alcaftadine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	4165	147084-10-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: R 89674 alcaftadine lastacaft	Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated. Molecular weight: 307.40 Formula: C19H21N3O CLOGP: 2.45 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 38.13 ALOGS: -2.97 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

R 89674
alcaftadine
lastacaft

Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

Molecular weight: 307.40
Formula: C19H21N3O
CLOGP: 2.45
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 38.13
ALOGS: -2.97
ROTB: 1

Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
July 28, 2010	FDA	ALLERGAN

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Ocular hyperaemia	424.21	70.52	83	425	25061	63463453
Eye irritation	218.07	70.52	47	461	21924	63466590
Scleral hyperaemia	125.19	70.52	16	492	283	63488231
Eye pruritus	108.96	70.52	26	482	18645	63469869
Eyelid oedema	89.97	70.52	20	488	10459	63478055
Eye swelling	87.86	70.52	23	485	23895	63464619
Erythema of eyelid	85.88	70.52	15	493	2271	63486243
Eye pain	75.48	70.52	22	486	33832	63454682
Eye discharge	71.28	70.52	15	493	6048	63482466

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Ocular hyperaemia	343.00	95.08	66	348	28140	79715834
Eye irritation	198.91	95.08	40	374	20641	79723333
Scleral hyperaemia	131.38	95.08	16	398	298	79743676

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	S01GX11	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:50857	anti-allergic drugs

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

Disease	Relation	SNOMED_ID	DOID
Allergic conjunctivitis	indication	473460002	DOID:11204

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.27	Basic
pKa2	2.99	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.25%	LASTACAFT	ABBVIE	N022134	July 28, 2010	OTC	SOLUTION/DROPS	OPHTHALMIC	10617695	March 19, 2027	USE OF LASTACAFT TO TEMPORARY RELIEVE ITCHY EYES DUE TO POLLEN, RAGWEED, GRASS, ANIMAL HAIR AND DANDER
0.25%	LASTACAFT	ABBVIE	N022134	July 28, 2010	OTC	SOLUTION/DROPS	OPHTHALMIC	8664215	Dec. 23, 2027	USE OF LASTACAFT TO TEMPORARY RELIEVE ITCHY EYES DUE TO POLLEN, RAGWEED, GRASS, ANIMAL HAIR AND DANDER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST				CHEMBL	CHEMBL

External reference:

ID	Source
4030132	VUID
N0000181719	NUI
D06552	KEGG_DRUG
4030132	VANDF
C2348241	UMLSCUI
CHEBI:71023	CHEBI
CHEMBL1201747	ChEMBL_ID
DB06766	DRUGBANK_ID
C557708	MESH_SUPPLEMENTAL_RECORD_UI
7587	IUPHAR_LIGAND_ID
8707	INN_ID
7Z8O94ECSX	UNII
19371515	PUBCHEM_CID
1000082	RXNORM
175605	MMSL
27322	MMSL
013612	NDDF
447208001	SNOMEDCT_US
447209009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
LASTACAFT	HUMAN PRESCRIPTION DRUG LABEL	1	0023-4290	SOLUTION/ DROPS	2.50 mg	OPHTHALMIC	NDA	24 sections
LASTACAFT	HUMAN OTC DRUG LABEL	1	0023-4291	SOLUTION/ DROPS	2.50 mg	OPHTHALMIC	NDA	12 sections
LASTACAFT	HUMAN OTC DRUG LABEL	1	0023-4291	SOLUTION/ DROPS	2.50 mg	OPHTHALMIC	NDA	12 sections
LASTACAFT	HUMAN PRESCRIPTION DRUG LABEL	1	42254-288	SOLUTION/ DROPS	2.50 mg	OPHTHALMIC	NDA	23 sections
LASTACAFT	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6294	SOLUTION/ DROPS	2.50 mg	OPHTHALMIC	NDA	23 sections
Alcaftadine	Human OTC Drug Label	1	58602-605	SOLUTION/ DROPS	2.50 mg	OPHTHALMIC	ANDA	13 sections