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

General Information of Drug (ID: DM4Y1SP)

• Drug Name: Carisbamate Drug Info
• Synonyms: Comfyde; JNJ 10234094; RWJ 333369; YKP 509; Carisbamate (USAN); JNJ-10234094; RWJ-333369; YKP-509; S-2-O-Carbamoyl-1-o-chlorophenyl-ethanol; [(2S)-2-(2-chlorophenyl)-2-hydroxyethyl] carbamate

Indication

Disease Entry	ICD 11	Status	REF
Epilepsy	8A60-8A68	Phase 3	[1]
Focal dystonia	8A02.1	Phase 3	[1]
Seizure disorder	8A6Z	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 6918474
  ChEBI ID: CHEBI:135966
  CAS Number: CAS 194085-75-1
  TTD Drug ID: DM4Y1SP
  INTEDE Drug ID: DR1891

Molecule-Related Drug Atlas

Drug(s) Targeting Sodium channel unspecific (NaC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Phenytoin	DMNOKBV	Epilepsy	8A60-8A68	Approved	[3]
Carbamazepine	DMZOLBI	Epilepsy	8A60-8A68	Approved	[4]
Zonisamide	DM0DTF7	Alcohol dependence	6C40.2	Approved	[5]
Eslicarbazepine	DMZREFQ	Seizure disorder	8A6Z	Approved	[1]
LIDOFLAZINE	DMV23GL	Angina pectoris	BA40	Approved	[6]
LOMERIZINE	DME0TC8	Migraine	8A80	Approved	[7]
Levobupivacaine	DM783CH	Anaesthesia	9A78.6	Approved	[8]
Tetrodotoxin	DMWMPRG	Bacterial infection	1A00-1C4Z	Approved	[9]
Permethrin	DMZ0Q1G	Pediculus capitis infestation	1G00.0	Approved	[10]
Rufinamide	DMWE60C	Epilepsy	8A60-8A68	Approved	[11]

Drug(s) Metabolized By UDP-glucuronosyltransferase 1A1 (UGT1A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[12]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[13]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[14]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[15]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[16]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[17]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[18]
Metronidazole	DMTIVEN	Abscess		Approved	[19]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[20]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Sodium channel unspecific (NaC)	TTRK8B9	NOUNIPROTAC	Blocker	[1]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME	DEYGVN4	UD11_HUMAN	Substrate	[2]

References

• [1] Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43.
• [2] Carisbamate addon therapy for drugresistant partial epilepsy. The Cochrane Library. John Wiley Sons, Ltd, 2016.
• [3] Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68.
• [4] Sidedness of carbamazepine accessibility to voltage-gated sodium channels. Mol Pharmacol. 2014 Feb;85(2):381-7.
• [5] Antiepileptic drugs and relapse after epilepsy surgery. Epileptic Disord. 2008 Sep;10(3):193-8.
• [6] Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. J Med Chem. 1994 Jan 21;37(2):268-74.
• [7] Medicinal chemistry of neuronal voltage-gated sodium channel blockers. J Med Chem. 2001 Jan 18;44(2):115-37.
• [8] Block of neuronal tetrodotoxin-resistant Na+ currents by stereoisomers of piperidine local anesthetics. Anesth Analg. 2000 Dec;91(6):1499-505.
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] In vitro assays for repellents and deterrents for ticks: differing effects of products when tested with attractant or arrestment stimuli. Med Vet Entomol. 2003 Dec;17(4):370-8.
• [11] Emerging drugs for epilepsy. Expert Opin Emerg Drugs. 2007 Sep;12(3):407-22.
• [12] Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
• [13] Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
• [14] Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
• [15] UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
• [16] Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
• [17] Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
• [18] Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
• [19] Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
• [20] Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
• [21] Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.