Delving into the Latest Updates on Alcaftadine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Alcaftadine (JAN/USAN/INN)

+ [1]

Target

H1 receptor

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

VISTAKON Pharmaceuticals LLCAllergan Ltd. (Ireland)

Drug Highest PhaseApproved

First Approval Date

US (28 Jul 2010),

Conjunctivitis, AllergicPruritus

Regulation-

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Structure

Molecular FormulaC19H21N3O

InChIKeyMWTBKTRZPHJQLH-UHFFFAOYSA-N

CAS Registry147084-10-4

AbstractCutaneous sympathetic nerve is a crucial part of neuropsychiatric factors contributing to skin immune response, but its role in the psoriasis pathogenesis remains unclear. It is found that cutaneous calcium/calmodulin‐dependent protein kinase II‐γ (CAMK2γ), expressed mainly in sympathetic nerves, is activated by stress and imiquimod in mouse skin. Camk2g‐deficient mice exhibits attenuated imiquimod‐induced psoriasis‐like manifestations and skin inflammation. CaMK2γ regulates dermal γδT‐cell interleukin‐17 production in imiquimod‐treated mice, dependent on norepinephrine production following cutaneous sympathetic nerve activation. Adrenoceptor β1, the primary skin norepinephrine receptor, colocalises with γδT cells. CaMK2γ aggravates psoriasiform inflammation via sympathetic nerve–norepinephrine–γδT cell–adrenoceptor β1–nuclear factor‐κB and –p38 axis activation. Application of alcaftadine, a small‐molecule CaMK2γ inhibitor, relieves imiquimod‐induced psoriasis‐like manifestations in mice. This study reveals the mechanisms of sympathetic‐nervous‐system regulation of γδT‐cell interleukin‐17 secretion, and provides insight into neuropsychiatric factors dictating psoriasis pathogenesis and new potential targets for clinical psoriasis treatment.

01 Sep 2023·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Spectrophotometric platform windows' exploitation for the green determination of Alcaftadine in presence of its oxidative degradation product

Article

Author: Hussein, Ola G. ; Ahmed, Dina A. ; Rezk, Mamdouh R. ; Abdelkawy, Mohamed ; Rostom, Yasmin

This study presents the determination of Alcaftadine (ALF) in its oxidative degradation product presence by applying comprehensive study comparative of four different green stability indicating spectrophotometric approaches through successful exploitation of different spectrophotometric platform windows. Window I; based on absorption spectrum zero order data manipulation using the newly developed extended absorbance difference (EAD). Window II; based on derivative spectra by second order derivative (D²) data manipulation. Window III; based on ratio spectra applying constant multiplication (CM) and absorptivity centering via factorized ratio difference spectrum (ACT-FSR_ΔP) methods data manipulation. Finally, window IV; based on derivative of ratio spectrum by virtue of first derivative of ratio spectral (DD¹) method data manipulation. Calibration curves construction were over linearity range; 1.0-14.0 µg/mL for ALF. The proposed methods accuracy, precision, and linearity range were determined and validated as per ICH guidelines. Moreover, they were able to analyze ALF in raw form, dosage form and in existence of its oxidative degradation product. Statistical comparisons were done between the proposed methods and the reported one showing no significant difference concerning accuracy and precision. Furthermore, greenness profile assessment was accomplished by means of four metric tools; namely: analytical greenness (AGREE), green analytical procedure index (GAPI), analytical eco-scale, and national environmental method index (NEMI).

01 Jan 2023·Indian Journal of Ophthalmology

Practice patterns and opinions in the treatment of allergic eye disease: A survey among Indian ophthalmologists

Article

Author: Das, Sujata ; Priyadarshini, Smruti Rekha

Purpose:Management of allergic eye disease is seldom straightforward and often challenging. We conducted an online survey to elicit opinions on the preferred practice pattern in the treatment of allergic eye disease.Methods:An online survey questionnaire was sent to all practicing ophthalmologists using social media platforms. The respondents were asked about their clinical experience and preferred treatment in various scenarios such as mild-moderate vernal keratoconjunctivitis (VKC), chronic VKC, refractory VKC, steroid responders, giant papillae, and shield ulcer. Respondents were asked about the newer molecule (alcaftadine) and reservations regarding systemic immuno-suppressants and ordering allergy tests in their practice.Results:Ninety - one participants responded to the survey. About 57.1% of ophthalmologists reported coming across more than 10 cases per week in their practice. The most common age group was 5–10 years (61.1%), but adult onset VKC was also reported at 41.6% (1–2 per month), 37.1% (3–5 per month), and 13.5% (more than 10 per month). The disease is perennially present (36.7%), and a mixed form has been reported by 47.8% of ophthalmologists. Dual-acting agents were preferred by 40% in mild-moderate clinical variants. Topical steroids in slow tapering dosage were preferred by 86.7% in their prescription. Tacrolimus 0.03% was preferred by 65.9% and given for at least 3 months of continuous usage by 47.6% of ophthalmologists. High-dose topical steroids were preferred for giant papillae (67.8%) and Shields ulcers (68.3%) in our survey. Supratarsal steroid injection was preferred by 50% in treating refractory VKC in our survey.Conclusion:Allergic eye disease is a common yet annoying disease. The signs and symptoms can vary from subtle, innocuous forms to devastating variants affecting vision and day-to-day work. This survey aims to elicit responses from clinicians spreading across different geographical areas and compares responses based on experience in practice.

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	US	AbbVie, Inc.	28 Jul 2010
Pruritus	US	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 1	JP	Allergan Ltd. (Ireland)	01 Mar 2014
Seasonal allergic conjunctivitis	Phase 1	US	VISTAKON Pharmaceuticals LLC	01 Aug 2006
Acute conjunctivitis	Phase 1	US	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


ARVO2016	Not Applicable	Anaphylaxis	111	Lastacaft	(aufdaebzly) = cwhtwyfqed ynqxureumf (cukniqcpsn )	-	01 May 2016
				Pataday	(aufdaebzly) = nupcfdehac ynqxureumf (cukniqcpsn )
NCT02161146 (CTgov)	Phase 3	Conjunctivitis, Allergic	240	AGN-229666 (AGN-229666)	qlfecconym(olusiuqcbo) = ieljjwjwvi hhvgoxvdrq (wyjxmahivj, fwunmvyjrc - lyvncqenet) View more	-	07 Mar 2016
				Vehicle to AGN-229666 (Vehicle)	qlfecconym(olusiuqcbo) = kbejkhhshr hhvgoxvdrq (wyjxmahivj, wkmqyfijpv - rzvhrzsgmn) View more
NCT02082262 (CTgov)	Phase 3	Perennial allergic conjunctivitis	140	AGN-229666	benfqppgnf(nhuiueldgl) = sozqoknafi mnlxcqtbci (vcyqszramh, mxkgfsbmea - skfdsdrebq) View more	-	08 Oct 2015
NCT01470118 \| NCT01732757 (Pubmed \| Adv Ther)	Phase 4	Conjunctivitis, Allergic	284	Alcaftadine 0.25%	(vowvctuulz) = msfervttjj yskkorkmpn (usoxwwuole )	Positive	01 Oct 2014
				Olopatadine 0.2%	(vowvctuulz) = kcsxvuxbtm yskkorkmpn (usoxwwuole )
NCT01754766 (CTgov)	Phase 2	Conjunctivitis, Allergic	90	AGN-229666 (AGN-229666 Dose A)	ptqjshbbsa(wrikcruqfm) = elvitzpcya wrwzqckgqx (voezoctjmn, wpolgfmsuo - bujlljiijg) View more	-	04 Feb 2014
				AGN-229666 (AGN-229666 Dose B)	ptqjshbbsa(wrikcruqfm) = ycwqxihgcc wrwzqckgqx (voezoctjmn, wqxravaagb - ilfubpodyj) View more
NCT01732757 (CTgov)	Phase 4	Acute conjunctivitis \| Conjunctivitis, Allergic	157	Alcaftadine 0.25% (Lastacaft®)	nnjbuzcalg(swcnfwdily) = iinfdothdi gxnmewuuze (zfwpjskiwd, dewywojvem - zyibivzexh) View more	-	14 Jan 2014
				Olopatadine 0.2% (Pataday™)	nnjbuzcalg(swcnfwdily) = zvcezzddxi gxnmewuuze (zfwpjskiwd, jctowkmehd - lwrketetqv) View more
NCT01470118 (CTgov)	Phase 4	Acute conjunctivitis \| Conjunctivitis, Allergic	127	alcaftadine 0.25% ophthalmic solution (LASTACAFT® (Alcaftadine 0.25%))	pnrvmkffdn(vmlghjyupd) = cxjrccizsr tqsubmhxum (szquudlyzf, ibekngviyj - ucgdkzossb) View more	-	21 Feb 2013
				olopatadine 0.2% ophthalmic solution (Pataday™ (Olopatadine 0.2%))	pnrvmkffdn(vmlghjyupd) = wmhwgdyywg tqsubmhxum (szquudlyzf, jomzjjrvai - gmevfjdgaf) View more
AAAAI2013	Not Applicable	-	-	Olopatadine	vvhnzgwxqq(peffujrbku) = tznnhpxent pknztxxocv (qqyqfpzgtw )	-	01 Feb 2013
				Alcaftadine	vvhnzgwxqq(peffujrbku) = beabwypynb pknztxxocv (qqyqfpzgtw )
NCT00889330 (ARVO2011)	Phase 3	Pruritus	-	Alcaftadine 0.25% ophthalmic solution	(smhmysbkng) = Alcaftadine significantly reduced conjunctival redness, and almost all other allergic signs and symptoms at both 15 minutes and 16 hours after drug administration seintijxzx (ikfxoyggeh ) View more	Positive	01 Apr 2011
				Vehicle