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

Stem definitionDrug idCAS RN
antiallergics, cromoglicic acid derivatives 741 16110-51-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sodium cromoglicate
  • cromolyn sodium
  • sodium cromolyn
  • sodium cromoglycate
  • cromoglicic acid
  • cromoglycic acid
  • cromolyn
  • cromoglycate
  • cromoglicate
  • intal
  • cromolyn disodium salt
  • cromolyn disodium
  • disodium cromoglycate
A chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.
  • Molecular weight: 468.37
  • Formula: C23H16O11
  • CLOGP: 1.48
  • LIPINSKI: 1
  • HAC: 11
  • HDO: 3
  • TPSA: 165.89
  • ALOGS: -4.12
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O
40 mg N
40 mg Inhal.aerosol
80 mg Inhal.powder
80 mg Inhal.solution

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 210 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 28.40 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -2.725 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.143 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.200 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.019 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 16.380 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 37.980 % High 1
herg hERG pIC50 4.571 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.303 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.412 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 4.890 % High 1
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,KDR,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 67
kinase-selectivity-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK9,DDR1,DYRK1B,ERBB2,GRK2,MAP2K6,MAP3K14,MAPK7,PIK3CB,PIK3CG,PRKDC,SIK2,STK33,TEK,TTK 21
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.533 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.054 High 1
mh-clint Mouse hepatocyte intrinsic clearance 1.253 High 1
mppb Mouse plasma protein binding (% unbound) 26.950 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.016 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 16.670 % High 1
rat-kpuu-brain Rat brain Kpuu 0.004 % High 1
rh-clint Rat hepatocyte intrinsic clearance 1.581 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 88.860 % High 1
rppb Rat plasma protein binding (% unbound) 5.490 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 891.251 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 28, 1982 FDA KING PHARMS

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
Treatment failure 201.75 21.59 152 4846 303776 90319673
Perfume sensitivity 115.99 21.59 23 4975 972 90622477
Mastocytosis 98.86 21.59 20 4978 936 90622513
Anaphylactic reaction 79.05 21.59 53 4945 87471 90535978
Mast cell activation syndrome 77.91 21.59 18 4980 1576 90621873
Urticaria 41.42 21.59 67 4931 312667 90310782
Skin reaction 40.52 21.59 20 4978 18533 90604916
Flushing 38.93 21.59 35 4963 88456 90534993
Scratch 38.67 21.59 16 4982 9850 90613599
Drug ineffective for unapproved indication 36.73 21.59 30 4968 66614 90556835
Oesophageal irritation 34.46 21.59 7 4991 334 90623115
Postural orthostatic tachycardia syndrome 33.93 21.59 10 4988 2262 90621187
Asthma 32.19 21.59 52 4946 242108 90381341
Bone pain 30.22 21.59 26 4972 61957 90561492
Conjunctivitis allergic 29.60 21.59 8 4990 1324 90622125
Food allergy 29.34 21.59 18 4980 25460 90597989
Feeling abnormal 28.01 21.59 40 4958 167195 90456254
Swelling face 27.81 21.59 28 4970 81324 90542125
Osteoporosis 22.21 21.59 27 4971 96504 90526945

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
Treatment failure 169.91 26.55 75 1989 62549 42556722
Mast cell activation syndrome 73.86 26.55 13 2051 325 42618946
Spleen congestion 35.06 26.55 7 2057 350 42618921
Meralgia paraesthetica 33.60 26.55 6 2058 163 42619108
Nasal inflammation 33.55 26.55 7 2057 436 42618835
Urticaria 33.28 26.55 28 2036 74008 42545263
Anaphylactic reaction 32.17 26.55 22 2042 42721 42576550
Penile erythema 31.65 26.55 6 2058 228 42619043
Hypertrichosis 31.46 26.55 7 2057 591 42618680
Food allergy 30.97 26.55 9 2055 2212 42617059
Mouth swelling 30.87 26.55 9 2055 2237 42617034
Asthma 26.83 26.55 23 2041 62291 42556980

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
Perfume sensitivity 115.50 19.37 23 5658 1068 110582550
Mastocytosis 109.22 19.37 21 5660 811 110582807
Anaphylactic reaction 76.39 19.37 56 5625 114244 110469374
Urticaria 71.76 19.37 85 5596 318772 110264846
Mast cell activation syndrome 69.18 19.37 16 5665 1512 110582106
Food allergy 46.53 19.37 22 5659 19926 110563692
Asthma 45.48 19.37 60 5621 250231 110333387
Skin reaction 39.38 19.37 20 5661 21124 110562494
Nasal disorder 36.36 19.37 12 5669 4222 110579396
Scratch 35.54 19.37 16 5665 12963 110570655
Swelling face 33.90 19.37 32 5649 92289 110491329
Penile erythema 32.64 19.37 6 5675 181 110583437
Flushing 32.30 19.37 33 5648 104703 110478915
Spleen congestion 32.30 19.37 7 5674 492 110583126
Postural orthostatic tachycardia syndrome 31.91 19.37 9 5672 1873 110581745
Oesophageal irritation 29.71 19.37 6 5675 299 110583319
Myalgia 29.61 19.37 46 5635 222335 110361283
Hypersensitivity 28.99 19.37 64 5617 403934 110179684
Nasal inflammation 27.37 19.37 7 5674 1006 110582612
Bone pain 26.67 19.37 24 5657 65109 110518509
Mouth swelling 26.47 19.37 11 5670 7343 110576275
Mechanical urticaria 25.83 19.37 6 5675 577 110583041
Meralgia paraesthetica 25.50 19.37 6 5675 611 110583007
pH body fluid increased 23.63 19.37 4 5677 74 110583544
Hypertrichosis 23.47 19.37 7 5674 1771 110581847
Injection site pruritus 23.21 19.37 20 5661 51238 110532380
Osteoporosis 22.51 19.37 25 5656 87127 110496491
Cardiac valve sclerosis 22.22 19.37 4 5677 107 110583511
Feeling abnormal 22.14 19.37 36 5645 180675 110402943
Migraine 22.13 19.37 35 5646 171617 110412001
Angioedema 21.65 19.37 26 5655 98474 110485144
Gastrointestinal submucosal tumour 21.35 19.37 4 5677 134 110583484
Viral uveitis 19.79 19.37 4 5677 200 110583418

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A07EB01 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
INTESTINAL ANTIINFLAMMATORY AGENTS
Antiallergic agents, excl. corticosteroids
ATC D11AH03 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Agents for dermatitis, excluding corticosteroids
ATC R01AC01 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Antiallergic agents, excl. corticosteroids
ATC R01AC51 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Antiallergic agents, excl. corticosteroids
ATC R03AK04 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AK05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03BC01 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Antiallergic agents, excl. corticosteroids
ATC S01GX01 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
ATC S01GX51 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
MeSH PA D000082142 Mast Cell Stabilizers
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D019141 Respiratory System Agents
FDA PE N0000175628 Decreased Histamine Release
FDA EPC N0000175630 Mast Cell Stabilizer
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:38215 calcium channel blocker
CHEBI has role CHEBI:49167 anti-asthmatic drug
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:77715 nasal decongestant
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:65023 anti-asthmatic agent
CHEBI has role CHEBI:66981 ophthalmology drug
CHEBI has role CHEBI:88188 drug allergen

Related Drugs by ATC class:

D11AH Agents for dermatitis, excluding corticosteroids 11 drugs
abrocitinibalitretinoincrisaboroledelgocitinibdupilumablebrikizumabnemolizumabpimecrolimusruxolitinibtacrolimustralokinumab
R01AC Antiallergic agents, excl. corticosteroids 7 drugs
antazolineazelastinelevocabastinenedocromilolopatadinespaglumic acidthonzylamine
R03AK Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics 13 drugs
beclometasone dipropionatebudesonideepinephrinefluticasone furoatefluticasone propionateformoterolindacaterolisoprenalinemometasone furoatereproterolsalbutamolsalmeterol show all 13 →
R03BC Antiallergic agents, excl. corticosteroids 1 drug
nedocromil
S01GX Other antiallergics 12 drugs
alcaftadineazelastinebilastinecetirizineemedastineepinastineketotifenlevocabastinelodoxamidenedocromilolopatadinespaglumic acid

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

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Asthma indication 195967001 DOID:2841
Giant papillary conjunctivitis indication 231857004 DOID:2457
Vernal keratoconjunctivitis indication 317349009
Vernal conjunctivitis indication 318316003 DOID:2474
Systemic mast cell disease indication 397016004 DOID:349
Asthma management indication 406162001
Allergic conjunctivitis indication 473460002 DOID:11204
Allergic Keratoconjunctivitis indication
Bronchospasm Prevention indication
Vernal Keratitis indication
Inflammatory bowel disease off-label use 24526004 DOID:0050589
Gastrointestinal food allergy off-label use 414314005
Nasal polyp contraindication 52756005
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.32 acidic
pKa2 1.92 acidic

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
G-protein coupled receptor 35 GPCR Ki 5.63 CHEMBL
Taste receptor type 2 member 20 GPCR AGONIST EC50 4.35 IUPHAR
Protein S100-P Cytosolic other SCIENTIFIC LITERATURE
G protein-coupled receptor GPR35 GPCR EC50 6.01 CHEMBL
G-protein coupled receptor 35 GPCR EC50 5.32 CHEMBL

External reference:

IDSource
4018903 VUID
N0000147197 NUI
D00526 KEGG_DRUG
15826-37-6 SECONDARY_CAS_RN
151906 RXNORM
C0086073 UMLSCUI
CHEBI:59773 CHEBI
CHEMBL428880 ChEMBL_ID
CHEMBL74 ChEMBL_ID
DB01003 DRUGBANK_ID
7608 IUPHAR_LIGAND_ID
2882 PUBCHEM_CID
159 MMSL
2410 MMSL
2558 MMSL
4510 MMSL
d00200 MMSL
003422 NDDF
004808 NDDF
21701005 SNOMEDCT_US
372672009 SNOMEDCT_US
387221005 SNOMEDCT_US
D004205 MESH_DESCRIPTOR_UI
2427 INN_ID
4018903 VANDF
4019696 VANDF
Q2WXR1I0PK UNII
Q2WXR1I0PK INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Gastrocrom HUMAN PRESCRIPTION DRUG LABEL 1 0037-0678 LIQUID 20 mg ORAL NDA 19 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0172-6406 SOLUTION 20 mg INTRABRONCHIAL ANDA 22 sections
CROMOLYN SODIUM Human Prescription Drug Label 1 16571-600 SOLUTION, CONCENTRATE 100 mg ORAL ANDA 18 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 17478-291 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 18 sections
CROMOLYN SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 42571-132 SOLUTION, CONCENTRATE 100 mg ORAL ANDA 17 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 42571-350 INHALANT 20 mg INTRABRONCHIAL ANDA 21 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-1202 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 16 sections
NasalCrom HUMAN OTC DRUG LABEL 1 52183-199 SPRAY, METERED 5.20 mg NASAL ANDA 16 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 53002-0140 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 16 sections
Cromolyn Sodium HUMAN OTC DRUG LABEL 1 57782-397 SPRAY, METERED 5.20 mg NASAL ANDA 15 sections
Cromolyn Sodium HUMAN OTC DRUG LABEL 1 59779-075 SPRAY, METERED 5.20 mg NASAL ANDA 14 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 61314-237 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 16 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 68788-8490 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 16 sections
CROMOLYN SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 70556-101 SOLUTION, CONCENTRATE 100 mg ORAL ANDA 18 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 70556-102 SOLUTION 20 mg INTRABRONCHIAL ANDA 22 sections
Cromolyn Sodium HUMAN PRESCRIPTION DRUG LABEL 1 71205-230 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 16 sections
Cromolyn Sodium Oral Solution (Concentrate) HUMAN PRESCRIPTION DRUG LABEL 1 76204-025 SOLUTION, CONCENTRATE 100 mg ORAL ANDA 14 sections
Cromolyn Sodium Inhalation Solution HUMAN PRESCRIPTION DRUG LABEL 1 76204-028 SOLUTION 20 mg RESPIRATORY (INHALATION) ANDA 21 sections
CROMOLYN SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 81665-104 SOLUTION, CONCENTRATE 100 mg ORAL ANDA 18 sections