Delving into the Latest Updates on Cyclosporine (Huons) with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Ciclosporin (Huons), Clacier, HE 10

+ [2]

Target

CaN

Mechanism

CaN inhibitors(Calcineurin inhibitors)

Therapeutic Areas

Eye Diseases

Active Indication

Xerophthalmia

Inactive Indication-

Originator Organization

Huons Co., Ltd.

Active Organization

Huons Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

KR (26 Nov 2018),

Xerophthalmia

Regulation-

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Structure

Molecular FormulaC62H111N11O12

InChIKeyPMATZTZNYRCHOR-CGLBZJNRSA-N

CAS Registry59865-13-3

Five polypeptides with a potential umami taste were isolated and purified from Yanjin black bone chicken. However, the flavor characteristics and umami mechanism have not been clarified. The umami properties of these five peptides were investigated in this work using a range of analytical techniques, computer simulation, and sensory evaluation. HE-10 and TP-7 exhibited the strongest umami flavors. Furthermore, dose-response experiments showed that the umami peptides enhanced umami by generating peptide mineral chelates. Environmental scanning electron microscopy (ESEM) microstructural analyses supported this finding. The molecular docking results indicated that the five polypeptides bind to four critical amino acid residues, namely Glu217, Glu148, Asp216, and His145, of the T1R1/T1R3 receptor. The binding occurred through van der Waals, electrostatic interactions, hydrogen bonding, and hydrophobic interactions. The main surface forces implicated include aromatic interactions, hydrogen bonding, hydrophilicity, and solvent accessibility.

18 Nov 2024·BRITISH JOURNAL OF DERMATOLOGY

A prospective observational cohort study comparing the treatment effectiveness and safety of ciclosporin, dupilumab and methotrexate in adult and paediatric patients with atopic dermatitis: results from the UK–Irish A-STAR register

Article

Author: Baden, Manisha ; Cameron, Shona ; Coker, Bola ; Gribaleva, Elizaveta ; Wainman, Hannah ; Beattie, Paula ; Darné, Sharmela ; Brown, Sara ; Ferguson, Leila ; Burton, Tim ; Irvine, Alan D ; Man, Irene ; Warren, Richard B ; Warren, Richard B ; Wan, Mandy ; Topliffe, Joanne ; Layton, Alison ; Wernham, Aaron ; Fadhil, May ; Thompson, Ben ; Hearn, Ross ; Alexander, Helen ; Ingram, John R ; Flohr, Carsten ; Ardern-Jones, Michael R ; Prieto-Merino, David ; Sergeant, Ann ; Malek, Rayka ; Ladoyanni, Effi ; Lambert, Alice ; Reynolds, Nick ; Woolf, Richard ; Patel, Prakash ; Popli, Urvi ; Cork, Michael J ; Newell, Louise ; Fahy, Caoimhe ; Leitch, Claire ; Lunt, Mark ; Yiu, Zenas Z N ; Wahie, Shyamal ; Johnston, Graham A ; Brown, Victoria ; Llewellyn, Joanne ; Ogg, Graham

Abstract:

Background:

The main conventional systemic treatments for atopic dermatitis (AD) are methotrexate (MTX) and ciclosporin (CyA). Dupilumab was the first novel systemic agent to enter routine clinical practice. There are no head-to-head randomized controlled trials or real-world studies comparing these agents directly. Network meta-analyses provide indirect comparative efficacy and safety data and have shown strong evidence for dupilumab and CyA.

Objectives:

To compare the real-world clinical effectiveness and safety of CyA, dupilumab and MTX in AD.

Methods:

We compared the effectiveness and safety of these systemic agents in a prospective observational cohort study of adult and paediatric patients recruited into the UK–Irish Atopic eczema Systemic TherApy Register (A-STAR). Treatment effectiveness measures included Eczema Area and Severity Index (EASI), Patient-Oriented Eczema Measure (POEM), Peak Pruritus Numerical Rating Scale (PP-NRS), Dermatology Life Quality Index (DLQI) and children’s DLQI (cDLQI). The minimum duration of treatment was 28 days and follow-up was 12 months. Adjusted Cox-regression analysis was used to compare the hazard ratios of achieving EASI-50, EASI-75 and EASI-90 over time, and linear mixed-effects models were used to estimate changes in efficacy scores. Treatment safety was assessed by examining adverse events (AEs) at follow-up visits.

Results:

We included 488 patients (311 adults and 177 children/adolescents) on dupilumab (n = 282), MTX (n = 149) or CyA (n = 57). CyA and MTX were primarily used as the first-line treatment, while dupilumab was mainly a second-line systemic treatment as per UK National Institute of Clinical and Care Excellence (NICE) recommendations. EASI-50, EASI-75 and EASI-90 were achieved more rapidly in the dupilumab and CyA groups compared with MTX. After adjustment for previous severity, the reduction in EASI, POEM, PP-NRS and DLQI was greater for patients treated with dupilumab compared with MTX. In patients with severe disease the reduction in EASI, POEM and PP-NRS was even greater with CyA. The incidence rates of AEs were similar across groups (734, 654 and 594 per 10 000 person-month on CyA, dupilumab and MTX, respectively).

Conclusions:

This real-world comparison of CyA, dupilumab and MTX in AD suggests that dupilumab is consistently more effective than MTX and that CyA is most effective in very severe disease within 1 year of follow-up.

01 Oct 2024·GRAEFES ARCHIVE FOR CLINICAL AND EXPERIMENTAL OPHTHALMOLOGY

Real-world insights and outcomes related to ciclosporin A 0.1% cationic emulsion for the long-term treatment of dry eye disease in Germany: Country-level sub-analysis of the PERSPECTIVE study

Article

Author: Deuter, Christoph M E ; Geerling, Gerd ; Lorenz, Katrin ; Lanzl, Ines

Abstract:

Purpose:

The PERSPECTIVE study was a real-world European, non-interventional, multicenter, observational study that evaluated the effectiveness, tolerability, and safety of ciclosporin A (CsA) 0.1% cationic emulsion (CE) in routine clinical practice as a treatment for adults with severe keratitis and dry eye disease (DED) that remained insufficiently controlled with artificial tears. This sub-analysis examined data from ophthalmology clinics in Germany to provide more precise insights into treatment patterns, outcomes, and clinical decision-making related to CsA 0.1% CE.

Methods:

Study data were collected from adults starting CsA 0.1% CE (one drop in both eyes at bedtime) and followed up at Week 4, 12, and 24, and Month 12. The primary endpoint was mean change from baseline in corneal fluorescein staining (CFS) score (Oxford Grade Scale) at Month 12. Secondary endpoints examined the severity of ocular signs and symptoms, and adverse events (AEs).

Results:

A total of 236 patients from 20 ophthalmology clinics in Germany participated in the PERSPECTIVE study (69.9% female; mean age 60.8 years). Following treatment with CsA 0.1% CE, patients experienced significant reductions in CFS score from Week 4, which were maintained through to Month 12 (P < 0.0001). From baseline, 81.6% of patients experienced an improvement in CFS score at Month 12. CsA 0.1% CE provided significant reductions in the severity of eyelid and conjunctival erythema at Month 12 compared with baseline (P < 0.001), as well as significant reductions in the severity of subjective ocular symptoms (all P ≤ 0.015). Safety data were consistent with the known safety profile of CsA 0.1% CE. Tolerability was rated as “satisfactory,” “good,” or “very good” by 97.2% of physicians and 95.7% of patients.

Conclusion:

Outcomes in Germany were similar to those reported for the overall European study population and are indicative of the treatment results that ophthalmologists may expect to see with CsA 0.1% CE treatment in real-life clinical practice. Treatment with CsA 0.1% CE provided long-term improvements over 12 months and was generally well tolerated.

100 Deals associated with Cyclosporine (Huons)

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Xerophthalmia	KR	Huons Co., Ltd.	26 Nov 2018

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Dry Eye Syndromes	Phase 3	-	Huons Co., Ltd.	01 May 2013

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01252667 (CTgov)	-	Acute Myeloid Leukemia	44	Peripheral Blood Stem Cell Transplantation+Clofarabine+Cyclosporine+Mycophenolate Mofetil (Part 1 - Dose 1 (30 mg/m^2 Clofarabine))	vfnukzzqix(vrbamywbvl) = bxqokrzqqh yudxykddzm (abbpqadpnv, pynjwxpxqa - ebaejknvlj) View more	-	16 Apr 2020
				Peripheral Blood Stem Cell Transplantation+Clofarabine+Cyclosporine+Mycophenolate Mofetil (Part 1 - Dose 2 (40 mg/m^2 Clofarabine))	vfnukzzqix(vrbamywbvl) = xqwnieelig yudxykddzm (abbpqadpnv, ecjaylzjst - bxmkxepkiz) View more
NCT00987480 (CTgov)	Phase 2	Leukemia \| Myelodysplastic Syndromes \| Fanconi Anemia	45	CliniMACS device+fludarabine+Busulfan+cyclosporine.+cyclophosphamide	utdzmknuzz(iuteuqaxyh) = ghmkuzbjgw dssbxdzhww (fqfehjaqhq, mpxpeyhgkg - aikwwywevq) View more	-	10 Jul 2018
NCT00974142 (CTgov)	Phase 1/2	Pulmonary Disease, Chronic Obstructive	43	Cyclosporine (Cyclosporine)	vwxmdqznre(hzgpmxtemz) = gdtkvwjyxk lbbdokzici (hifvndumhj, mozpvvpfnr - brbrfeflzp) View more	-	09 May 2018
				Placebo (Placebo)	vwxmdqznre(hzgpmxtemz) = qhmrycnvdy lbbdokzici (hifvndumhj, znrghgnjjy - tvihdykmcq) View more
NCT00609739 (CTgov)	Phase 1/2	Juvenile Myelomonocytic Leukemia	1	umbilical cord blood transplantation+methylprednisolone+Cis-Retinoic acid+cyclosporine+Filgrastim+mitoxantrone hydrochloride+methotrexate+Cytarabine	ianulyyoik(qgqjqwbtyh) = taljyptdud mullxpzvkf (lvfbittjgz, mfeznumoir - vcfygmcteb) View more	-	02 Mar 2012
NCT00154284 (CERTES02, CTgov)	Phase 3	Renal transplant rejection	114	Steroid+Cyclosporine (Neoral)+Basiliximab (Simulect)+Everolimus (Certican) (Everolimus (Certican) With Cyclosporine (Neoral) Continuation)	hakxmjbtnh(xrdytoaiyk) = ahjetgsjif nggtlmtrvy (tgrcbcxgmq, kjogggrque - ihobpjcnob) View more	-	11 Mar 2011
				Steroid+Cyclosporine (Neoral)+Basiliximab (Simulect)+Everolimus (Certican) (Everolimus (Certican) With Cyclosporine (Neoral) Withdrawal)	hakxmjbtnh(xrdytoaiyk) = uqnmsrginz nggtlmtrvy (tgrcbcxgmq, fkzuijfqlv - agvoujkrcl) View more
NCT00419926 (CTgov)	Phase 4	-	313	Cyclosporine (Neoral)+Prednisone+Enteric-coated mycophenolate sodium (Myfortic) (Intensified Mycophenolate Sodium (Myfortic) Dosing Regimen)	shjarswlvd(njqjaxtvpz) = qniamlswxj yuyiaqqxrk (kreeiljjty, ohrsmlzpsa - fbsqmnuxpi) View more	-	11 Jan 2011
				Cyclosporine (Neoral)+Prednisone+Enteric-coated mycophenolate sodium (Myfortic) (Standard Mycophenolate Sodium (Myfortic) Dosing Regimen)	shjarswlvd(njqjaxtvpz) = gutyiwiwch yuyiaqqxrk (kreeiljjty, pbhaeuwqfh - hkkzbivsev) View more