (VDR) TTK59TV VDR_HUMAN Agonist [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cathelicidin antimicrobial peptide (CAMP) OT3Y8011 CAMP_HUMAN Gene/Protein Processing [3]
Cyclin-dependent kinase 2 (CDK2) OTB5DYYZ CDK2_HUMAN Gene/Protein Processing [4]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Gene/Protein Processing [4]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Gene/Protein Processing [4]
G1/S-specific cyclin-E1 (CCNE1) OTLD7UID CCNE1_HUMAN Gene/Protein Processing [4]
Osteocalcin (BGLAP) OTK1YLWQ OSTCN_HUMAN Gene/Protein Processing [5]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Post-Translational Modifications [4]
Vitamin D3 receptor OTFC7K35 VDR_HUMAN Protein Interaction/Cellular Processes [6]

References

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2 The vitamin D analog, KH1060, is rapidly degraded both in vivo and in vitro via several pathways: principal metabolites generated retain significant biological activity. Endocrinology. 1997 Dec;138(12):5485-96.
3 Human cathelicidin antimicrobial peptide (CAMP) gene is a direct target of the vitamin D receptor and is strongly up-regulated in myeloid cells by 1,25-dihydroxyvitamin D3. FASEB J. 2005 Jul;19(9):1067-77. doi: 10.1096/fj.04-3284com.
4 Inhibition of MG-63 cell cycle progression by synthetic vitamin D3 analogs mediated by p27, Cdk2, cyclin E, and the retinoblastoma protein. Biochem Pharmacol. 2003 Aug 1;66(3):495-504. doi: 10.1016/s0006-2952(03)00283-1.
5 9-cis retinoic acid accelerates calcitriol-induced osteocalcin production and promotes degradation of both vitamin D receptor and retinoid X receptor in human osteoblastic cells. J Cell Biochem. 2003 Aug 15;89(6):1164-76. doi: 10.1002/jcb.10572.
6 Targacept active conformation search: a new method for predicting the conformation of a ligand bound to its protein target. J Med Chem. 2004 Dec 30;47(27):6831-9.
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12 In vivo metabolism of the vitamin D analog, dihydrotachysterol. Evidence for formation of 1 alpha,25- and 1 beta,25-dihydroxy-dihydrotachysterol metabolites and studies of their biological activity. J Biol Chem. 1993 Jan 5;268(1):282-92.
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21 Glucosamine promotes osteogenic differentiation of dental pulp stem cells through modulating the level of the transforming growth factor-beta type I receptor. J Cell Physiol. 2010 Oct;225(1):140-51.
22 Pamidronate increases markers of bone formation in patients with multiple myeloma in plateau phase under interferon-alpha treatment. Calcif Tissue Int. 2001 May;68(5):285-90.
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24 Simvastatin and atorvastatin enhance gene expression of collagen type 1 and osteocalcin in primary human osteoblasts and MG-63 cultures. J Cell Biochem. 2007 Aug 15;101(6):1430-8. doi: 10.1002/jcb.21259.
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30 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
31 Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
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33 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
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36 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.
37 Estrogen receptor regulates E2F1 expression to mediate tamoxifen resistance. Mol Cancer Res. 2010 Mar;8(3):343-52. doi: 10.1158/1541-7786.MCR-09-0395. Epub 2010 Mar 9.
38 Ribavirin inhibits colorectal cancer growth by downregulating PRMT5 expression and H3R8me2s and H4R3me2s accumulation. Toxicol Appl Pharmacol. 2021 Mar 15;415:115450. doi: 10.1016/j.taap.2021.115450. Epub 2021 Feb 9.
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40 Fluoxetine mediates G0/G1 arrest by inducing functional inhibition of cyclin dependent kinase subunit (CKS)1. Biochem Pharmacol. 2008 May 15;75(10):1924-34. doi: 10.1016/j.bcp.2008.02.013. Epub 2008 Feb 17.
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42 Retinoic acid regulates cell cycle progression and cell differentiation in human monocytic THP-1 cells. Exp Cell Res. 2004 Jul 1;297(1):68-81. doi: 10.1016/j.yexcr.2004.02.017.
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47 Selenite and selenomethionine promote HL-60 cell cycle progression. J Nutr. 2002 Apr;132(4):674-9. doi: 10.1093/jn/132.4.674.
48 Nonsteroidal anti-inflammatory drugs inhibit growth of human neuroendocrine tumor cells via G1 cell-cycle arrest. Int J Cancer. 2003 Dec 10;107(5):844-53. doi: 10.1002/ijc.11446.
49 Peripheral blood expression of nuclear factor-kappab-regulated genes is associated with rheumatoid arthritis disease activity and responds differentially to anti-tumor necrosis factor-alpha versus methotrexate. J Rheumatol. 2007 Sep;34(9):1817-22. Epub 2007 Aug 1.
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51 Zidovudine induces S-phase arrest and cell cycle gene expression changes in human cells. Mutagenesis. 2005 Mar;20(2):139-46. doi: 10.1093/mutage/gei019. Epub 2005 Mar 22.
52 Cannabidiol Activates Neuronal Precursor Genes in Human Gingival Mesenchymal Stromal Cells. J Cell Biochem. 2017 Jun;118(6):1531-1546. doi: 10.1002/jcb.25815. Epub 2016 Dec 29.
53 Gene expression profiles with activation of the estrogen receptor alpha-selective estrogen receptor modulator complex in breast cancer cells expressing wild-type estrogen receptor. Cancer Res. 2002 Aug 1;62(15):4419-26.
54 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
55 Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
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60 Methotrexate increases expression of cell cycle checkpoint genes via JNK activation. Arthritis Rheum. 2012 Jun;64(6):1780-9. doi: 10.1002/art.34342. Epub 2011 Dec 19.
61 Simvastatin inhibits growth via apoptosis and the induction of cell cycle arrest in human melanoma cells. Melanoma Res. 2008 Apr;18(2):85-94. doi: 10.1097/CMR.0b013e3282f60097.
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66 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
67 Global effects of inorganic arsenic on gene expression profile in human macrophages. Mol Immunol. 2009 Feb;46(4):649-56.
68 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
69 Dual anti-inflammatory and anti-parasitic action of topical ivermectin 1% in papulopustular rosacea. J Eur Acad Dermatol Venereol. 2017 Nov;31(11):1907-1911. doi: 10.1111/jdv.14437. Epub 2017 Aug 29.
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72 Blood transcript immune signatures distinguish a subset of people with elevated serum ALT from others given acetaminophen. Clin Pharmacol Ther. 2016 Apr;99(4):432-41.
73 Characterizing the genetic basis for nicotine induced cancer development: a transcriptome sequencing study. PLoS One. 2013 Jun 18;8(6):e67252.