bilastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antihistaminics 4353 202189-78-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bellozal
  • F-96221-BM1
  • bilastine
  • bilaxten
  • Molecular weight: 463.62
  • Formula: C28H37N3O3
  • CLOGP: 1.95
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 67.59
  • ALOGS: -5.36
  • ROTB: 10

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.61 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.87 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.13 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.16 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 0.61 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.462 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 22.233 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 3.784 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.661 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 37.380 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 43.870 % High 1
herg hERG pIC50 4.951 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 0.859 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 2.931 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 30.880 % High 1
kinase-safety-class ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PRKDC 7
kinase-selectivity-class AXL,EIF2AK3 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 9.638 High 1
mh-clint Mouse hepatocyte intrinsic clearance 10.495 High 1
mppb Mouse plasma protein binding (% unbound) 38.800 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 14.191 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 41.390 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.207 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 77.780 % High 1
rppb Rat plasma protein binding (% unbound) 35.620 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 979.490 uM High 1

Approvals:

DateAgencyCompanyOrphan
None PMDA

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
Urticaria 460.10 18.75 353 11234 312381 90304479
Angioedema 193.53 18.75 114 11473 64762 90552098
Pruritus 178.18 18.75 277 11310 541248 90075612
Chronic spontaneous urticaria 155.93 18.75 38 11549 1782 90615078
Skin plaque 109.63 18.75 43 11544 9932 90606928
Erythema 94.90 18.75 131 11456 229115 90387745
Anaphylactic reaction 77.15 18.75 74 11513 87450 90529410
Urticaria chronic 75.16 18.75 18 11569 783 90616077
Inappropriate schedule of product administration 68.57 18.75 90 11497 149843 90467017
Mast cell activation syndrome 67.39 18.75 19 11568 1575 90615285
Scratch 66.37 18.75 30 11557 9836 90607024
Urticaria thermal 65.99 18.75 15 11572 518 90616342
Urticarial vasculitis 65.53 18.75 17 11570 1028 90615832
Inflammatory bowel disease 59.32 18.75 23 11564 5148 90611712
Face oedema 59.22 18.75 37 11550 23281 90593579
Incorrect dose administered 55.38 18.75 59 11528 78871 90537989
Monocyte count abnormal 52.45 18.75 11 11576 259 90616601
Product availability issue 48.18 18.75 22 11565 7382 90609478
Illness 46.75 18.75 55 11532 81914 90534946
Middle insomnia 46.15 18.75 28 11559 16723 90600137
Administration site erythema 43.77 18.75 12 11575 897 90615963
Perfume sensitivity 42.70 18.75 12 11575 983 90615877
Lip swelling 42.51 18.75 37 11550 38573 90578287
Stress 42.14 18.75 52 11535 81343 90535517
Lymphocyte count abnormal 39.47 18.75 11 11576 874 90615986
Mouth breathing 39.29 18.75 8 11579 162 90616698
Pharyngeal swelling 39.18 18.75 21 11566 9923 90606937
Dizziness postural 38.16 18.75 20 11567 9033 90607827
Asthma 37.15 18.75 90 11497 242070 90374790
Insomnia 37.09 18.75 110 11477 333364 90283496
Death 36.64 18.75 7 11580 456544 90160316
Pigmentation disorder 36.59 18.75 17 11570 5932 90610928
Systemic lupus erythematosus 35.14 18.75 3 11584 361893 90254967
Nasal congestion 34.93 18.75 48 11539 83366 90533494
Cold urticaria 34.61 18.75 8 11579 298 90616562
Heart rate increased 33.08 18.75 55 11532 112847 90504013
Swelling face 32.85 18.75 46 11541 81306 90535554
Mandibular mass 32.63 18.75 7 11580 184 90616676
Diverticulum oesophageal 32.31 18.75 7 11580 193 90616667
Cough 32.20 18.75 112 11475 368850 90248010
Malaise 30.71 18.75 152 11435 585834 90031026
Loose tooth 30.41 18.75 13 11574 3730 90613130
Hepatic enzyme increased 30.09 18.75 5 11582 360731 90256129
Myalgia 30.02 18.75 68 11519 175057 90441803
Throat tightness 29.95 18.75 27 11560 29457 90587403
Exposure to allergen 29.95 18.75 8 11579 542 90616318
Oropharyngeal spasm 29.44 18.75 7 11580 295 90616565
Allergy to animal 28.78 18.75 10 11577 1644 90615216
Rhinorrhoea 28.56 18.75 45 11542 88271 90528589
Bruxism 28.50 18.75 13 11574 4350 90612510
Oropharyngeal pain 28.39 18.75 52 11535 115135 90501725
Skin lesion 28.10 18.75 29 11558 37336 90579524
Prescription form tampering 27.74 18.75 8 11579 719 90616141
Blood pressure systolic increased 26.60 18.75 35 11552 58310 90558550
Carcinoid syndrome 26.15 18.75 6 11581 216 90616644
Quality of life decreased 25.58 18.75 17 11570 11872 90604988
Contraindicated product administered 25.47 18.75 5 11582 320134 90296726
Nasal disorder 25.32 18.75 11 11576 3281 90613579
Functional residual capacity increased 24.91 18.75 5 11582 94 90616766
Eosinophilia 24.88 18.75 24 11563 28509 90588351
Lactic acidosis 24.14 18.75 31 11556 50432 90566428
Papule 23.66 18.75 14 11573 7988 90608872
Joint swelling 23.51 18.75 18 11569 503282 90113578
Herpes dermatitis 23.44 18.75 5 11582 128 90616732
Therapeutic response shortened 23.33 18.75 21 11566 22858 90594002
Oropharyngeal oedema 23.14 18.75 6 11581 362 90616498
Dyshidrotic eczema 23.03 18.75 7 11580 754 90616106
Lymphadenopathy mediastinal 22.48 18.75 10 11577 3157 90613703
Nerve compression 22.47 18.75 15 11572 10551 90606309
Haematoma 21.92 18.75 26 11561 39022 90577838
Vitamin B12 deficiency 21.88 18.75 13 11574 7473 90609387
Wound 21.59 18.75 6 11581 302974 90313886
Allergic oedema 21.50 18.75 7 11580 943 90615917
Secretion discharge 21.15 18.75 17 11570 15879 90600981
Allergy to chemicals 20.85 18.75 10 11577 3744 90613116
Cryopyrin associated periodic syndrome 20.56 18.75 6 11581 562 90616298
Stomatitis 20.41 18.75 5 11582 274693 90342167
Lichen planus 20.41 18.75 9 11578 2782 90614078
Faecal calprotectin increased 20.28 18.75 10 11577 3977 90612883
Cholestasis 20.09 18.75 24 11563 36275 90580585
Swollen tongue 20.07 18.75 27 11560 45929 90570931
Pericarditis 19.91 18.75 5 11582 270146 90346714
Histamine abnormal 19.74 18.75 3 11584 9 90616851
Nervousness 19.65 18.75 23 11564 34033 90582827
Influenza 19.48 18.75 50 11537 139214 90477646
Psoriatic arthropathy 19.40 18.75 3 11584 228332 90388528
Synovitis 19.31 18.75 9 11578 329743 90287117
Heart rate abnormal 19.11 18.75 11 11576 5960 90610900
Psychological trauma 19.08 18.75 7 11580 1346 90615514
Nasal pruritus 18.92 18.75 6 11581 744 90616116
Weight decreased 18.77 18.75 97 11490 379813 90237047

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
Urticaria 170.04 21.89 93 3321 73943 42543978
Pruritus 101.29 21.89 98 3316 188673 42429248
Angioedema 67.18 21.89 42 3372 42435 42575486
Angioimmunoblastic T-cell lymphoma 54.04 21.89 11 3403 362 42617559
Reversible cerebral vasoconstriction syndrome 46.54 21.89 11 3403 729 42617192
Rash maculovesicular 44.61 21.89 7 3407 48 42617873
Urticaria chronic 43.62 21.89 8 3406 150 42617771
Lip erythema 39.63 21.89 7 3407 105 42617816
Lichenoid keratosis 39.40 21.89 14 3400 3936 42613985
Nasal mucosal disorder 37.98 21.89 7 3407 135 42617786
Eosinophilia 36.23 21.89 26 3388 32873 42585048
Enanthema 32.52 21.89 8 3406 627 42617294
Asthma 30.71 21.89 31 3383 62283 42555638
Product availability issue 29.46 21.89 11 3403 3556 42614365
Eczema 28.81 21.89 23 3391 34063 42583858
Laryngeal discomfort 28.34 21.89 6 3408 240 42617681
Chronic spontaneous urticaria 27.31 21.89 6 3408 286 42617635
Conjunctival hyperaemia 26.98 21.89 10 3404 3166 42614755
SARS-CoV-2 test false positive 26.57 21.89 4 3410 20 42617901
Allergy to chemicals 26.04 21.89 5 3409 121 42617800
Mydriasis 25.66 21.89 13 3401 8757 42609164
Allergy to metals 25.48 21.89 5 3409 136 42617785
Genital ulceration 25.18 21.89 7 3407 884 42617037
Oral mucosa erosion 23.81 21.89 7 3407 1079 42616842
Lupus-like syndrome 23.42 21.89 9 3405 3145 42614776
Psychological trauma 22.98 21.89 5 3409 228 42617693
Death 22.79 21.89 5 3409 471180 42146741

FDA Adverse Event Reporting System (Geriatric)

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
Urticaria 577.99 17.22 414 14235 318443 110256207
Pruritus 267.09 17.22 355 14294 581205 109993445
Angioedema 201.08 17.22 138 14511 98362 110476288
Chronic spontaneous urticaria 171.24 17.22 42 14607 1951 110572699
Skin plaque 111.46 17.22 47 14602 12598 110562052
Erythema 102.33 17.22 157 14492 291290 110283360
Inappropriate schedule of product administration 87.89 17.22 121 14528 203516 110371134
Anaphylactic reaction 83.97 17.22 89 14560 114211 110460439
Product availability issue 75.16 17.22 31 14618 7859 110566791
Urticaria thermal 70.91 17.22 16 14633 515 110574135
Urticarial vasculitis 65.91 17.22 17 14632 969 110573681
Asthma 62.67 17.22 116 14533 250175 110324475
Mast cell activation syndrome 58.53 17.22 17 14632 1511 110573139
Scratch 57.53 17.22 30 14619 12949 110561701
Death 56.28 17.22 12 14637 698857 109875793
Urticaria chronic 55.05 17.22 14 14635 754 110573896
Face oedema 54.68 17.22 41 14608 33428 110541222
Middle insomnia 54.68 17.22 34 14615 20468 110554182
Illness 53.39 17.22 60 14589 82111 110492539
Incorrect dose administered 53.04 17.22 67 14582 103574 110471076
Administration site erythema 52.02 17.22 12 14637 427 110574223
Eosinophilia 51.44 17.22 50 14599 57886 110516764
Lip swelling 51.24 17.22 47 14602 50620 110524030
Inflammatory bowel disease 51.07 17.22 23 14626 7211 110567439
Pharyngeal swelling 45.43 17.22 25 14624 12007 110562643
Angioimmunoblastic T-cell lymphoma 42.38 17.22 11 14638 643 110574007
Perfume sensitivity 41.18 17.22 12 14637 1079 110573571
Dizziness postural 40.92 17.22 25 14624 14584 110560066
Rash maculovesicular 40.71 17.22 7 14642 51 110574599
Eczema 39.00 17.22 48 14601 72245 110502405
Stress 38.65 17.22 58 14591 105290 110469360
Malaise 36.79 17.22 181 14468 671638 109903012
Cough 36.50 17.22 139 14510 461502 110113148
Nasal congestion 35.90 17.22 54 14595 98228 110476422
Pigmentation disorder 35.58 17.22 18 14631 7293 110567357
Insomnia 34.85 17.22 116 14533 360474 110214176
Papule 32.71 17.22 19 14630 10114 110564536
Psychological trauma 32.18 17.22 11 14638 1662 110572988
Loose tooth 31.73 17.22 13 14636 3240 110571410
Diverticulum oesophageal 31.63 17.22 7 14642 206 110574444
Allergy to chemicals 31.45 17.22 13 14636 3312 110571338
Swelling face 31.29 17.22 49 14600 92272 110482378
Mandibular mass 30.71 17.22 7 14642 236 110574414
Myalgia 30.48 17.22 81 14568 222300 110352350
Lip erythema 30.05 17.22 8 14641 516 110574134
Throat tightness 29.91 17.22 29 14620 33460 110541190
Rash 29.67 17.22 198 14451 820766 109753884
Lichenoid keratosis 29.17 17.22 15 14634 6287 110568363
Heart rate increased 29.10 17.22 61 14588 143773 110430877
Skin lesion 27.39 17.22 34 14615 51597 110523053
Allergy to animal 27.00 17.22 10 14639 1906 110572744
Hepatic enzyme increased 26.85 17.22 5 14644 320887 110253763
Bruxism 26.38 17.22 13 14636 4981 110569669
Oropharyngeal pain 25.78 17.22 56 14593 135220 110439430
Influenza 25.65 17.22 64 14585 169037 110405613
Migraine 25.03 17.22 64 14585 171588 110403062
Cold urticaria 25.02 17.22 6 14643 253 110574397
Exposure to allergen 24.85 17.22 7 14642 558 110574092
Frustration tolerance decreased 24.60 17.22 15 14634 8716 110565934
Lichen planus 24.57 17.22 11 14638 3399 110571251
Conjunctival hyperaemia 24.48 17.22 13 14636 5818 110568832
Functional residual capacity increased 24.44 17.22 5 14644 100 110574550
Carcinoid syndrome 24.20 17.22 6 14643 291 110574359
Weight decreased 24.08 17.22 124 14525 467933 110106717
Mouth breathing 24.01 17.22 6 14643 301 110574349
Enanthema 23.95 17.22 8 14641 1126 110573524
SARS-CoV-2 test false positive 23.53 17.22 4 14645 27 110574623
Toxic skin eruption 23.03 17.22 23 14626 27492 110547158
Dyshidrotic eczema 22.85 17.22 7 14642 747 110573903
Eosinophilic granulomatosis with polyangiitis 21.83 17.22 15 14634 10671 110563979
Swollen tongue 21.80 17.22 33 14616 60329 110514321
Blood pressure systolic increased 21.41 17.22 39 14610 82952 110491698
Nasal pruritus 21.33 17.22 7 14642 933 110573717
Allergic oedema 21.27 17.22 7 14642 941 110573709
Lip oedema 21.27 17.22 13 14636 7587 110567063
Systemic lupus erythematosus 21.20 17.22 4 14645 254334 110320316
Oropharyngeal spasm 21.11 17.22 6 14643 494 110574156
Reversible cerebral vasoconstriction syndrome 21.08 17.22 11 14638 4750 110569900
Gluten sensitivity 20.95 17.22 6 14643 507 110574143
Confusional state 20.65 17.22 19 14630 468661 110105989
Rash maculo-papular 20.58 17.22 36 14613 74186 110500464
Atrial fibrillation 20.50 17.22 3 14646 229639 110345011
Nasal mucosal disorder 20.00 17.22 8 14641 1875 110572775
Cryopyrin associated periodic syndrome 19.78 17.22 6 14643 619 110574031
Alopecia 19.65 17.22 12 14637 364741 110209909
Histamine abnormal 19.63 17.22 3 14646 9 110574641
Eye discharge 19.58 17.22 13 14636 8741 110565909
Pemphigoid 19.37 17.22 18 14631 19689 110554961
Nasal disorder 19.37 17.22 10 14639 4224 110570426
Sinus polyp 19.36 17.22 6 14643 665 110573985
Food allergy 19.19 17.22 18 14631 19930 110554720
Nervousness 19.12 17.22 24 14625 36827 110537823
Rhinorrhoea 18.99 17.22 42 14607 102624 110472026
Nerve compression 18.98 17.22 14 14635 11123 110563527
Rheumatoid arthritis 18.91 17.22 8 14641 299605 110275045
Drug hypersensitivity 18.50 17.22 113 14536 453977 110120673
Laryngeal discomfort 18.45 17.22 6 14643 777 110573873
Dehydration 18.40 17.22 7 14642 279504 110295146
Haematoma 18.38 17.22 30 14619 58446 110516204
Herpes dermatitis 18.31 17.22 5 14644 355 110574295
Therapeutic response shortened 18.18 17.22 21 14628 29562 110545088
Quality of life decreased 18.06 17.22 15 14634 14154 110560496
Disease progression 18.02 17.22 5 14644 244029 110330621
Oral mucosa erosion 17.97 17.22 8 14641 2440 110572210
Vitamin B12 deficiency 17.96 17.22 13 14636 10042 110564608
Nasopharyngitis 17.91 17.22 101 14548 394260 110180390
Laryngitis allergic 17.55 17.22 3 14646 21 110574629

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AX29 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
ATC S01GX13 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
CHEBI has role CHEBI:50857 anti-allergic agent
CHEBI has role CHEBI:66981 ophthalmology drug

Related Drugs by ATC class:

R06AX Other antihistamines for systemic use 26 drugs
acrivastineantazolineastemizoleazatadineazelastinebamipinecyproheptadinedeptropinedesloratadineebastineepinastinefexofenadine show all 26 →
S01GX Other antiallergics 12 drugs
alcaftadineazelastinecetirizinecromoglicic acidemedastineepinastineketotifenlevocabastinelodoxamidenedocromilolopatadinespaglumic acid

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Urticaria indication 126485001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.42 acidic
pKa2 7.88 Basic
pKa3 5.11 Basic

Orange Book patent data (new drug applications)

None

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 7.19 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
D09570 KEGG_DRUG
C1101148 UMLSCUI
CHEBI:135954 CHEBI
CHEMBL1742423 ChEMBL_ID
DB11591 DRUGBANK_ID
C445659 MESH_SUPPLEMENTAL_RECORD_UI
11579 IUPHAR_LIGAND_ID
7905 INN_ID
PA1123N395 UNII
185460 PUBCHEM_CID
013709 NDDF
697973006 SNOMEDCT_US
714622001 SNOMEDCT_US
PA1123N395 INXIGHT DRUGS

Pharmaceutical products:

None