General Information of Drug (ID: DMTIQF3)

Drug Name
Treprostinil Drug Info
Synonyms
Treprostinilo; Treprostinilum; Uniprost; Viveta; Treprostinil sodium; LRX 15; U 62840; Remodulin (TN); Treprostinil [USAN:INN]; UT-15; Treprostinil (USAN/INN); U-62,840; ((1R,2R,3aS,9aS)-2-hydroxy-1-((3S)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1H-cylopent(b)naphthalen-5-yl)oxy)acetate; ({(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]naphthalen-5-yl}oxy)acetic acid; 15 AU81; 2-[[(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[g]naphthalen-5-yl]oxy]acetic acid; 2-[[(1S,2S,3aR,9aR)-2-hydroxy-1-[(3R)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[g]naphthalen-5-yl]oxy]acetic acid
Indication
Disease Entry ICD 11 Status REF
Pulmonary arterial hypertension BB01.0 Approved [1]
Pulmonary hypertension BB01 Approved [2]
Critical limb ischemia BD4Y Investigative [2]
Peripheral vascular disease BD4Z Investigative [2]
Therapeutic Class
Antihypertensive Agents
Cross-matching ID
PubChem CID
6918140
ChEBI ID
CHEBI:50861
CAS Number
CAS 81846-19-7
TTD Drug ID
DMTIQF3
INTEDE Drug ID
DR1632

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Selexipag DMAHSU0 Pulmonary arterial hypertension BB01.0 Approved [7]
Epoprostenol DMUTYR2 Allergic rhinitis CA08.0 Approved [8]
Dinoprost Tromethamine DMXQKSL Abortion JA00 Approved [9]
Misoprostol DMHVJFK Medical abortion JA00.1Z Approved [9]
LAROPIPRANT DM5FABJ Coronary heart disease BA80.Z Phase 4 [10]
Beraprost DML634R Pulmonary hypertension BB01 Phase 4 [11]
esuberaprost DMXLGED Gout FA25 Phase 3 [12]
Ralinepag DM7G4Y9 Pulmonary arterial hypertension BB01.0 Phase 2 [13]
Clinprost DM6E5VA Asthma CA23 Discontinued in Preregistration [14]
Ataprost DMPTG39 Asthma CA23 Discontinued in Phase 3 [15]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [17]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [18]
Verapamil DMA7PEW Angina pectoris BA40 Approved [19]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [20]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [21]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [17]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [22]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C9 (CYP2C9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [26]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [18]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [18]
Verapamil DMA7PEW Angina pectoris BA40 Approved [28]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [29]
Estrone DM5T6US Acne vulgaris ED80 Approved [30]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [32]
Pantothenic acid DM091H2 Vitamin deficiency 5B55-5B71 Approved [33]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [34]
Selenium DM25CGV N. A. N. A. Approved [35]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [37]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [38]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [39]
Leflunomide DMR8ONJ Arthritis FA20 Approved [40]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [41]
⏷ 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
Prostacyclin receptor (PTGIR) TTOFYT1 PI2R_HUMAN Agonist [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [4]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
DNA-binding protein inhibitor ID-1 (ID1) OTKGNZN5 ID1_HUMAN Gene/Protein Processing [6]

References

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2 Treprostinil FDA Label
3 Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009 Apr;157(4):625-35.
4 Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers. J Clin Pharmacol. 2010 Jul;50(7):829-34.
5 FDA label of Treprostinil. The 2020 official website of the U.S. Food and Drug Administration.
6 Smad-dependent and smad-independent induction of id1 by prostacyclin analogues inhibits proliferation of pulmonary artery smooth muscle cells in vitro and in vivo. Circ Res. 2010 Jul 23;107(2):252-62. doi: 10.1161/CIRCRESAHA.109.209940. Epub 2010 Jun 3.
7 Selexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. Eur Respir J. 2012 Oct;40(4):874-80.
8 Novel signaling pathways promote a paracrine wave of prostacyclin-induced vascular smooth muscle differentiation. J Mol Cell Cardiol. 2009 May;46(5):682-94.
9 Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J Biol Chem. 2003 Feb 28;278(9):6947-58.
10 Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806.
11 Prostaglandin I2 IP Receptor Agonist, Beraprost, Prevents Transient Global Cerebral Ischemia Induced Hippocampal CA1 Injury in Aging Mice. J Neurol Disord. 2014;2:1000174.
12 Specific binding of the new stable epoprostenol analogue beraprost sodium to prostacyclin receptors on human and rat platelets. Arzneimittelforschung. 1989 Apr;39(4):495-9.
13 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
14 Protective effect of a prostaglandin I2 analog, TEI-7165, on ischemic neuronal damage in gerbils. Brain Res. 1997 Sep 26;769(2):321-8.
15 Pharmacokinetics of intravenous ataprost alfadex, a new prostaglandin I2 analog in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1993 Aug;31(8):373-5.
16 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
17 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
18 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
19 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
20 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
21 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
22 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
23 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
24 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
25 Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
26 Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
27 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
28 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
29 New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126.
30 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
31 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
32 Targeting multiple cannabinoid anti-tumour pathways with a resorcinol derivative leads to inhibition of advanced stages of breast cancer. Br J Pharmacol. 2014 Oct;171(19):4464-77. doi: 10.1111/bph.12803. Epub 2014 Sep 5.
33 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.
34 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
35 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
36 Retinoic acid-induced downmodulation of telomerase activity in human cancer cells. Exp Mol Pathol. 2005 Oct;79(2):108-17.
37 Study of As(2)O(3) regulating proliferation and apoptosis of Tca8113 cells by inhibiting the expression of Id-1. Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1932-1937. doi: 10.1080/21691401.2019.1613419.
38 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
39 THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
40 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
41 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.