Delving into the Latest Updates on Timapiprant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [4]

Target

CRTH2 x PGD2 receptor

Action

antagonists

Mechanism

CRTH2 antagonists(Prostaglandin D2 receptor 2 antagonists), PGD2 receptor antagonists(Prostaglandin D2 receptor antagonists)

Therapeutic Areas

Immune System DiseasesRespiratory DiseasesInfectious Diseases+ [6]

Active Indication-

Inactive Indication

Allergic asthmaAsthmaCommon Cold+ [8]

Originator Organization

Oxagen Ltd.

Active Organization-

Inactive Organization

CHIESI Farmaceutici SpA

Oxagen Ltd.

Atopix Therapeutics Ltd.

Drug Highest PhasePendingPhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC21H17FN2O2

InChIKeyFATGTHLOZSXOBC-UHFFFAOYSA-N

CAS Registry851723-84-7

The present work focused on evaluating the feasibility of fused deposition modeling (FDM) in the development of a dosage form containing Timapiprant (TMP), also known as CHF6532, which is a novel active molecule indicated in the potential treatment of eosinophilic asthma upon oral administration. The resulting product could be an alternative, with potential towards personalization, of immediate release (IR) tablets used in the clinical studies. Formulations based on different polymeric carriers were screened, leading to the identification of a polyvinyl alcohol-based one, which turned out acceptable for versatility in terms of active ingredient content, printability and dissolution performance (i.e. capability to meet the dissolution specification set, envisaging >80% of the drug dissolved within 30 min). Following an in-depth evaluation on the influence of TMP solid state and of the voids volume resulting from printing on dissolution, few prototypes with shapes especially devised for therapy customization were successfully printed and were compliant with the dissolution specification set.

01 May 2023·Translational vision science & technology

Attenuation of Laser-Induced Choroidal Neovascularization by Blockade of Prostaglandin D2 Receptor 2.

Article

Author: Ueta, Takashi ; Inoue, Tatsuya ; Aihara, Makoto ; Urade, Yoshihiro ; Soga, Hirotsugu ; Kawashima, Hidetoshi ; Kaburaki, Toshikatsu

PurposeThe purpose of this study was to investigate the impact of prostaglandin D2 (PGD2) receptor 2 (DP2) on choroidal neovascularization (CNV) formation in mice.MethodsUsing a laser-induced CNV model, the CNV size of wild-type (WT) mice treated with DP2 antagonist (CAY10471 or OC000459) was compared with that of untreated mice. Vascular endothelial growth factor (VEGF) and MCP-1 levels were also compared between the two groups. Similar experiments were performed comparing DP2 knockout (DP2KO) mice with WT mice (8 and 56 weeks old). The number of infiltrating macrophages to laser spots was also compared between the WT and DP2KO mice. We administered a DP2 antagonist to 15-methyl PGD2 (a DP2 agonist)-stimulated ARPE-19 cells and measured VEGF secretion by enzyme-linked immunosorbent assay. Tube formation assay was performed on human umbilical vein endothelial cells with or without a DP2 antagonist.ResultsCNV sizes were significantly smaller in mice treated with CAY10471 or OC000459 than in those treated with vehicle. Similarly, the CNV size of DP2KO mice was significantly smaller than that of WT mice. The number of macrophages at laser spots in DP2KO mice was significantly lower than that in WT mice. The VEGF concentration of lasered DP2KO mice's eyes was significantly lower than that of lasered WT mice' eyes. DP2 antagonist treatment suppressed VEGF secretion in ARPE-19 cells under 15-methyl PGD2 stimulation. The tube formation assay suggested that lumen formation was inhibited by a DP2 antagonist.ConclusionsDP2 blockade attenuated choroidal neovascularization.Translational RelevanceDrugs targeting DP2 are potentially a novel treatment for age-related macular degeneration.

01 Feb 2023·Digestive and Liver Disease

Treatment Trends for Eosinophilic Esophagitis and the Other Eosinophilic Gastrointestinal Diseases: Systematic Review of Clinical Trials

Review

Author: de Bortoli, Nicola ; Barberio, Brigida ; Maniero, Daria ; Greco, Eliana ; Savarino, Vincenzo ; Visaggi, Pierfrancesco ; Black, Christopher J ; Ford, Alexander C ; Ghisa, Matteo ; Savarino, Edoardo

BACKGROUNDEosinophilic gastrointestinal diseases (EGIDs) are chronic inflammatory disorders of the gut, including eosinophilic esophagitis (EoE), gastritis (EoG), duodenitis (EoD), gastroenteritis (EoGE), and colitis (EoC). Available treatments may be ineffective in some patients, and several clinical trials are investigating alternative treatments.AIMWe performed a systematic review of clinical trials to illustrate EGIDs treatment research trends.METHODSWe searched clinicaltrials.gov to identify studies investigating EGIDs treatment. For each trial we analysed relevant data, including therapeutic intervention, method of administration, study outcomes, and temporal trends.RESULTSFor EoE, 66 studies were eligible: 26 testing topical corticosteroids (39.4%), 17 (25.8%) monoclonal antibodies, eight (12.1%) dietary measures, five (7.6%) immunomodulators, one (1.5%) esophageal dilation, and nine (13.6%) other medical treatment strategies. With regard to EoG, EoD, and EoGE, 10 studies were testing monoclonal antibodies (71.5%), one immunomodulators (7.1%), one dietary measures (7.1%), and two other treatments (14.3%). There were no trials for EoC. Ongoing studies on corticosteroids are focused on novel delivery systems, including viscous suspensions, orally disintegrating tablets, or capsules. Increased research on monoclonal antibodies was seen from 2018, with interleukin (IL)-4 receptor-α, IL-5 receptor-α, IL-5, IL-13, IL-15, and Siglec-8 as the targets.CONCLUSIONClinical trials on EGIDs are predominantly investigating corticosteroids or monoclonal antibodies. EGIDs therapeutic landscape will be trasnformed imminently.

100 Deals associated with Timapiprant

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB11900

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 3	United States	CHIESI Farmaceutici SpA	22 Sep 2021
Eosinophilic Esophagitis	Phase 3	Switzerland	Oxagen Ltd.	01 Aug 2010
Persistent asthma	Phase 3	Russia	Oxagen Ltd.	01 Apr 2009
Persistent asthma	Phase 3	Romania	Oxagen Ltd.	01 Apr 2009
Persistent asthma	Phase 3	Poland	Oxagen Ltd.	01 Apr 2009
Persistent asthma	Phase 3	Bulgaria	Oxagen Ltd.	01 Apr 2009
Persistent asthma	Phase 3	Hungary	Oxagen Ltd.	01 Apr 2009
Persistent asthma	Phase 3	Ukraine	Oxagen Ltd.	01 Apr 2009
Rhinitis, Allergic, Seasonal	Phase 3	Austria	Oxagen Ltd.	01 Mar 2007
Allergic asthma	Phase 3	United Kingdom	Oxagen Ltd.	01 Feb 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02660489 (CTgov)	Phase 2	Rhinovirus infection \| Asthma \| Common Cold	44	OC459+Rhinovirus (OC459 (CRTH2 Antagonist))	mkmyzdgebk(pcmynrquto) = szlgcxjduk xbeakazxki (bbgdmtfdoj, iteovdovjw - ocwnbvdwtz) View more	-	26 Feb 2021
				Rhinovirus (Placebo)	mkmyzdgebk(pcmynrquto) = hxfhuksdxr xbeakazxki (bbgdmtfdoj, byrzkgckcl - vcslgstukt) View more
ERS2019	Not Applicable	Pulmonary Eosinophilia sputum eosinophil counts	68	Timapiprant 50 mg	qveczkbiun(kfpdpcfffo): ml = 127 (95% CI, -77 to 330), P-Value = 0.214	Positive	28 Sep 2019
				Placebo
NCT02002208 (CTgov)	Phase 2	Moderate Atopic Dermatitis \| Severe Atopic Dermatitis	142	OC000459 (OC000459 Tablets)	nhcwwtnmqh(phkzdyswma) = txcmjdkhqn biuowtdtax (dxcdykbbst, icwhuqproi - znmrmyrqhc) View more	-	08 Dec 2016
				OC000459 (Placebo Tablets)	nhcwwtnmqh(phkzdyswma) = emvdhtztsq biuowtdtax (dxcdykbbst, ykfspefmia - xyeheyiocr) View more
UEGW2013	Not Applicable	Eosinophilic Esophagitis	-	OC000459 100 mg	ahnwjmtcuo(hlhydbixor) = donqfbvkzh ifvvphufyn (uwxpavnfhm ) View more	-	01 Oct 2013
				Placebo	ahnwjmtcuo(hlhydbixor) = oypewodqwp ifvvphufyn (uwxpavnfhm ) View more
NCT01057927 (Pubmed \| Clin Exp Allergy)	Phase 2	Moderate persistent asthma	132	OC000459 200 mg	(wmlarladjx) = cezguyxrlp jqujkizgta (zjewgwxgoh )	Positive	01 Jan 2012
				Placebo	(wmlarladjx) = qwcyzkgudy jqujkizgta (zjewgwxgoh )