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

General Information of Drug (ID: DMOB01U)

Drug Name
Amsilarotene Drug Info
Synonyms Am-555S; TAC-101; Anticancer retinoic acid receptor antagonist (oral), Taiho
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 2 [1]
Cross-matching ID
PubChem CID
9800306
CAS Number
CAS 125973-56-0
TTD Drug ID
DMOB01U

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Retinoic acid receptor (RAR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Vitamin A DMJ2AH4 Night blindness 9D45 Approved [7]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [8]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [9]
Adapalene DMX2358 Acne vulgaris ED80 Approved [10]
Fenretinide DMRD5SP Macular degeneration 9B78.3 Phase 3 [11]
Peretinoin DMESAZK Hepatocellular carcinoma 2C12.02 Phase 3 [12]
13-cis-retinoic acid DMTZ1A5 Glioma 2A00.0 Phase 3 [13]
Velac Gel DMXHI89 Acne vulgaris ED80 Phase 3 [14]
LAS-41001 DMXZ4BK Rosacea ED90.0 Discontinued in Preregistration [15]
IRX-4310 DMUYQH8 Psoriasis vulgaris EA90 Discontinued in Phase 3 [16]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Retinoblastoma-associated protein (RB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [17]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [18]
Gefitinib DM15F0X Colon adenocarcinoma Approved [19]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [20]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [21]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [22]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [23]
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [25]
Quercetin DM3NC4M Obesity 5B81 Approved [26]
⏷ Show the Full List of 10 Drug(s)
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 [27]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [28]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [29]
Gefitinib DM15F0X Colon adenocarcinoma Approved [30]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [20]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [31]
Etretinate DM2CZFA Keratosis ED56 Approved [32]
Prednisone DM2HG4X Acute asthma CA23 Approved [33]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [34]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [35]
⏷ Show the Full List of 10 Drug(s)
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 [18]
Gefitinib DM15F0X Colon adenocarcinoma Approved [36]
Prednisone DM2HG4X Acute asthma CA23 Approved [33]
Methotrexate DM2TEOL Anterior urethra cancer Approved [37]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [38]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [39]
Quercetin DM3NC4M Obesity 5B81 Approved [40]
Fluoxetine DM3PD2C Bipolar depression Approved [41]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [42]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [43]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Hepatocyte growth factor receptor (MET)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [44]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [45]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [46]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [46]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [46]
Methotrexate DM2TEOL Anterior urethra cancer Approved [47]
Quercetin DM3NC4M Obesity 5B81 Approved [48]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [46]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [49]
Methylprednisolone DM4BDON Acute adrenal insufficiency Approved [47]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-8 (CXCL8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [50]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [51]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [52]
Pantothenic acid DM091H2 Vitamin deficiency 5B55-5B71 Approved [53]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [54]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [55]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [46]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [56]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [57]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Tumor necrosis factor receptor superfamily member 6 (FAS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [58]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [31]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [59]
Methotrexate DM2TEOL Anterior urethra cancer Approved [60]
Epinephrine DM3KJBC Acute asthma CA23 Approved [61]
Quercetin DM3NC4M Obesity 5B81 Approved [62]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [63]
Fructose DM43AN2 Vomiting MD90 Approved [64]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [58]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [65]
⏷ 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
Retinoic acid receptor (RAR) TTOD7B3 NOUNIPROTAC Antagonist [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Gene/Protein Processing [3]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Gene/Protein Processing [3]
Hepatocyte growth factor receptor (MET) OT7K55MU MET_HUMAN Gene/Protein Processing [4]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Gene/Protein Processing [5]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Post-Translational Modifications [3]
Thymidylate synthase OTXTG0C7 TYSY_HUMAN Gene/Protein Processing [3]
Tumor necrosis factor receptor superfamily member 6 (FAS) OTP9XG86 TNR6_HUMAN Gene/Protein Processing [6]

References

1 ClinicalTrials.gov (NCT00687596) Study of TAC-101 as Second Line Treatment in Patients With Advanced Hepatocellular Carcinoma Who Received Sorafenib as First Line Therapy. U.S. National Institutes ofHealth.
2 Initial clinical trial of oral TAC-101, a novel retinoic acid receptor-alpha selective retinoid, in patients with advanced cancer. J Clin Oncol. 2002 Aug 15;20(16):3522-32.
3 Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44.
4 4-[3,5-Bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) inhibits the intrahepatic spread of hepatocellular carcinoma and prolongs the life-span of tumor-bearing animals. Clin Exp Metastasis. 1998 Oct;16(7):633-43. doi: 10.1023/a:1006567229929.
5 Contribution of AP-1 interference induced by TAC-101 to tumor growth suppression in a hepatocellular carcinoma model. Tumour Biol. 2009;30(1):1-7. doi: 10.1159/000189712. Epub 2009 Jan 12.
6 4- [3,5-bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) induced fas expression and activated caspase-3 and -8 in a DLD-1 colon cancer cell line. In Vivo. 2007 Mar-Apr;21(2):381-7.
7 Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.
8 Retinoids--which dermatological indications will benefit in the near future Skin Pharmacol Appl Skin Physiol. 2001 Sep-Oct;14(5):303-15.
9 Retinoid agonist isotretinoin ameliorates obstructive renal injury. J Urol. 2003 Oct;170(4 Pt 1):1398-402.
10 A review of adapalene in the treatment of acne vulgaris. J Adolesc Health. 2008 Nov;43(5):421-4.
11 National Cancer Institute Drug Dictionary (drug id 39582).
12 Peretinoin, an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. BMC Cancer. 2013 Apr 15;13:191.
13 13-cis retinoic acid exerts its specific activity on human sebocytes through selective intracellular isomerization to all-trans retinoic acid and binding to retinoid acid receptors. J Invest Dermatol. 2000 Aug;115(2):321-7.
14 Chromosomal translocation t(15;17) in human acute promyelocytic leukemia fuses RAR alpha with a novel putative transcription factor, PML. Cell. 1991 Aug 23;66(4):663-74.
15 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027956)
16 An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium. Br J Cancer. 2004 Aug 2;91(3):580-8.
17 Indomethacin inhibits cell growth of medullary thyroid carcinoma by reducing cell cycle progression into S phase. Exp Biol Med (Maywood). 2008 Nov;233(11):1433-40. doi: 10.3181/0804-RM-127. Epub 2008 Sep 12.
18 Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer. Endocr Relat Cancer. 2011 Apr 28;18(3):333-45. doi: 10.1530/ERC-10-0262. Print 2011 Jun.
19 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
20 BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile. J Biochem Mol Toxicol. 2019 May;33(5):e22286. doi: 10.1002/jbt.22286. Epub 2019 Jan 23.
21 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
22 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.
23 Sulindac induces specific degradation of the HPV oncoprotein E7 and causes growth arrest and apoptosis in cervical carcinoma cells. Cancer Lett. 2007 Jan 8;245(1-2):103-11. doi: 10.1016/j.canlet.2005.12.034. Epub 2006 Feb 20.
24 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
25 HMG-CoA reductase inhibitor simvastatin inhibits cell cycle progression at the G1/S checkpoint in immortalized lymphocytes from Alzheimer's disease patients independently of cholesterol-lowering effects. J Pharmacol Exp Ther. 2008 Jan;324(1):352-9. doi: 10.1124/jpet.107.128959. Epub 2007 Oct 10.
26 Inhibition of prostate cancer cell colony formation by the flavonoid quercetin correlates with modulation of specific regulatory genes. Clin Diagn Lab Immunol. 2004 Jan;11(1):63-9. doi: 10.1128/cdli.11.1.63-69.2004.
27 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.
28 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.
29 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.
30 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.
31 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.
32 Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26. doi: 10.1111/j.1365-2133.2008.08931.x. Epub 2008 Nov 25.
33 Glucocorticoids induce G1 arrest of lymphoblastic cells through retinoblastoma protein Rb1 dephosphorylation in childhood acute lymphoblastic leukemia in vivo. Cancer Biol Ther. 2004 May;3(5):470-6. doi: 10.4161/cbt.3.5.838. Epub 2004 May 9.
34 Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
35 Utilization of CDKN1A/p21 gene for class discrimination of DNA damage-induced clastogenicity. Toxicology. 2014 Jan 6;315:8-16. doi: 10.1016/j.tox.2013.10.009. Epub 2013 Nov 6.
36 Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
37 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.
38 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.
39 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
40 Effects of structurally related flavonoids on cell cycle progression of human melanoma cells: regulation of cyclin-dependent kinases CDK2 and CDK1. Biochem Pharmacol. 2001 May 15;61(10):1205-15. doi: 10.1016/s0006-2952(01)00583-4.
41 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.
42 Induction mechanism of apoptosis by troglitazone through peroxisome proliferator-activated receptor-gamma in gastric carcinoma cells. Anticancer Res. 2003 Jan-Feb;23(1A):267-73.
43 Down-regulation of CD44 contributes to the differentiation of HL-60 cells induced by ATRA or HMBA. Cell Mol Immunol. 2007 Feb;4(1):59-63.
44 ROS-dependent DNA damage contributes to crizotinib-induced hepatotoxicity via the apoptotic pathway. Toxicol Appl Pharmacol. 2019 Nov 15;383:114768. doi: 10.1016/j.taap.2019.114768. Epub 2019 Oct 19.
45 Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. Mol Cancer Ther. 2012 Jul;11(7):1557-64. doi: 10.1158/1535-7163.MCT-11-0934. Epub 2012 Jun 22.
46 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
47 Antirheumatic drug response signatures in human chondrocytes: potential molecular targets to stimulate cartilage regeneration. Arthritis Res Ther. 2009;11(1):R15.
48 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
49 All-trans retinoic acid inhibits the cell proliferation but enhances the cell invasion through up-regulation of c-met in pancreatic cancer cells. Cancer Lett. 2005 Jun 28;224(2):303-10. doi: 10.1016/j.canlet.2004.10.016. Epub 2004 Dec 8.
50 Monomeric and oligomeric flavanols maintain the endogenous glucocorticoid response in human macrophages in pro-oxidant conditions in vitro. Chem Biol Interact. 2018 Aug 1;291:237-244.
51 Nicotine up-regulates IL-8 expression in human gingival epithelial cells following stimulation with IL-1 or P. gingivalis lipopolysaccharide via nicotinic acetylcholine receptor signalling. Arch Oral Biol. 2012 May;57(5):483-90. doi: 10.1016/j.archoralbio.2011.10.007. Epub 2011 Nov 25.
52 Ca(2+) Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2. Int J Mol Sci. 2018 Sep 19;19(9):2829. doi: 10.3390/ijms19092829.
53 Calcium pantothenate modulates gene expression in proliferating human dermal fibroblasts. Exp Dermatol. 2009 Nov;18(11):969-78. doi: 10.1111/j.1600-0625.2009.00884.x. Epub 2009 Apr 8.
54 Nitrogen mustard prevents transport of Fra-1 into the nucleus to promote c-Fos- and FosB-dependent IL-8 induction in injured mouse epidermis. Toxicol Lett. 2020 Feb 1;319:256-263. doi: 10.1016/j.toxlet.2019.10.006. Epub 2019 Oct 19.
55 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
56 Gypenosides protect retinal pigment epithelium cells from oxidative stress. Food Chem Toxicol. 2018 Feb;112:76-85.
57 Nitric oxide synthase inhibitors attenuate ozone-induced airway inflammation in guinea pigs. Possible role of interleukin-8. Am J Respir Crit Care Med. 2000 Jan;161(1):249-56. doi: 10.1164/ajrccm.161.1.9804096.
58 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
59 Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
60 Topotecan and methotrexate alter expression of the apoptosis-related genes BCL2, FAS and BCL2L12 in leukemic HL-60 cells. Biol Chem. 2006 Dec;387(12):1629-33. doi: 10.1515/BC.2006.203.
61 Carvedilol prevents epinephrine-induced apoptosis in human coronary artery endothelial cells: modulation of Fas/Fas ligand and caspase-3 pathway. Cardiovasc Res. 2000 Feb;45(3):788-94. doi: 10.1016/s0008-6363(99)00369-7.
62 Multifaceted preventive effects of single agent quercetin on a human prostate adenocarcinoma cell line (PC-3): implications for nutritional transcriptomics and multi-target therapy. Med Oncol. 2011 Dec;28(4):1395-404. doi: 10.1007/s12032-010-9603-3. Epub 2010 Jul 2.
63 Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
64 Non-nutritional sweeteners effects on endothelial vascular function. Toxicol In Vitro. 2020 Feb;62:104694. doi: 10.1016/j.tiv.2019.104694. Epub 2019 Oct 23.
65 Transcriptome-based functional classifiers for direct immunotoxicity. Arch Toxicol. 2014 Mar;88(3):673-89.