General Information of Drug (ID: DMF3AN7)

Drug Name
Loratadine Drug Info
Synonyms
Aerotina; Alarin; Alavert; Alerpriv; Allertidin; Anhissen; Biloina; Bonalerg; Civeran; Claratyne; Clarinase; Claritin; Claritine; Clarityn; Clarityne; Clarium; Fristamin; Histaloran; Lergy; Lertamine; Lesidas; Lisino; Loracert; Loradex; Loradif; Loranox; Lorantis; Lorastine; Loratadina; Loratadinum; Loratidine; Loratyne; Loraver; Lorfast; Loritine; Lowadina; Nularef; Optimin; Polaratyne; Pylor; Restamine; Rhinase; Rinomex; Roletra; Sanelor; Sensibit; Sohotin; Tadine; Velodan; Versal; Zeos; Bedix Loratadina; Claratyne Cold; Claratyne Decongestant; Clarinase Reperabs; Claritin D; Claritin Hives Relief; Claritin Hives Relief Reditab; Claritin Reditabs; Claritin reditab; Clarityne Dy Repetabs; Loratadina [Spanish]; Loratadine Redidose; Loratadine Wyeth Brand; Loratadinum [Latin]; Sinhistan Dy; Talorat Dy; Wyeth Brand of Loratadine; L 9664; Sch 29851; Sch29851; Alavert (TN); AllergyX (TN); Children's Claritin; Claritin (TN); Claritine (TN); Clarityn (TN); Clarityne (TN); Clarityne-D; Flonidan (TN); Fristamin (TN); Lomilan (TN); Lorfast (TN); Rinolan (TN); Roletra (TN); Sch-29851; Symphoral (TN); Tidilor (TN); Alavert, Claritin, Loratadine; Loratadine [USAN:BAN:INN]; Loratadine (JAN/USAN/INN); Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidine-1-carboxylate; Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylate; 1-Piperidenecarboxylic acid, 4-(8-chloro-5,6-duhydro-11H-benzo [5,6]cyclohepta[1,2-b]-pyridin-11-ylidene)-, ethyl ester; 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-, ethyl ester; 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester; 1-piperidinecarboxylic acid,4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-,ethyl ester; 4-(8-Chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylic Acid Ethyl Ester; 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene-1-piperidinecarboxylic acidethyl ester; 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cycloheptal[1,2-b]pyridin-11-ylidene-1-piperidinecarboxylic acid ethyl ester
Indication
Disease Entry ICD 11 Status REF
Allergy 4A80-4A85 Approved [1] , [2]
Allergic rhinitis CA08.0 Discontinued in Phase 2 [3]
Therapeutic Class
Antihistamines
Cross-matching ID
PubChem CID
3957
ChEBI ID
CHEBI:6538
CAS Number
CAS 79794-75-5
TTD Drug ID
DMF3AN7
VARIDT Drug ID
DR00541
INTEDE Drug ID
DR0977
ACDINA Drug ID
D00374

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [4] , [5] , [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [8]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [9]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [10]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [11]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [12]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [12]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [12]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [13]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Histamine H1 receptor (H1R) DTT HRH1 5.972 5.7 5.816 6.002
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Allergy
ICD Disease Classification 4A80-4A85
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.74E-01 0.13 0.43
P-glycoprotein 1 (ABCB1) DTP P-GP 6.54E-01 1.95E-01 4.04E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 5.57E-01 -7.89E-02 -7.93E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 4.32E-01 4.39E-02 4.30E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 8.46E-01 -6.63E-03 -4.49E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.57E-01 9.43E-03 1.29E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 9.62E-01 2.57E-02 1.10E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.70E-01 2.98E-02 1.22E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.35E-01 2.78E-02 2.09E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.76E-01 1.26E-01 8.27E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

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2 Desloratadine treatment for intermittent and persistent allergic rhinitis: a review. Clin Ther. 2007 Sep;29(9):1795-802.
3 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015252)
4 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
5 Second-generation antihistamines: a comparative review. Drugs. 1999 Jan;57(1):31-47.
6 Effect of descarboethoxyloratadine, the major metabolite of loratadine, on the human cardiac potassium channel Kv1.5. Br J Pharmacol. 1997 Nov;122(5):796-8.
7 P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos. 2003 Mar;31(3):312-8.
8 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
9 In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes. Drug Metab Dispos. 2001 Sep;29(9):1173-5.
10 In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact. 1999 Nov 15;123(1):63-79.
11 Advances in high-resolution MS and hepatocyte models solve a long-standing metabolism challenge: the loratadine story. Bioanalysis. 2016 Aug;8(16):1645-62.
12 Metabolism of loratadine and further characterization of its in vitro metabolites. Drug Metab Lett. 2009 Aug;3(3):162-70.
13 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.