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

General Information of Drug (ID: DMPEHBJ)

• Drug Name: OX-NLA Drug Info
• Synonyms: NLA; BLX-NLA; NCX-1510; NO-donating therapeutics, Biolipox; Anti-allergy drug, NicOx/Biolipox; NO-donating allergy therapeutics, Biolipox/Nicox; NO-donating respiratory therapeutics, NicOx/Biolipox; NO-donating therapeutics, Biolipox/Nicox; Liposomal nitric oxide-donating cetirizine derivative (nasal, rhinitis), Biolipox; Nitric oxide-donating cetirizine derivative (liposomal, intranasal, rhinitis), Orexo; OX-NLA (nasal/liposomal formulation, allergic rhinitis/rhinitis); OX-NLA (nasal/liposomal formulation, allergic rhinitis/rhinitis), Meda

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Discontinued in Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 55182
  ChEBI ID: CHEMBL3562
  CAS Number: CAS 83881-52-1
  TTD Drug ID: DMPEHBJ

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine receptor (HR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Histamine Phosphate	DMV7IM6	Diagnostic imaging	N.A.	Approved	[4]
Repirinast	DM6KI0D	Asthma	CA23	Approved	[5]
Levomequitazine	DMAYC76	Seasonal allergic rhinitis	CA08.01	Phase 3	[6]
ETX-9101	DMZOA2L	Asthma	CA23	Phase 2	[7]
LCB-2183	DMY4IWC	Asthma	CA23	Phase 2	[8]
ETS-6218	DMV96BY	Fibromyalgia	MG30.01	Phase 2	[7]
Votucalis	DMW4LTI	Allergic rhinitis	CA08.0	Phase 2	[9]
Tesmilifene	DMPB36I	Breast cancer	2C60-2C65	Discontinued in Phase 2	[10]
CP-118	DMNJD9H	Allergic rhinitis	CA08.0	Discontinued in Phase 2	[11]
REV-598	DM314CZ	Carcinoid syndrome	5B10	Terminated	[12]

Drug(s) Affected By ATP-dependent translocase ABCB1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flupentixol	DM0DJ9O	Schizophrenia	6A20	Approved	[13]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[14]
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[15]
Lamotrigine	DM8SXYG	Bipolar disorder	6A60	Approved	[16]
Cepharanthine	DM9Y5JB	N. A.	N. A.	Approved	[17]
Itraconazole	DMCR1MV	Aspergillosis	1F20	Approved	[18]
Clozapine	DMFC71L	Schizophrenia	6A20	Approved	[19]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[20]
Trifluoperazine	DMKBYWI	Anxiety		Approved	[21]
Olanzapine	DMPFN6Y	Bipolar depression		Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine receptor (HR)	TT7CXIM	NOUNIPROTAC	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
ATP-dependent translocase ABCB1 (ABCB1)	OTEJROBO	MDR1_HUMAN	Regulation of Drug Effects	[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 800020184)
• [2] Clinical pipeline report, company report or official report of Orexo.
• [3] P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos. 2003 Mar;31(3):312-8.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. Br J Pharmacol. 1992 Mar;105(3):587-90.
• [6] Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes. J Pharmacol Exp Ther. 1998 Feb;284(2):437-42.
• [7] Clinical pipeline report, company report or official report of e-Therapeutics.
• [8] LCB 2183 inhibits the inflammation associated with oxazolone-induced contact sensitivity. Int J Immunopharmacol. 1994 Aug;16(8):675-83.
• [9] CA patent application no. 520580, Histamine binding compounds for treatment method for disease conditions mediated by neutrophils.
• [10] Effects of tesmilifene, a substrate of CYP3A and an inhibitor of P-glycoprotein, on the pharmacokinetics of intravenous and oral docetaxel in rats. J Pharm Pharmacol. 2010 Aug;62(8):1084-8.
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025139)
• [12] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)
• [13] Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
• [14] Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
• [15] Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
• [16] Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
• [17] Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
• [18] Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
• [19] Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
• [20] Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
• [21] Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.