Compounds > alcaftadine
Page last updated: 2024-11-12

alcaftadine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

alcaftadine : An imidazobenzazepine that is 6,11-dihydro-5H-imidazo[2,1-b][3]benzazepine substituted at position 3 by a formyl group and at position 11 by a 1-methylpiperidin-4-ylidene group. An antihistamine used for treatment of allergic conjunctivitis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID19371515
CHEMBL ID1201747
CHEBI ID71023
SCHEMBL ID1602418
MeSH IDM0557151

Synonyms (61)

Synonym
lastacaft (tn)
147084-10-4
alcaftadine (jan/usan/inn)
D06552
alcaftadine
DB06766
r-89674
r 89674
CHEMBL1201747
chebi:71023 ,
FT-0661472
r89674
lastacaft
alcaftadine [usan:inn]
7z8o94ecsx ,
5h-imidazo(2,1-b)(3)benzazepine-3-carboxaldehyde, 6,11-dihydro-11-(1-methyl-4- piperidinylidene)-
unii-7z8o94ecsx
BCP9000269
S4625
BCP0726000082
AM84429
alcaftadinum
11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5h-imidazo[2,1-b][3]benzazepine-3-carbaldehyde
alcaftadina
alcaftadine [mart.]
alcaftadine [who-dd]
alcaftadine [inn]
alcaftadine [orange book]
4-(1-methyl-piperidin-4-ylidene)-9,10-dihydro-4h-3,10a-diaza-benzo(f)azulene-1-carbaldehyde
alcaftadine [vandf]
alcaftadine [jan]
5h-imidazo(2,1-b)(3)benzazepine-3-carboxaldehyde, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-
alcaftadine [usan]
11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5h-imidazolo[2,1-b][3]benzazepine-3-carbaldehyde
HY-17039
gtpl7587
11-(1-methylpiperidin-4-ylidene)-5,6-dihydroimidazo[2,3-b][3]benzazepine-3-carbaldehyde
SCHEMBL1602418
AC-28019
AKOS025402002
5h-imidazo[2,1-b][3]benzazepine-3-carboxaldehyde,6,11-dihydro-11-(1-methyl-4-piperidinylidene)-
2-(1-methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3,5,10,12-pentaene-6-carbaldehyde
DTXSID80598455
5h-imidazo[2,1-b][3]benzazepine-3-carboxaldehyde, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-
alcaftadine, >=98% (hplc)
11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5h-benzo[d]imidazo[1,2-a]azepine-3-carbaldehyde
BCP04261
Q4712900
2-(1-methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde
1794775-80-6
HMS3885B12
NCGC00390732-04
mfcd09954106
CCG-267551
11-(1-methylpiperidin-4-ylidene)-5,6-dihydroimidazo[2,1-b][3]benzazepine-3-carbaldehyde
AS-56303
2-(1-methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0,3,7]tetradeca-1(10),3,5,11,13-pentaene-6-carbaldehyde
EN300-18738255
alcaftadine (mart.)
s01gx11
11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5h-imidazolo(2,1-b)(3)benzazepine-3-carbaldehyde

Research Excerpts

Overview

Alcaftadine is a safe and effective option for the prevention of ocular itching associated with allergic conjunctivitis, is dosed once daily, and is competitively priced among prescription medications.

ExcerptReferenceRelevance
"Alcaftadine is a safe and effective option for the prevention of ocular itching associated with allergic conjunctivitis, is dosed once daily, and is competitively priced among prescription medications for allergic conjunctivitis. "( Alcaftadine for the prevention of itching associated with allergic conjunctivitis.
Buckley, WA; Hornecker, JR; Mahvan, TD, )		3.02

Actions

ExcerptReferenceRelevance
"Alcaftadine displays therapeutic properties beyond its antihistamine action. "( Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis.
Lane, K; Ono, SJ, 2011)		2.12

Treatment

Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p < 0.0001) No serious adverse events were reported.

ExcerptReferenceRelevance
"Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p < 0.0001)."( Comparison of cytotoxicities and anti-allergic effects of topical ocular dual-action anti-allergic agents.
Fordjuor, G; Kim, SI; Lee, JE; Lee, JH; Lee, JS; Park, CY, 2019)		1.24
"Treatment with alcaftadine 0.25% and olopatadine 0.2% was safe and well tolerated; no serious adverse events were reported."( Ocular itch relief with alcaftadine 0.25% versus olopatadine 0.2% in allergic conjunctivitis: pooled analysis of two multicenter randomized clinical trials.
Ackerman, SL; Ciolino, JB; Hollander, DA; Marsico, NP; McLaurin, EB; Villanueva, L; Williams, JM, 2014)		1.05

Toxicity

ExcerptReferenceRelevance
" Visual acuity, slit lamp biomicroscopy and adverse event reporting were the predetermined safety measures."( The safety and efficacy of alcaftadine 0.25% ophthalmic solution for the prevention of itching associated with allergic conjunctivitis.
Shedden, A; Torkildsen, G, 2011)		0.67
"All three topical ophthalmic medications used in the study are safe and effective in the treatment of allergic conjunctivitis."( Comparative analysis of safety and efficacy of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% in allergic conjunctivitis.
Ayyappanavar, S; Gangasagara, SB; Jayanthi, CR; Kumar, K; Mittal, P; Preethi, B; Rathod, BLS; Sridhar, S, 2021)		0.88

Dosage Studied

ExcerptRelevanceReference
"Alcaftadine is a safe and effective option for the prevention of ocular itching associated with allergic conjunctivitis, is dosed once daily, and is competitively priced among prescription medications for allergic conjunctivitis."( Alcaftadine for the prevention of itching associated with allergic conjunctivitis.
Buckley, WA; Hornecker, JR; Mahvan, TD, )		3.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
H1-receptor antagonistH1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
anti-allergic agentA drug used to treat allergic reactions.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
aldehydeA compound RC(=O)H, in which a carbonyl group is bonded to one hydrogen atom and to one R group.
piperidines
imidazobenzazepineAny organic heterotricyclic compound that consists of an imidazole ring ortho-fused to a benzazepine.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Alcaftadine H1-Antihistamine Action87

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1755501Drug metabolism in human assessed as AUC (0 to infinity) of acid metabolite at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755502Drug metabolism in human assessed as half life of acid metabolite at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755498Protein binding in human plasma incubated for 240 mins by equilibrium dialysis2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755499Drug metabolism in human assessed as Cmax of acid metabolite at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755497Half life in human at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755496AUC (0 to infinity) in human at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755494Cmax in human at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755495Tmax in human at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755500Drug metabolism in human assessed as Tmax of acid metabolite at 0.25%, OU administered once daily for 7 days2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755503Half life in human liver supernatant2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's15 (78.95)24.3611
2020's4 (21.05)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 51.42

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index51.42 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index92.57 (26.88)
Search Engine Supply Index2.36 (0.95)

This Compound (51.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (31.82%)5.53%
Reviews5 (22.73%)6.00%
Case Studies2 (9.09%)4.05%
Observational0 (0.00%)0.25%
Other8 (36.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of the Safety and Effectiveness of Lastacaft® Ophthalmic Solution 0.25% (Alcaftadine) for the Prevention of Itching Associated With Allergic Conjunctivitis: A Postmarketing Surveillance Study in Korea [NCT02555761]3,423 participants (Actual)Observational2015-10-19Completed
To Assess the Impact of Ocular Allergy Treatment on Patients Using an Opthalmic Agent (or no Treatment) Versus Alcaftadine(Lastacaft™) [NCT01808768]Phase 450 participants (Anticipated)Interventional2013-04-30Recruiting
[NCT00889330]Phase 360 participants (Actual)Interventional2009-04-30Completed
[NCT02308501]Phase 425 participants (Actual)Interventional2014-12-31Completed
[NCT01470118]Phase 4127 participants (Actual)Interventional2011-10-31Completed
[NCT01732757]Phase 4157 participants (Actual)Interventional2012-11-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00889330 (13) [back to overview]Conjunctival Redness at Visit 3 (Day 0) at 20 Minutes Following Allergen Challenge, 16 Hours After Treatment Instillation
NCT00889330 (13) [back to overview]Conjunctival Redness at Visit 4 (Day 14) at 20 Minutes Following Allergen Challenge, 15 Minutes Post Treatment Instillation
NCT00889330 (13) [back to overview]Number of Eyes With a Visual Acuity Change From Visit 1 (Day -21) at Day -14
NCT00889330 (13) [back to overview]Number of Eyes With a Visual Acuity Change From Visit 1 (Day -21) at Day 0 Pre-dose, Pre-allergen Challenge
NCT00889330 (13) [back to overview]Number of Eyes With a Visual Acuity Change From Visit 1 (Day -21) at Day 14 Pre-dose, Pre-allergen Challenge
NCT00889330 (13) [back to overview]Ocular Itching at Visit 3 (Day 0) at 7 Minutes Following Allergen Challenge, 16 Hours After Treatment Instillation.
NCT00889330 (13) [back to overview]Ocular Itching at Visit 4 (Day 14) at 7 Minutes Following Allergen Challenge, 15 Minutes Post- Treatment Instillation
NCT00889330 (13) [back to overview]Number of Eyes With a Undilated Fundoscopy Changes From Visit 1 (Day -21) at Day 14
NCT00889330 (13) [back to overview]Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day -14
NCT00889330 (13) [back to overview]Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 0 Post-dose, Pre-allergen Challenge
NCT00889330 (13) [back to overview]Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 0 Pre-dose, Pre-allergen Challenge
NCT00889330 (13) [back to overview]Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 14 Post-dose, Pre-allergen Challenge
NCT00889330 (13) [back to overview]Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 14 Pre-dose, Pre-allergen Challenge
NCT01470118 (8) [back to overview]Eyelid Swelling Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24
NCT01470118 (8) [back to overview]Ocular Itching Evaluated by the Subject at 3, 5, and 7 Minutes Post Challenge on Day 0 at Hour 16
NCT01470118 (8) [back to overview]Ocular Itching Evaluated by the Subject at 3, 5, and 7 Minutes Post Challenge on Day 14 at Hour 24
NCT01470118 (8) [back to overview]Tearing Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24
NCT01470118 (8) [back to overview]Chemosis Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24
NCT01470118 (8) [back to overview]Ciliary Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24
NCT01470118 (8) [back to overview]Conjunctival Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24
NCT01470118 (8) [back to overview]Episcleral Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24
NCT01732757 (11) [back to overview]Ocular Itching Evaluated by the Subject 3 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Chemosis Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Ciliary Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Conjunctival Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Episcleral Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Eyelid Swelling Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Ocular Itching Evaluated by the Subject at 5 and 7 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Percentage of Subject Eyes in Each Category of the Itching Score Distribution Post Challenge on Day 0
NCT01732757 (11) [back to overview]Percentage of Subjects With a Zero Itch Score at 3, 5, and 7 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Percentage of Subjects With Minimal Itching Score at 3, 5, and 7 Minutes Post Challenge on Day 0
NCT01732757 (11) [back to overview]Tearing Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 0
NCT02308501 (4) [back to overview]Conjunctival Inflammation 1 Hour (+30 Minutes) Post CAC on Day 2
NCT02308501 (4) [back to overview]Conjunctival Inflammation at 1 Hour (+30 Minutes) Post CAC on Day 1
NCT02308501 (4) [back to overview]Ocular Itching on Day 1 (15 Minutes Post-study Medication Instillation)
NCT02308501 (4) [back to overview]Ocular Itching on Day 2 (15 Minutes Post-study Medication Instillation)

Conjunctival Redness at Visit 3 (Day 0) at 20 Minutes Following Allergen Challenge, 16 Hours After Treatment Instillation

"A 0 to 4 scale used, allowing for half increment scores to measure redness, where 0 indicates none and 4 indicates extremely red; measurement taken at 20 minutes following allergen challenge, 16 hours post treatment instillation." (NCT00889330)
Timeframe: Visit 3 (Day 0) At 20 minutes following Allergen Challenge, 16 hours post-treatment

Interventionunits on a scale (Mean)
Alcaftadine Ophthalmic Solution1.96
Inactive Vehicle Ophthalmic Solution2.50

[back to top]

Conjunctival Redness at Visit 4 (Day 14) at 20 Minutes Following Allergen Challenge, 15 Minutes Post Treatment Instillation

"A 0 to 4 scale used, allowing for half increment scores to measure redness, where 0 indicates none and 4 indicates extremely red; measurement taken at 20 minutes following allergen challenge, 16 hours post treatment instillation." (NCT00889330)
Timeframe: Visit 4 (Day 14) At 20 minutes following Allergen Challenge

Interventionunits on a scale (Mean)
Alcaftadine Ophthalmic Solution1.57
Inactive Vehicle Ophthalmic Solution2.15

[back to top]

Number of Eyes With a Visual Acuity Change From Visit 1 (Day -21) at Day -14

The number of eyes with any change in visual acuity measurements compared to Day -21. (NCT00889330)
Timeframe: Visit 2 (Day -14) pre-allergen challenge

Interventioneyes (Number)
Alcaftadine Ophthalmic Solution0
Inactive Vehicle Ophthalmic Solution1

[back to top]

Number of Eyes With a Visual Acuity Change From Visit 1 (Day -21) at Day 0 Pre-dose, Pre-allergen Challenge

The number of eyes with any change in visual acuity measurements compared to Day -21 (NCT00889330)
Timeframe: Visit 3 (Day 0) pre-dose, pre-allergen challenge

Interventioneyes (Number)
Alcaftadine Ophthalmic Solution1
Inactive Vehicle Ophthalmic Solution0

[back to top]

Number of Eyes With a Visual Acuity Change From Visit 1 (Day -21) at Day 14 Pre-dose, Pre-allergen Challenge

The number of eyes with any change in visual acuity measurements compared to Day -21 (NCT00889330)
Timeframe: Visit 4 (Day 14) pre-dose, pre-allergen challenge

Interventioneyes (Number)
Alcaftadine Ophthalmic Solution0
Inactive Vehicle Ophthalmic Solution1

[back to top]

Ocular Itching at Visit 3 (Day 0) at 7 Minutes Following Allergen Challenge, 16 Hours After Treatment Instillation.

"A 0 to 4 scale used, allowing for half increment scores, where 0 indicates none and 4 indicates incapacitating itch with an irresistible urge to rub; measurement taken at up to 7 minutes following allergen challenge, 16 hours post treatment instillation." (NCT00889330)
Timeframe: Visit 3 (Day 0) 16 hours post-dose, at up to 7 minutes following Allergen Challenge

Interventionunits on a scale (Mean)
Alcaftadine Ophthalmic Solution0.69
Inactive Vehicle Ophthalmic Solution2.27

[back to top]

Ocular Itching at Visit 4 (Day 14) at 7 Minutes Following Allergen Challenge, 15 Minutes Post- Treatment Instillation

"0 to 4 scale, allowing for half increment scores, where 0 indicates none and 4 indicates incapacitating itch with an irresistible urge to rub" (NCT00889330)
Timeframe: Visit 4 (Day 14) up to 7 minutes following Allergen Challenge

Interventionunits on a scale (Mean)
Alcaftadine Ophthalmic Solution0.42
Inactive Vehicle Ophthalmic Solution1.90

[back to top]

Number of Eyes With a Undilated Fundoscopy Changes From Visit 1 (Day -21) at Day 14

The number of eyes with any change to the following: Vitreous, Retina, Macula, Choroid, Optic Nerve (NCT00889330)
Timeframe: Visit 4 (Day 14) pre-dose, pre-allergen challenge

,
Interventioneyes (Number)
VitreousRetinaMaculaChoroidOptic Nerve
Alcaftadine Ophthalmic Solution00000
Inactive Vehicle Ophthalmic Solution00000

[back to top]

Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day -14

The number of eyes with any change in the following: anterior chamber, conjunctiva, cornea, iris, lens, lids, tear meniscus (NCT00889330)
Timeframe: Visit 2 (Day -14) pre-allergen challenge

,
Interventioneyes (Number)
anterior chamberconjunctivacorneairislenslidstear meniscus
Alcaftadine Ophthalmic Solution0000000
Inactive Vehicle Ophthalmic Solution0000000

[back to top]

Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 0 Post-dose, Pre-allergen Challenge

The number of eyes with any change in the following: anterior chamber, conjunctiva, cornea, iris, lens, lids, tear meniscus (NCT00889330)
Timeframe: Visit 3 (Day 0) post-dose, pre-allergen challenge

,
Interventioneyes (Number)
anterior chamberconjunctivacorneairislenslidstear meniscus
Alcaftadine Ophthalmic Solution0000010
Inactive Vehicle Ophthalmic Solution0000000

[back to top]

Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 0 Pre-dose, Pre-allergen Challenge

The number of eyes with any change in the following: anterior chamber, conjunctiva, cornea, iris, lens, lids, tear meniscus (NCT00889330)
Timeframe: Visit 3 (Day 0) pre-dose, pre-allergen challenge

,
Interventioneyes (Number)
anterior chamberconjunctivacorneairislenslidstear meniscus
Alcaftadine Ophthalmic Solution0000010
Inactive Vehicle Ophthalmic Solution0000000

[back to top]

Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 14 Post-dose, Pre-allergen Challenge

The number of eyes with any change in the following: anterior chamber, conjunctiva, cornea, iris, lens, lids, tear meniscus (NCT00889330)
Timeframe: Visit 4 (Day 14) post-dose, pre-allergen challenge

,
Interventioneyes (Number)
anterior chamberconjunctivacorneairislenslidstear meniscus
Alcaftadine Ophthalmic Solution0000010
Inactive Vehicle Ophthalmic Solution0000000

[back to top]

Number of Eyes With Slit Lamp Biomicroscopy Changes From Visit 1 (Day -21) at Day 14 Pre-dose, Pre-allergen Challenge

The number of eyes with any change in the following: anterior chamber, conjunctiva, cornea, iris, lens, lids, tear meniscus (NCT00889330)
Timeframe: Visit 4 (Day 14) pre-dose, pre-allergen challenge

,
Interventioneyes (Number)
anterior chamberconjunctivacorneairislenslidstear meniscus
Alcaftadine Ophthalmic Solution0000010
Inactive Vehicle Ophthalmic Solution0000000

[back to top]

Eyelid Swelling Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24

Eyelid swelling evaluated by the subject at 7, 15, and 20 minutes post challenge on Day 14 (Visit 4) at hour 24. Subjects scored eyelid swelling on a numeric analog 4-point scale ranging from 0=None to 3=Severe. For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less lid swelling. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
LASTACAFT® (Alcaftadine 0.25%)0.40.50.6
Pataday™ (Olopatadine 0.2%)0.40.60.6
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)1.01.01.1

[back to top]

Ocular Itching Evaluated by the Subject at 3, 5, and 7 Minutes Post Challenge on Day 0 at Hour 16

Ocular itching evaluated by the subject at 3, 5, and 7 minutes post challenge on Day 0 (Visit 3) at hour 16. Subjects scored their ocular itching on a numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments were allowed). For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less itching. (NCT01470118)
Timeframe: Day 0 Hour 16

,,
InterventionScores on a Scale (Mean)
3 Minutes5 Minutes7 Minutes
LASTACAFT® (Alcaftadine 0.25%)0.620.931.07
Pataday™ (Olopatadine 0.2%)1.011.131.12
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.142.352.20

[back to top]

Ocular Itching Evaluated by the Subject at 3, 5, and 7 Minutes Post Challenge on Day 14 at Hour 24

Ocular itching evaluated by the subject at 3, 5, and 7 minutes post challenge on Day 14 (Visit 4) at hour 24. Subjects scored their ocular itching on a numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments were allowed). For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less itching. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
3 Minutes5 Minutes7 Minutes
LASTACAFT® (Alcaftadine 0.25%)0.640.840.93
Pataday™ (Olopatadine 0.2%)0.971.161.01
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.272.191.96

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Tearing Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24

Tearing evaluated by the subject at 7, 15, and 20 minutes post challenge on Day 14 (Visit 4) at hour 24. Subjects scored tearing on a 5-point numeric analog scale ranging from 0=None/Normal to 4=Very Severe. For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less tearing. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
LASTACAFT® (Alcaftadine 0.25%)0.30.50.5
Pataday™ (Olopatadine 0.2%)0.40.60.6
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)1.00.90.8

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Chemosis Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24

Chemosis evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 14 (Visit 4) at hour 24. Investigators scored chemosis on a numeric analog scale ranging from 0=None to 4=Severe (0.5 increments were allowed). For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less chemosis. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
LASTACAFT® (Alcaftadine 0.25%)0.901.031.14
Pataday™ (Olopatadine 0.2%)0.971.091.13
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)1.151.341.42

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Ciliary Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24

Ciliary redness evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 14 (Visit 4) at hour 24. Investigators scored ciliary redness on a numeric analog scale ranging from 0=None to 4=Extremely Severe (0.5 increments were allowed). For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less ciliary redness. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
LASTACAFT® (Alcaftadine 0.25%)1.361.641.67
Pataday™ (Olopatadine 0.2%)1.471.671.65
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)1.832.001.94

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Conjunctival Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24

Conjunctival redness evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 14 (Visit 4) at hour 24. Investigators scored conjunctival redness on a numeric analog scale ranging from 0=None to 4=Extremely Severe (0.5 increments were allowed). For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less conjunctival redness. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
LASTACAFT® (Alcaftadine 0.25%)1.742.011.99
Pataday™ (Olopatadine 0.2%)1.782.011.92
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.082.222.20

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Episcleral Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 14 at Hour 24

Episcleral redness evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 14 (Visit 4) at hour 24. Investigators scored episcleral redness on a numeric analog scale ranging from 0=None to 4=Extremely Severe (0.5 increments were allowed). For each subject, the score for both eyes was averaged (i.e., one score per subject). A lower score was indicative of less episcleral redness. (NCT01470118)
Timeframe: Day 14 Hour 24

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
LASTACAFT® (Alcaftadine 0.25%)1.651.951.91
Pataday™ (Olopatadine 0.2%)1.561.821.79
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.012.152.13

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Ocular Itching Evaluated by the Subject 3 Minutes Post Challenge on Day 0

Ocular itching is evaluated by the subject at 3 minutes post challenge on Day 0 (Visit 3B). Subjects score their ocular itching on a 9-point numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less itching. (NCT01732757)
Timeframe: Day 0 at 3 Minutes Post Challenge

InterventionScores on a Scale (Mean)
Lastacaft®0.40
Pataday™0.76
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.00

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Chemosis Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0

Chemosis is swelling of the tissue that lines the eyelids and surface of the eye. Chemosis is evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 0 (Visit 3B). Investigators score chemosis on a 9-point numeric analog scale ranging from 0=None to 4=Severe (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less chemosis. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
Lastacaft®0.370.620.73
Pataday™0.270.510.56
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)0.510.760.96

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Ciliary Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0

Ciliary redness is redness spreading out around the cornea of the eye. Ciliary redness is evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 0 (Visit 3B). Investigators score ciliary redness on a 9-point numeric analog scale ranging from 0=None to 4=Extremely Severe (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less ciliary redness. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
Lastacaft®1.621.972.06
Pataday™1.471.711.78
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.102.122.13

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Conjunctival Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0

The conjunctiva is a thin membrane that covers the inner surface of the eyelid and the white part of the eye. Conjunctival redness is evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 0 (Visit 3B). Investigators score conjunctival redness on a 9-point numeric analog scale ranging from 0=None to 4=Extremely Severe (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less conjunctival redness. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
Lastacaft®1.732.022.10
Pataday™1.611.811.89
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.172.172.22

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Episcleral Redness Evaluated by the Investigator at 7, 15, and 20 Minutes Post Challenge on Day 0

The episclera is the tissue that lies over the white part of the eye. Episcleral redness is evaluated by the investigator at 7, 15, and 20 minutes post challenge on Day 0 (Visit 3B). Investigators score episcleral redness on a 9-point numeric analog scale ranging from 0=None to 4=Extremely Severe (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less episcleral redness. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
Lastacaft®1.611.881.97
Pataday™1.531.701.78
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.042.042.09

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Eyelid Swelling Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 0

Eyelid swelling is evaluated by the subject at 7, 15, and 20 minutes post challenge on Day 0 (Visit 3B). Subjects score eyelid swelling on a 4-point numeric analog scale ranging from 0=None to 3=Severe. For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less lid swelling. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
Lastacaft®0.20.40.4
Pataday™0.30.50.6
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)0.80.90.7

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Ocular Itching Evaluated by the Subject at 5 and 7 Minutes Post Challenge on Day 0

Ocular itching is evaluated by the subject at 5 and 7 minutes post challenge on Day 0 (Visit 3B). Subjects score their ocular itching on a 9-point numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less itching. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
5 Minutes7 Minutes
Lastacaft®0.610.69
Pataday™0.790.71
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)2.081.89

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Percentage of Subject Eyes in Each Category of the Itching Score Distribution Post Challenge on Day 0

Ocular itching is evaluated by the subject at Hour 16 post challenge on Day 0. Subjects score their ocular itching on a 9-point numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments are allowed). (NCT01732757)
Timeframe: Day 0

,,
InterventionPercentage of Subject Eyes (Number)
00.51.01.52.02.53.03.54.0
Lastacaft®41.732.112.53.55.84.20.30.00.0
Pataday™34.324.020.87.76.75.11.30.00.0
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)8.710.98.06.417.922.815.15.84.5

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Percentage of Subjects With a Zero Itch Score at 3, 5, and 7 Minutes Post Challenge on Day 0

Ocular itching is evaluated by the subject at 3, 5, and 7 minutes post challenge on Day 0 (Visit 3B). Subjects score their ocular itching on a 9-point numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). Zero itch is considered a score = 0. (NCT01732757)
Timeframe: Day 0

,,
InterventionPercentage of Subjects (Number)
3 Minutes5 Minutes7 Minutes
Lastacaft®48.126.926.9
Pataday™26.926.932.7
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)5.83.87.7

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Percentage of Subjects With Minimal Itching Score at 3, 5, and 7 Minutes Post Challenge on Day 0

Ocular itching is evaluated by the subject at 3, 5, and 7 minutes post challenge on Day 0 (Visit 3B). Subjects score their ocular itching on a 9-point numeric analog scale ranging from 0=None to 4=Incapacitating Itch with an Irresistible Urge to Rub (0.5 increments are allowed). For each subject, the score for both eyes is averaged (i.e., one score per subject). Minimal itching is considered a score <1. (NCT01732757)
Timeframe: Day 0

,,
InterventionPercentage of Subjects (Number)
3 Minutes5 Minutes7 Minutes
Lastacaft®84.675.069.2
Pataday™65.453.861.5
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)21.221.225.0

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Tearing Evaluated by the Subject at 7, 15, and 20 Minutes Post Challenge on Day 0

Tearing is evaluated by the subject at 7, 15, and 20 minutes post challenge on Day 0 (Visit 3B). Subjects score tearing on a 5-point numeric analog scale ranging from 0=None/Normal to 4=Very Severe. For each subject, the score for both eyes is averaged (i.e., one score per subject). A lower score is indicative of less tearing. (NCT01732757)
Timeframe: Day 0

,,
InterventionScores on a Scale (Mean)
7 Minutes15 Minutes20 Minutes
Lastacaft®0.20.40.3
Pataday™0.40.50.6
Placebo (Dextran 70 0.1%/Hydroxypropyl Methylcellulose 0.3%)0.90.80.7

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Conjunctival Inflammation 1 Hour (+30 Minutes) Post CAC on Day 2

"Conjunctival Inflammation was assessed by a trained technician post-conjunctival allergen challenge (CAC) on a 0 to 4 scale (0 = best [least inflammation] and 4 = worst [most inflammation]).~The Conjunctival Inflammation was averaged across all Lastacaft-treated eyes to create the average Lastacaft eye Conjunctival Inflammation score, and the Conjunctival Inflammation score was averaged across all Tears Naturale-treated eyes to create the average Tears Naturale eye Conjunctival Inflammation score." (NCT02308501)
Timeframe: 1 hour (+30 minutes) post CAC on Day 2

Interventionunits on a scale (Mean)
Lastacaft®2.44
Tears Naturale ® (Placebo)2.90

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Conjunctival Inflammation at 1 Hour (+30 Minutes) Post CAC on Day 1

"Conjunctival Inflammation was assessed by a trained technician post-conjunctival allergen challenge (CAC) on a 0 to 4 scale (0 = best [least inflammation] and 4 = worst [most inflammation]).~The Conjunctival Inflammation was averaged across all Lastacaft-treated eyes to create the average Lastacaft eye Conjunctival Inflammation score, and the Conjunctival Inflammation score was averaged across all Tears Naturale-treated eyes to create the average Tears Naturale eye Conjunctival Inflammation score." (NCT02308501)
Timeframe: 1 hour (+30 minutes) post CAC on Day 1

Interventionunits on a scale (Mean)
Lastacaft®3.12
Tears Naturale ® (Placebo)3.02

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Ocular Itching on Day 1 (15 Minutes Post-study Medication Instillation)

CAC was performed 15 minutes after study medication instillation. Ocular Itching was assessed by the patient on a 0-4 scale (0 = best [no itching] to 4 = worst [severe itching]). The ocular itching score was averaged across all Lastacaft-treated eyes to create the average Lastacaft eye ocular itching score, and the ocular itching score was averaged across all Tears Naturale-treated eyes to create the average Tears Naturale eye ocular itching score. (NCT02308501)
Timeframe: 15 minutes post-study medication instillation

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
Lastacaft®0.720.880.91
Tears Naturale ® (Placebo)2.192.412.38

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Ocular Itching on Day 2 (15 Minutes Post-study Medication Instillation)

CAC was performed 15 minutes after study medication instillation. Ocular Itching was assessed by the patient on a 0-4 scale (0 = best [no itching] to 4 = worst [severe itching]). The ocular itching score was averaged across all Lastacaft-treated eyes to create the average Lastacaft eye ocular itching score, and the ocular itching score was averaged across all Tears Naturale-treated eyes to create the average Tears Naturale eye ocular itching score. (NCT02308501)
Timeframe: 15 minutes post-study medication instillation

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
Lastacaft®0.841.161.19
Tears Naturale® (Placebo)2.002.222.22

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
pyridoxal
[no description available]		3.3510hydroxymethylpyridine;
methylpyridines;
monohydroxypyridine;
pyridinecarbaldehyde;
vitamin B6		cofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
pyridoxine
4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms).		3.3510hydroxymethylpyridine;
methylpyridines;
monohydroxypyridine;
vitamin B6		cofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
azelastine
azelastine: azeptin is azelastine hydrochloride; structure; eye drop formulation effective in relieving symptoms of allergic conjunctivitis; do not confuse with 5-loxin which is an extract of Boswellia. azelastine : A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.		3.2710monochlorobenzenes;
phthalazines;
tertiary amino compound		anti-allergic agent;
anti-asthmatic drug;
bronchodilator agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
H1-receptor antagonist;
platelet aggregation inhibitor
epinastine
epinastine: RN given refers parent cpd. epinastine : A benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine.		5.0920benzazepine;
guanidines		anti-allergic agent;
H1-receptor antagonist;
histamine antagonist;
ophthalmology drug
gossypol
Gossypol: A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer.		3.3510
ketotifen
Ketotifen: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.. ketotifen : An organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect.		5.0920cyclic ketone;
olefinic compound;
organic heterotricyclic compound;
organosulfur heterocyclic compound;
piperidines;
tertiary amino compound		anti-asthmatic drug;
H1-receptor antagonist
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		2.21106-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
hydroxycitronellal
hydroxycitronellal : The tertiary alcohol arising from addition of water across the C=C double bond of citronellal.		3.3510tertiary alcoholallergen;
fragrance
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.0710azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
thiazoles
[no description available]		2.07101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		2.0710
cromolyn sodium
Cromolyn Sodium: 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.. disodium cromoglycate : An organic sodium salt that is the disodium salt of cromoglycic acid.		3.2710organic sodium saltanti-asthmatic drug;
drug allergen
nedocromil
Nedocromil: A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with ASTHMA, including EOSINOPHILS; NEUTROPHILS; MACROPHAGES; MAST CELLS; MONOCYTES; AND PLATELETS.		3.2710dicarboxylic acid;
organic heterotricyclic compound		anti-allergic agent;
anti-asthmatic drug;
non-steroidal anti-inflammatory drug
levocabastine
levocabastine: for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis		3.2710piperidines
tucaresol
tucaresol: causes a dose-dependent left-shift of the oxygen saturation curve of hemoglobin S by stabilization of its oxy-(R)-conformation; an anti-sickling agent		3.3510
pemirolast
pemirolast: RN from Toxlit; structure given in first source; antiallergic drug		3.2710pyridopyrimidine
cephalosporin c
cephalosporin C: RN given refers to parent cpd; structure in Merck, 9th ed, #1937. cephalosporin C : A cephalosporin antibiotic carrying a 3-acetoxymethyl substituent and a 6-oxo-N(6)-L-lysino group at position 7.		2.0710cephalosporinfungal metabolite
bw 12c79
5-(2-formyl-3-hydroxyphenoxy)pentanoic acid: aromatic aldehyde; aldehyde group interacts with N-terminal amino group of both alpha-globin chains		3.3510
ecopipam
ecopipam: structure given in first source		2.1510benzazepine
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.0710amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
tau 284
bepotastine besilate: an antiallergic agent; structure in first source. bepotastine besylate : An organosulfonate salt obtained by combining equimolar amounts of bepotastine and benzenesulfonic acid. A topical, selective and non-sedating histamine (H1) receptor antagonist used for treatment of itching associated with allergic conjunctivitis.. bepotastine : An ether that is (S)-(4-chlorophenyl)(pyridin-2-yl)methanol in which the hydroxyl hydrogen is substituted by a 1-(3-carboxypropyl)piperidin-4-yl group. A topical, selective and non-sedating histamine (H1) receptor antagonist used (as its benzenesulfonate salt) for treatment of itching associated with allergic conjunctivitis.		4.8732organosulfonate saltanti-allergic agent;
H1-receptor antagonist
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		2.0710
roflumilast
[no description available]		2.0710aromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound		anti-asthmatic drug;
phosphodiesterase IV inhibitor
apogossypol
apogossypol: structure in first source		3.3510
cinnamaldehyde
3-phenylprop-2-enal : A member of the class of cinnamaldehydes that is prop-2-enal in which a hydrogen at position 3 has been replaced by a phenyl group. The configuration of the double bond is not specified; the name "cinnamaldehyde" is widely used to refer to the E (trans) isomer.. (E)-cinnamaldehyde : The E (trans) stereoisomer of cinnamaldehyde, the parent of the class of cinnamaldehydes.		3.35103-phenylprop-2-enal;
cinnamaldehydes		antifungal agent;
EC 4.3.1.24 (phenylalanine ammonia-lyase) inhibitor;
flavouring agent;
hypoglycemic agent;
plant metabolite;
sensitiser;
vasodilator agent
olopatadine hydrochloride
Olopatadine Hydrochloride: An antihistamine with mast-cell stabilizing properties used as eye drops in the treatment of ALLERGIC CONJUNCTIVITIS.		15.36106dibenzooxazepine
demycarosylturimycin h
[no description available]		3.3510
vilazodone hydrochloride
[no description available]		2.0710hydrochlorideantidepressant;
serotonergic agonist;
serotonin uptake inhibitor
linagliptin
Linagliptin: A purine and quinazoline derivative that functions as an INCRETIN and DIPEPTIDYL-PEPTIDASE IV INHIBTOR. It is used as a HYPOGLYCEMIC AGENT in the treatment of TYPE II DIABETES MELLITUS.. linagliptin : A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes.		2.0710aminopiperidine;
quinazolines		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		2.0710
lurasidone hydrochloride
Lurasidone Hydrochloride: A thiazole derivative and atypical ANTIPSYCHOTIC AGENT that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST; SEROTONIN 5-HT2 RECEPTOR ANTAGONIST, serotonin 5-HT7 receptor antagonist, and antagonist of the adrenergic α2A and α2C receptors, as well as a partial SEROTONIN 5-HT1A RECEPTOR AGONIST. It is used in the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER.. lurasidone hydrochloride : A hydrochloride obtained by reaction of lurasidone with one equivalent of hydrochloric acid. An atypical antipsychotic agent used for the treatment of schizophrenia.		2.0710hydrochlorideadrenergic antagonist;
dopaminergic antagonist;
second generation antipsychotic;
serotonergic antagonist
piperidines
Piperidines: A family of hexahydropyridines.		6.1842
tak 491
azilsartan medoxomil: an azilsartan prodrug and angiotensin II type 1 receptor blocker. azilsartan medoxomil : A carboxylic ester obtained by formal condensation of the carboxy group of azilsartan with the hydroxy group of 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one. A prodrug for azilsartan, it is used for treatment of hypertension.		2.07101,2,4-oxadiazole;
aromatic ether;
benzimidazoles;
carboxylic ester;
cyclic carbonate ester;
dioxolane		angiotensin receptor antagonist;
antihypertensive agent;
prodrug
pyrimidinones
Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.		3.2710
ConditionIndicatedRelationship StrengthStudiesTrials
Allergic Conjunctivitis
[description not available]		011.91710
Conjunctivitis, Allergic
Conjunctivitis due to hypersensitivity to various allergens.		113.91710
Active Hyperemia
[description not available]		03.0910
Itching
[description not available]		014.8985
Hyperemia
The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).		03.0910
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		09.8985
Allergic Contact Dermatitis
[description not available]		07.2110
Dermatitis, Allergic Contact
A contact dermatitis due to allergic sensitization to various substances. These substances subsequently produce inflammatory reactions in the skin of those who have acquired hypersensitivity to them as a result of prior exposure.		02.2110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0610