General Information of Drug (ID: DMCHV4I)

Drug Name
Rifapentine Drug Info
Synonyms
RIFAPENTINE; Rifapentina; Rifapentinum; Cyclopentylrifampicin; Rifamycin AF/ACPP; Antibiotic DL 473IT; KTC 1; 61379-65-5; MDL 473; DRG-0283; DL 473; R-773; R 77-3; 3-(N-(4-Cyclopentyl-1-piperazinyl)formimidoyl)rifamycin; 3-(4-Cyclopentyl-1-piperazinyl)iminomethylrifamycin SV; 3-(((4-Cyclopentyl-1-piperazinyl)imino)methyl)rifamycin; Rifapentin,(S); NCGC00167431-01; ZINC169621228; NCGC00167431-03; AN-15578; RPE
Indication
Disease Entry ICD 11 Status REF
Pulmonary tuberculosis 1B10.Z Approved [1]
Tuberculosis 1B10-1B1Z Approved [2]
Macular degeneration 9B78.3 Investigative [3]
Therapeutic Class
Antituberculosis Agents
Cross-matching ID
PubChem CID
135403821
ChEBI ID
CHEBI:45304
CAS Number
CAS 61379-65-5
TTD Drug ID
DMCHV4I
INTEDE Drug ID
DR1421
ACDINA Drug ID
D00592

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rifabutin DM1YBHK Mycobacterium infection 1B10-1B21 Approved [9]
Rifaximin DR DMKTS2M Crohn disease DD70 Phase 3 [10]
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [11]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [12]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [13]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [14]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [15]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [16]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [17]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [18]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [12]
Verapamil DMA7PEW Angina pectoris BA40 Approved [19]
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [20]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [21]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [22]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [23]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [24]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [24]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [25]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [26]
Capsaicin DMGMF6V Back pain ME84.Z Approved [27]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [28]
⏷ Show the Full List of 20 Drug(s)
Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [29]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [30]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [30]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [31]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [29]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [30]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [32]
Gefitinib DM15F0X Colon adenocarcinoma Approved [29]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [7]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [33]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [34]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [35]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [36]
Fenofibrate DMFKXDY Coronary atherosclerosis Approved [34]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [34]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [37]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [35]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [6]
Flutamide DMK0O7U Prostate cancer 2C82.0 Approved [38]
⏷ 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
DNA-directed RNA polymerase (RNAP) TTHKJLN NOUNIPROTAC Binder [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Arylacetamide deacetylase (AADAC) OT8VACT2 AAAD_HUMAN Biotransformations [6]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [7]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Gene/Protein Processing [8]

References

1 Rifapentine FDA Label
2 Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8.
3 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
4 Contribution of rpoB mutations to development of rifamycin cross-resistance in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 1998 Jul;42(7):1853-7.
5 Inhibitory potential of twenty five anti-tuberculosis drugs on CYP activities in human liver microsomes. Biol Pharm Bull. 2015;38(9):1425-9.
6 Human arylacetamide deacetylase is responsible for deacetylation of rifamycins: rifampicin, rifabutin, and rifapentine. Biochem Pharmacol. 2011 Dec 1;82(11):1747-56.
7 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
8 Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction. Drug Metab Dispos. 2006 Oct;34(10):1742-8.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
11 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
12 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
13 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
14 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
15 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
16 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
17 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
18 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
19 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
20 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
21 Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
22 Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
23 The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
24 Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
25 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
26 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
27 Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
28 Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
29 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
30 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
31 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
32 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
33 Methotrexate modulates folate phenotype and inflammatory profile in EA.hy 926 cells. Eur J Pharmacol. 2014 Jun 5;732:60-7.
34 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
35 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.
36 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.
37 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
38 Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse. Drug Metab Dispos. 2012 Apr;40(4):671-9. doi: 10.1124/dmd.111.043067. Epub 2011 Dec 29.