fexofenadine Indications/Contra | FAERs | Orange Book | 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

Drug dosage:

DoseUnitRoute
0.12 g O

Approvals:

DateAgencyCompanyOrphan
July 25, 1996 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System

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 386.57 37.32 116 1021 42329 4595526
Drug ineffective 358.96 37.32 161 976 185900 4451955
Chronic spontaneous urticaria 178.17 37.32 24 1113 115 4637740
Urticaria 174.99 37.32 63 1074 39510 4598345
Angioedema 157.11 37.32 49 1088 19716 4618139
Palpitations 146.08 37.32 49 1088 24797 4613058
Pruritus 131.67 37.32 61 1076 72511 4565344
Drug hypersensitivity 116.25 37.32 55 1082 68345 4569510
Toxicity to various agents 107.49 37.32 53 1084 71987 4565868
Dyspnoea 94.45 37.32 61 1076 138924 4498931
Insomnia 94.23 37.32 42 1095 45303 4592552
Condition aggravated 93.27 37.32 45 1092 58126 4579729
Incorrect product administration duration 93.06 37.32 23 1114 3904 4633951
Chest discomfort 91.26 37.32 34 1103 23176 4614679
Dizziness 75.54 37.32 47 1090 99824 4538031
Haemoglobin abnormal 63.35 37.32 14 1123 1457 4636398
Oesophagitis 62.96 37.32 17 1120 4071 4633784
Cardiac arrest 56.43 37.32 27 1110 33980 4603875
Lip swelling 55.36 37.32 18 1119 8161 4629694
Skin infection 54.85 37.32 14 1123 2694 4635161
White blood cell count abnormal 54.03 37.32 12 1125 1277 4636578
Neutrophil count abnormal 52.95 37.32 11 1126 853 4637002
Malaise 52.30 37.32 36 1101 90121 4547734
Arrhythmia 49.95 37.32 19 1118 13613 4624242
Asthma 48.88 37.32 20 1117 17354 4620501
Blood pressure increased 47.67 37.32 23 1114 29437 4608418
Maternal exposure during pregnancy 45.79 37.32 19 1118 17074 4620781
Somnolence 44.52 37.32 25 1112 43635 4594220
Electrocardiogram QT prolonged 44.36 37.32 18 1119 15277 4622578
Hypoacusis 43.15 37.32 14 1123 6295 4631560
Respiratory arrest 43.10 37.32 17 1120 13403 4624452
Rash 42.03 37.32 34 1103 108354 4529501
Tachycardia 40.59 37.32 21 1116 31124 4606731
Nausea 38.19 37.32 40 1097 177293 4460562

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