General Information of Drug (ID: DMT0QK8)

Drug Name
TNP-470 Drug Info
Synonyms
tnp 470; CCRIS 8049; C19H28ClNO6; O-chloroacetylcarbamoyl fumagillol; MSHZHSPISPJWHW-HUTWWKRSSA-N; Carbamic acid, (chloroacetyl)-, 5-methoxy-4-(2-methyl-3-(3-methyl-2-butenyl)oxiranyl)-1-oxaspiro(2.5)oct-6-yl ester, (3R-(3alpha,4alpha(2R*,3R*),5beta,6beta))-
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
369976
ChEBI ID
CHEMBL90748
CAS Number
CAS 129298-91-5
TTD Drug ID
DMT0QK8

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Beloranib DM71CK8 Solid tumour/cancer 2A00-2F9Z Phase 3 [4]
D-Methionine DMMKGBP N. A. N. A. Phase 3 [5]
ZGN-1061 DM9KB7A Type 2 diabetes 5A11 Phase 2 [6]
M8891 DMZ9NVP Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
SDX-7320 DMU0Q6L Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
PPI-2458 DMSAQBC Autoimmune diabetes 5A10 Phase 1 [8]
2-Methyl-2-Propanol DMHM5GJ Discovery agent N.A. Investigative [5]
2-(phenylsulfonamido)-5-propylbenzoic acid DMDGAHO Discovery agent N.A. Investigative [9]
5-p-Tolyl-1H-[1,2,3]triazole DM2W0AD Discovery agent N.A. Investigative [10]
A-357300 DMZHDWN Discovery agent N.A. Investigative [2]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [11]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [12]
Gefitinib DM15F0X Colon adenocarcinoma Approved [13]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [14]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [15]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [16]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [17]
Methotrexate DM2TEOL Anterior urethra cancer Approved [18]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [19]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [21]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [22]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [23]
Gefitinib DM15F0X Colon adenocarcinoma Approved [24]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [14]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [25]
Etretinate DM2CZFA Keratosis ED56 Approved [26]
Prednisone DM2HG4X Acute asthma CA23 Approved [27]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [28]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [29]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Methionine aminopeptidase 2 (METAP2) TTZL0OI MAP2_HUMAN Inhibitor [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]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Post-Translational Modifications [3]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001587)
2 Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2. Cancer Res. 2003 Nov 15;63(22):7861-9.
3 Participation of cyclin D1 deregulation in TNP-470-mediated cytostatic effect: involvement of senescence. Biochem Pharmacol. 2004 Aug 15;68(4):729-38. doi: 10.1016/j.bcp.2004.05.020.
4 2011 Pipeline of Zafgen.
5 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
6 The methionine aminopeptidase 2 inhibitor ZGN-1061 improves glucose control and weight in overweight and obese individuals with type 2 diabetes: A randomized, placebo-controlled trial. Diabetes Obes Metab. 2020 Jul;22(7):1215-1219.
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. Drug Metab Dispos. 2013 Apr;41(4):814-26.
9 Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7.
10 4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo. J Med Chem. 2005 Sep 8;48(18):5644-7.
11 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.
12 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.
13 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
14 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.
15 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
16 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.
17 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.
18 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
19 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.
20 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.
21 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.
22 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.
23 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.
24 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.
25 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.
26 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.
27 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.
28 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.
29 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.