Delving into the Latest Updates on Alcaftadine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Alcaftadine (JAN/USAN/INN), AGN 229666, R-89674

+ [1]

Target

H1 receptor

Action

antagonists

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesEye DiseasesSkin and Musculoskeletal Diseases

Active Indication

Conjunctivitis, AllergicPruritus

Inactive Indication

Acute conjunctivitisPerennial allergic conjunctivitisSeasonal allergic conjunctivitis

Originator Organization

Vistakon Pharmaceuticals LLC

Active Organization

AbbVie, Inc.

Inactive Organization

Allergan UCVistakon Pharmaceuticals LLC

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (28 Jul 2010),

Conjunctivitis, AllergicPruritus

Regulation-

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Structure/Sequence

Molecular FormulaC19H21N3O

InChIKeyMWTBKTRZPHJQLH-UHFFFAOYSA-N

CAS Registry147084-10-4

The pharmaceutical industry has recently introduced a new combination of eye drop containing alcaftadine (ALF) and ketorolac tromethamine (KTC) utilized in managing allergic conjunctivitis. This new formulation elevates the necessity for developing sensitive, reliable, rapid and simple spectrophotometric methods to accurately quantify ALF and KTC in their dosage form with full consideration of its preservative benzalkonium chloride. In this study, three simple green spectrophotometric methods were developed to simultaneously determine ALF, KTC, and benzalkonium chloride in their ternary combinations without requiring preliminary separation steps. The expected methods employed unique spectral properties of the mixture including the extension of KTC's spectrum beyond that of ALF. The suggested methods were direct spectrophotometric, absorbance resolution, and factorized zero‐order methods. The proposed methods were assessed for validity in accordance with ICH guidelines and were determined to be linear within concentration ranges of 1.0–14.0 µg/mL for ALF and 3.0–30.0 µg/mL for KTC. A statistical comparison between the developed methods versus the reported and official methods revealed lack of any difference in terms of accuracy and precision. The work was also considered a successful attempt to stick to Green Analytical Chemistry principles and preserve our environment via using water as the main solvent. This was reflected by the highest greenness score of the proposed methods upon adopting state‐of‐the art assessment metric tools including Complementary Green Analytical Procedure Index (ComplexGAPI) and analytical GREEnness (AGREE). Considering these benefits, our developed methods were demonstrated to be green, sensitive, and accurate making it suitable for routine drug analysis.

01 Oct 2025·CONTACT DERMATITIS

Not Just Pink Eye: Allergic Contact Dermatitis to Alcaftadine 0.25% Ophthalmic Solution

Article

Author: Mayra Betancourt Ponce ; Margo Reeder

01 May 2025·Small

Poly‐Phosphamide Catalyzed Visible‐Light‐Driven CH₄ and Dark‐Phase‐Mediated Cyclic Carbonate Productions Utilizing CO₂

Article

Author: Halder, Sandipan ; Chakraborty, Biswarup ; Kumari, Nidhi ; Das, Koushik ; Chaudhary, Monika

Abstract:

A poly‐phosphamide (POP) with a band gap of 2.8 eV is used for the photochemical conversion of CO2 into CH4 and chemical conversion of CO2 and organo‐epoxides into cyclic carbonates. The Tauc plot and Mott Schottky analyses indicate the conduction band potential at −1.49 V (vs NHE), much more negative than the multi‐electron CO2 reduction potential and the lifetime of the photo‐excited electron is found 2.8 ns. On photoirradiation of 420 nm light, the POP in the presence of triethanolamine or ascorbic acid can selectively convert CO2 into CH4 (≈99%) with a yield of 4.6 mmol g−1. On visible‐light irradiation, the drop of charge‐transfer resistance (Rct) and an enhancement of cathodic current further confirm the photon‐harvesting efficiency of the POP. In situ, FTIR study identifies the CO2 adsorption to the POP and possible reaction intermediate, like *‐CO, *‐CH2OH. POP also behaves as a catalyst for CO2 conversion to cyclic carbonates under solvent‐free conditions with more than 98% yield. After the light‐phase and dark‐phase reactions, POP can be successfully recycled at least five times without structural degradation. Herein, the POP acts as a bi‐functional, and recyclable polymeric organic material to convert CO2 to essential feedstocks under mild reaction conditions.

1

News (Medical) associated with Alcaftadine

09 Jan 2024

·synapse.patsnap.com

Deciphering H1 receptor antagonists and Keeping Up with Their Recent Developments

The H1 receptor, also known as the histamine H1 receptor, plays a crucial role in the human body. It is primarily found in smooth muscle cells, endothelial cells, and nerve cells. Activation of the H1 receptor by histamine leads to various physiological responses, including vasodilation, increased vascular permeability, bronchoconstriction, and stimulation of sensory nerve endings. These responses are involved in allergic reactions, inflammation, and immune responses. Antagonists of the H1 receptor, commonly known as antihistamines, are widely used to treat allergies, hay fever, and other conditions associated with excessive histamine release. Understanding the role of the H1 receptor is essential for developing effective treatments for allergic and inflammatory disorders. The analysis of the target H1 receptor reveals a competitive landscape with multiple companies actively developing drugs. GSK Plc, Sanofi, Pfizer Inc., Bayer AG, and Novartis AG are among the companies with the highest number of approved drugs or drugs in advanced stages of development. The indications with the most approved drugs include Common Cold, Rhinitis, Allergic, Urticaria, Pruritus, and Hypersensitivity. Small molecule drugs are the most rapidly progressing drug type, indicating intense competition in this area. China, the United States, and Japan are the countries with the highest number of approved drugs, with China showing significant progress in the development of drugs targeting the H1 receptor. Overall, the target H1 receptor presents opportunities for further research and development, particularly in indications with high unmet medical needs. How do they work?H1 receptor antagonists, also known as H1 blockers or antihistamines, are a class of drugs that block the action of histamine at the H1 receptor. Histamine is a chemical released by the body during an allergic reaction, causing symptoms such as itching, sneezing, runny nose, and watery eyes. H1 receptor antagonists work by binding to the H1 receptors on cells, preventing histamine from binding and exerting its effects. From a biomedical perspective, H1 receptor antagonists are commonly used to treat allergic conditions, such as hay fever (allergic rhinitis), hives (urticaria), and allergic conjunctivitis. They help alleviate symptoms by reducing the effects of histamine, thereby relieving itching, sneezing, and other allergic reactions. There are different generations of H1 receptor antagonists, each with varying degrees of sedative effects. First-generation antihistamines, such as diphenhydramine and chlorpheniramine, can cause drowsiness and are often used for their sedative properties in addition to their antihistamine effects. Second-generation antihistamines, such as cetirizine, loratadine, and fexofenadine, are less likely to cause sedation and are preferred for daytime use. In summary, H1 receptor antagonists are drugs that block the action of histamine at the H1 receptor, providing relief from allergic symptoms. They are commonly used in the treatment of various allergic conditions and come in different generations with varying sedative effects. List of H1 receptor AntagonistsThe currently marketed H1 receptor antagonists include: Olopatadine Hydrochloride/Mometasone Furoate MonohydrateChlorpheniramine Maleate/Codeine PhosphateDiphenhydramine Hydrochloride/Naproxen SodiumRecombinant interferon alfa-2b/LoratadineRupatadine FumarateAzelastine/mometasoneEbastine/Pseudoephedrine HydrochlorideAzelastine Hydrochloride/Fluticasone PropionateChlorpheniramine Maleate/Hydrocodone Bitartrate/Pseudoephedrine HydrochlorideAlcaftadineFor more information, please click on the image below. What are H1 receptor antagonists used for?H1 receptor antagonists are widely used to treat allergies, hay fever, and other conditions associated with excessive histamine release. For more information, please click on the image below to log in and search. How to obtain the latest development progress of H1 receptor antagonists?In the Synapse database, you can keep abreast of the latest research and development advances of H1 receptor antagonists anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 Deals associated with Alcaftadine

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External Link

KEGG	Wiki	ATC	Drug Bank
D06552	Alcaftadine	S01GX11	DB06766

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Conjunctivitis, Allergic	United States	AbbVie, Inc.	28 Jul 2010
Pruritus	United States	AbbVie, Inc.	28 Jul 2010

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Perennial allergic conjunctivitis	Phase 3	Japan	Allergan UC	01 Mar 2014
Seasonal allergic conjunctivitis	Phase 3	United States	Vistakon Pharmaceuticals LLC	01 Aug 2006
Acute conjunctivitis	Phase 3	United States	Vistakon Pharmaceuticals LLC	01 Oct 2005

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02308501 (CTgov)	Phase 4	Conjunctivitis, Allergic	25	Lastacaft (Lastacaft®)	ehyfgtmwsc(eijggsjzob) = qpjletdblf vgnouuuhsf (iibiopcjdt, 0.79) View more	-	18 Mar 2021
				Placebo (Tears Naturale ® (Placebo))	ehyfgtmwsc(eijggsjzob) = rcljirysjx vgnouuuhsf (iibiopcjdt, 0.80) View more
NCT02161146 (CTgov)	Phase 3	Conjunctivitis, Allergic	240	AGN-229666 (AGN-229666)	xwtfmdjdgp(fidohetsrw) = wclijktlzv bwqqvxbhdr (ejjlrcelmp, 0.523) View more	-	07 Mar 2016
				Vehicle to AGN-229666 (Vehicle)	xwtfmdjdgp(fidohetsrw) = yugzvpmtlt bwqqvxbhdr (ejjlrcelmp, 0.904) View more
NCT02082262 (CTgov)	Phase 3	Perennial allergic conjunctivitis	140	AGN-229666	kzhwovjbmg(juclgdzier) = imftjezwsg wjhgsctnzb (hgzzunqehr, 0.49) View more	-	08 Oct 2015
NCT01470118 \| NCT01732757 (Pubmed \| Adv Ther)	Phase 4	Conjunctivitis, Allergic	284	Alcaftadine 0.25%	pyfgkpnfmj(yebzfakptr) = iuaiogoekq izyaibljjn (wqrzrsmvtk )	Positive	01 Oct 2014
				Olopatadine 0.2%	pyfgkpnfmj(yebzfakptr) = rhxfmyitli izyaibljjn (wqrzrsmvtk )
NCT01754766 (CTgov)	Phase 2	Conjunctivitis, Allergic	90	AGN-229666 (AGN-229666 Dose A)	dcpvvbldao(jvsgmuoveu) = qhdztazjhd bwizyjlbeo (fqmnbkcmow, 0.5123) View more	-	04 Feb 2014
				AGN-229666 (AGN-229666 Dose B)	dcpvvbldao(jvsgmuoveu) = grjzdylgor bwizyjlbeo (fqmnbkcmow, 0.3947) View more
NCT01732757 (CTgov)	Phase 4	Acute conjunctivitis \| Conjunctivitis, Allergic	157	Alcaftadine 0.25% (Lastacaft®)	cgozzauajp(mflgltndzp) = ogxzjshqne flcdrowkxh (hsqbmnhazn, 0.582) View more	-	14 Jan 2014
				Olopatadine 0.2% (Pataday™)	cgozzauajp(mflgltndzp) = annjvdfqyq flcdrowkxh (hsqbmnhazn, 0.752) View more
NCT01470118 (CTgov)	Phase 4	Acute conjunctivitis \| Conjunctivitis, Allergic	127	alcaftadine 0.25% ophthalmic solution (LASTACAFT® (Alcaftadine 0.25%))	mgadvtnkkk(nggmhmsqyq) = lrpcmrzrqa euzzvhbpft (aikshiorsb, 0.716) View more	-	21 Feb 2013
				olopatadine 0.2% ophthalmic solution (Pataday™ (Olopatadine 0.2%))	mgadvtnkkk(nggmhmsqyq) = kxradmqhfk euzzvhbpft (aikshiorsb, 0.8211) View more
NCT00889330 (ARVO2011)	Phase 3	Pruritus	-	Alcaftadine 0.25% ophthalmic solution	eakbkodthz(pgtpzydunp) = Alcaftadine significantly reduced conjunctival redness, and almost all other allergic signs and symptoms at both 15 minutes and 16 hours after drug administration yhinetennm (ekfzdusulg ) View more	Positive	01 Apr 2011
				Vehicle