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

General Information of Drug (ID: DM1SMAI)

• Drug Name: Eperisone Drug Info
• Synonyms: EMPP; Myonal; Myorelark; E-0646; E-2000; E-646; Eperisone (transdermal patch); Eperisone (oral), Eisai; Eperisone (transdermalpatch), Eisai; E-2000 (oral), Eisai; E-2000 (transdermal patch), Eisai

Indication

Disease Entry	ICD 11	Status	REF
Muscle spasm	MB47.3	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 3236
  ChEBI ID: CHEBI:77070
  CAS Number: CAS 64840-90-0
  TTD Drug ID: DM1SMAI
  INTEDE Drug ID: DR0585

Molecule-Related Drug Atlas

Drug(s) Targeting Voltage-gated calcium channel (Cav)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tolperisone	DMA2GHJ	Muscle spasm	MB47.3	Approved	[4]
GCC-1290K	DMJ7WRI	Parkinson disease	8A00.0	Phase 1	[5]

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	[6]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[7]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[8]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[9]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[10]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[11]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[12]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[13]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[7]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[14]

Drug(s) Metabolized By Cytochrome P450 2J2 (CYP2J2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Riociguat	DMXBLMP	Chronic thromboembolic pulmonary hypertension		Approved	[15]
Rivaroxaban	DMQMBZ1	Deep vein thrombosis	BD71	Approved	[16]
Ergocalciferol	DMHO0AR	Hypoparathyroidism	5A50	Approved	[17]
Vorapaxar	DMA16BR	Myocardial infarction	BA41-BA43	Approved	[18]
Vitamin D	DMWQUC9	N. A.	N. A.	Approved	[17]
Alfacalcidol	DM1237M	Hyperparathyroidism	5A51	Phase 4	[17]
Ebastine	DMH21D9	N. A.	N. A.	Phase 4	[19]
MANIDIPINE	DMJPGUA	N. A.	N. A.	Phase 3	[20]
Carebastine	DMUVMWZ	Ocular allergy	4A81	Phase 3	[21]
H3B-6545	DMIFCY2	Breast cancer	2C60-2C65	Phase 1/2	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated calcium channel (Cav)	TTCRJKY	NOUNIPROTAC	Modulator	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[3]
Cytochrome P450 2J2 (CYP2J2)	DERSX5P	CP2J2_HUMAN	Substrate	[3]

References

• [1] ClinicalTrials.gov (NCT02040415) Phase 3 Study to Evaluate the Efficacy and Safety of DW-1030 and Eperisone HCl in Acute Back Pain Patients. U.S. National Institutes of Health.
• [2] Suppression of calcium current in a snail neurone by eperisone and its analogues. Eur J Pharmacol. 1989 Sep 22;168(3):299-305.
• [3] Characterization of human cytochrome P450 enzymes involved in the biotransformation of eperisone. Xenobiotica. 2009 Jan;39(1):1-10.
• [4] Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. J Pharmacol Exp Ther. 2005 Dec;315(3):1237-46.
• [5] Inhibitory effect of glutamate release from rat cerebrocortical synaptosomes by dextromethorphan and its metabolite 3-hydroxymorphinan. Neurochem Int. 2009 Jul;54(8):526-34.
• [6] 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.
• [7] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [8] 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.
• [9] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [10] 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.
• [11] 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.
• [12] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [13] 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.
• [14] 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.
• [15] Riociguat (adempas): a novel agent for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. P T. 2014 Nov;39(11):749-58.
• [16] Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85.
• [17] Characterization of rat and human CYP2J enzymes as Vitamin D 25-hydroxylases. Steroids. 2006 Oct;71(10):849-56.
• [18] Vorapaxar: the missing link in antiplatelet therapy! J Anaesthesiol Clin Pharmacol. 2017 Apr-Jun;33(2):269-270.
• [19] Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51.
• [20] Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine. Chem Biol Interact. 2019 Jun 1;306:1-9.
• [21] Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A. Drug Metab Dispos. 2006 Nov;34(11):1793-7.
• [22] Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERalpha covalent antagonist (SERCA). Cancer Chemother Pharmacol. 2019 Jan;83(1):151-160.