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

General Information of Drug (ID: DM8QTJI)

• Drug Name: Loteprednol Etabonate Drug Info
• Synonyms: Alrex; Locort; Loteflam; Lotemax; Loterox; CDDD-5604; HGP-1; IDR-90102; IDR-90103; Lotemax (TN); P-5604; Alrex, Lotemax, Loteprednol etabonate; Loteprednol etabonate (JAN/USAN); Chloromethyl 17alpha-[(ethoxycarbonyl)oxy]-11beta-hydroxy-3-oxoandrosta-1,4-diene-17beta-carboxylate; Chloromethyl (8S,9S,10R,11S,13S,14S,17R)-17-ethoxycarbonyloxy-11-hydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-17-carboxylate

Indication

Disease Entry	ICD 11	Status	REF
Eye inflammation	9A02	Approved	[1]

• Therapeutic Class: Antiallergic Agents
• Cross-matching ID:
  PubChem CID: 444025
  ChEBI ID: CHEBI:31784
  CAS Number: CAS 82034-46-6
  TTD Drug ID: DM8QTJI
  INTEDE Drug ID: DR0985

Molecule-Related Drug Atlas

Drug(s) Targeting Steroid hormone receptor ERR (ESRR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cortisone Acetate	DMG8K57	Acne vulgaris	ED80	Approved	[2]
Beclomethasone	DMZPHIK	Allergic rhinitis	CA08.0	Approved	[2]
Auranofin	DMWE2N4	Inflammatory arthritis	FA2Z	Approved	[2]
Desonide	DMTP2NJ	Allergic rhinitis	CA08.0	Approved	[2]
Fluocinonide	DM65KL8	Exanthem		Approved	[2]
Medrysone	DMJ90O5	Corneal abrasion	NA06.4	Approved	[2]
Halcinonide	DMGLAX1	Exanthem		Approved	[2]
Amcinonide	DMM1JL9	Exanthem		Approved	[2]
Prednicarbate	DMBUNVW	Exanthem		Approved	[2]
Flurandrenolide	DMHCI9S	Exanthem		Approved	[2]

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	[5]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[6]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[7]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[8]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[9]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[10]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[11]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[12]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[6]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[13]

Drug(s) Metabolized By Serum paraoxonase/arylesterase 1 (PON1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Prulifloxacin	DMOK965	Urinary tract infection	GC08	Approved	[14]
RTR-003632	DM45NHF	N. A.	N. A.	Phase 2	[15]
PARAOXON	DMN4ZKC	Discovery agent	N.A.	Investigative	[15]
gamma-butyrolactone	DMDCZWY	Discovery agent	N.A.	Investigative	[15]
Coumaranone	DM7TCPG	N. A.	N. A.	Investigative	[15]
Dihydrocoumarin	DMGLX1R	N. A.	N. A.	Investigative	[15]
Gamma-thiobutyrolactone	DM83HUI	N. A.	N. A.	Investigative	[15]
Homogentisic acid	DMQD0YW	N. A.	N. A.	Investigative	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Steroid hormone receptor ERR (ESRR)	TTP3UTW	ERR1_HUMAN; ERR2_HUMAN; ERR3_HUMAN	Modulator	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[3]
Serum paraoxonase/arylesterase 1 (PON1)	DESDN74	PON1_HUMAN	Substrate	[4]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7085).
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] EMC: Lotemax 0.5% w/v Eye Drops, Suspension.
• [4] Identification of esterase involved in the metabolism of two corticosteroid soft drugs. Biochem Pharmacol. 2017 Mar 1;127:82-89.
• [5] 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.
• [6] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [7] 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.
• [8] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [9] 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.
• [10] 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.
• [11] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [12] 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.
• [13] 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.
• [14] Paraoxonases-1, -2 and -3: what are their functions? Chem Biol Interact. 2016 Nov 25;259(Pt B):51-62.
• [15] Human serum paraoxonase (PON1) isozymes Q and R hydrolyze lactones and cyclic carbonate esters. Drug Metab Dispos. 2000 Nov;28(11):1335-42.