fexofenadine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1170 83799-24-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fexofenadine
  • terfenadine carboxylate
  • fexofenadine hydrochloride
  • fexofenadine HCl
a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; ; RN refers to HCl
  • Molecular weight: 501.67
  • Formula: C32H39NO4
  • CLOGP: 1.96
  • LIPINSKI: 1
  • HAC: 5
  • HDO: 3
  • TPSA: 81
  • ALOGS: -5.28
  • ROTB: 10

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.12 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 25 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.13 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 70 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
July 25, 1996 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug ineffective 267.12 39.02 110 565 101514 2255896
Angioedema 177.85 39.02 45 630 8351 2349059
Chronic spontaneous urticaria 172.23 39.02 22 653 61 2357349
Urticaria 134.61 39.02 46 629 24215 2333195
Pruritus 125.71 39.02 51 624 43289 2314121
Drug hypersensitivity 111.99 39.02 48 627 46595 2310815
Completed suicide 109.17 39.02 38 637 20996 2336414
Condition aggravated 104.17 39.02 41 634 31938 2325472
Palpitations 102.06 39.02 34 641 16422 2340988
Insomnia 97.95 39.02 37 638 25750 2331660
Chest discomfort 85.83 39.02 29 646 14566 2342844
Oesophagitis 74.57 39.02 17 658 1989 2355421
Haemoglobin abnormal 73.47 39.02 14 661 681 2356729
Dyspnoea 63.74 39.02 39 636 78694 2278716
Skin infection 63.20 39.02 14 661 1436 2355974
Dizziness 63.17 39.02 35 640 58630 2298780
White blood cell count abnormal 60.77 39.02 12 663 703 2356707
Neutrophil count abnormal 59.90 39.02 11 664 436 2356974
Asthma 56.77 39.02 20 655 11294 2346116
Arrhythmia 51.76 39.02 16 659 6012 2351398
Incorrect product administration duration 50.70 39.02 13 662 2482 2354928
Hypoacusis 46.62 39.02 13 662 3412 2353998
Malaise 46.00 39.02 28 647 55557 2301853
Electrocardiogram QT prolonged 43.74 39.02 15 660 7799 2349611
Lip swelling 42.23 39.02 13 662 4808 2352602
Foetal exposure during pregnancy 41.13 39.02 13 662 5239 2352171
Maternal exposure during pregnancy 41.02 39.02 17 658 14846 2342564

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 259.60 43.94 66 271 16246 1730198
Toxicity to various agents 61.97 43.94 26 311 29115 1717329
Drug ineffective 45.26 43.94 27 310 63774 1682670

Pharmacologic Action:

SourceCodeDescription
ATC R06AX26 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:37955 H1-receptor antagonist
CHEBI has role CHEBI:50857 anti-allergic agent
FDA MoA N0000000190 Histamine H1 Receptor Antagonists
FDA EPC N0000175587 Histamine-1 Receptor Antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Sneezing indication 76067001
Chronic idiopathic urticaria indication 302162004
Seasonal allergic rhinitis indication 367498001
Allergic conjunctivitis indication 473460002 DOID:11204
Urticaria off-label use 126485001
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Diabetes mellitus contraindication 73211009 DOID:9351
Kidney disease contraindication 90708001 DOID:557
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Hypertensive urgency contraindication 443482000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.66 acidic
pKa2 8.85 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
180MG ALLEGRA-D 24 HOUR ALLERGY AND CONGESTION SANOFI AVENTIS US N021704 Jan. 24, 2011 OTC TABLET, EXTENDED RELEASE ORAL 6613357 Dec. 25, 2020 RELIEF OF SYMPTOMS ASSOCIATED WITH RESPIRATORY ALLERGIES, SWELLING OF THE NASAL PASSAGES AND SINUS CONGESTION AND PRESSURE IN ADULTS AND CHILDREN 12 YEARS OF AGE AND OLDER
30MG CHILDREN'S ALLEGRA ALLERGY SANOFI AVENTIS US N021909 Jan. 24, 2011 DISCN TABLET, ORALLY DISINTEGRATING ORAL 6723348 Nov. 26, 2021 RELIEF OF SYMPTOMS ASSOCIATED WITH RESPIRATORY ALLERGIES ADULTS AND CHILDREN 6 YEARS OF AGE AND OLDER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 8 WOMBAT-PK CHEMBL
Multidrug resistance protein 1 Transporter Km 5.70 WOMBAT-PK
Solute carrier organic anion transporter family member 1A2 Unclassified Km 5.70 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.67 CHEMBL

External reference:

IDSource
4024052 VUID
N0000022057 NUI
C0296800 UMLSCUI
D00671 KEGG_DRUG
2S068B75ZU UNII
153439-40-8 SECONDARY_CAS_RN
108650005 SNOMEDCT_US
4024052 VANDF
006063 NDDF
d04040 MMSL
87636 RXNORM
372522002 SNOMEDCT_US
CHEMBL914 ChEMBL_ID
DB00950 DRUGBANK_ID
CHEMBL1200618 ChEMBL_ID
7469 INN_ID
CHEBI:5050 CHEBI
3348 PUBCHEM_CID
4819 IUPHAR_LIGAND_ID
C093230 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Good Sense Aller Ease HUMAN OTC DRUG LABEL 1 0113-0425 TABLET, FILM COATED 60 mg ORAL ANDA 9 sections
good sense aller ease HUMAN OTC DRUG LABEL 1 0113-0571 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
basic care allergy HUMAN OTC DRUG LABEL 1 0113-7425 TABLET, FILM COATED 60 mg ORAL ANDA 9 sections
basic care allergy HUMAN OTC DRUG LABEL 1 0113-7571 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
Fexofenadine Hydrochloride and Pseudoephedrine Hydrochloride HUMAN OTC DRUG LABEL 2 0363-0094 TABLET, FILM COATED, EXTENDED RELEASE 60 mg ORAL ANDA 11 sections
Fexofenadine hydrochloride HUMAN OTC DRUG LABEL 1 0363-0095 TABLET, FILM COATED 60 mg ORAL ANDA 14 sections
Fexofenadine hydrochloride HUMAN OTC DRUG LABEL 1 0363-0097 TABLET, FILM COATED 180 mg ORAL ANDA 14 sections
wal fex allergy HUMAN OTC DRUG LABEL 1 0363-0571 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
Wal Fex 24 Hour Allergy HUMAN OTC DRUG LABEL 1 0363-0600 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
Wal-Fex HUMAN OTC DRUG LABEL 1 0363-0784 TABLET 180 mg ORAL ANDA 10 sections
Wal Fex HUMAN OTC DRUG LABEL 1 0363-0903 TABLET, FILM COATED 60 mg ORAL ANDA 9 sections
Indoor Outdoor Allergy Relief HUMAN OTC DRUG LABEL 1 0363-0904 TABLET, COATED 180 mg ORAL ANDA 9 sections
Fexofenadine HCl and Pseudoephedrine HCI HUMAN OTC DRUG LABEL 2 0363-1606 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 10 sections
Fexofenadine Hydrochloride and Pseudoephedrine Hydrochloride HUMAN OTC DRUG LABEL 2 0363-2110 TABLET, FILM COATED, EXTENDED RELEASE 60 mg ORAL ANDA 15 sections
Fexofenadine Hydrochloride HUMAN OTC DRUG LABEL 1 0363-9898 TABLET, FILM COATED 180 mg ORAL ANDA 15 sections
Fexofenadine Hydrochloride HUMAN OTC DRUG LABEL 1 0378-0781 TABLET, FILM COATED 60 mg ORAL ANDA 9 sections
Fexofenadine Hydrochloride HUMAN OTC DRUG LABEL 1 0378-0782 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
Fexofenadine HCl and Pseudoephedrine HCI HUMAN OTC DRUG LABEL 2 0536-1242 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 9 sections
Fexofenadine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-5619 TABLET, FILM COATED 180 mg ORAL NDA 12 sections
Fexofenadine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-5620 TABLET, FILM COATED 60 mg ORAL NDA 12 sections
Fexofenadine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7636 TABLET, FILM COATED 60 mg ORAL ANDA 15 sections
Fexofenodine Hydrochloride HUMAN OTC DRUG LABEL 1 0615-7695 TABLET, FILM COATED 60 mg ORAL ANDA 9 sections
Fexofenadine Hydrochloride HUMAN OTC DRUG LABEL 1 0615-7696 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
Fexofenadine hydrochloride HUMAN OTC DRUG LABEL 1 0904-6711 TABLET 180 mg ORAL ANDA 9 sections
Allergy Relief HUMAN OTC DRUG LABEL 1 0904-6978 TABLET, COATED 180 mg ORAL ANDA 9 sections
Fexofenadine Hydrochloride HUMAN OTC DRUG LABEL 1 0904-7050 TABLET 180 mg ORAL ANDA 9 sections
Allergy HUMAN OTC DRUG LABEL 1 10202-107 TABLET 180 mg ORAL ANDA 9 sections
Fexofenadine hydrochloride HUMAN OTC DRUG LABEL 1 10202-229 TABLET, FILM COATED 180 mg ORAL ANDA 14 sections
7 Select Allergy Relief HUMAN OTC DRUG LABEL 1 10202-571 TABLET, FILM COATED 180 mg ORAL ANDA 9 sections
Fexofenadine Hydrochloride HUMAN OTC DRUG LABEL 1 10544-231 TABLET, FILM COATED 60 mg ORAL ANDA 9 sections