Delving into the Latest Updates on Pexopiprant with Synapse

A randomized, double-blind, placebo-controlled, dose-ranging, multi-center study to evaluate the efficacy and safety of GB001 when added to standard-of care (SOC) asthma maintenance therapy in adults with moderate to severe asthma and an eosinophilic phenotype with respect to asthma worsening at the end of 24 weeks of treatment.

Start Date22 Oct 2018

Sponsor / Collaborator

GB001, Inc.

100 Clinical Results associated with Pexopiprant

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100 Translational Medicine associated with Pexopiprant

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100 Patents (Medical) associated with Pexopiprant

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Literatures (Medical) associated with Pexopiprant

01 Aug 2022·CHEST

Results of a Phase 2b Trial With GB001, a Prostaglandin D2 Receptor 2 Antagonist, in Moderate to Severe Eosinophilic Asthma

Article

Author: Tompkins, Cindy-Ann ; Vyshnyvetskyy, Ivan ; Saralaya, Dinesh ; Bruey, Jean-Marie ; Hanania, Nicola A ; Ortega, Hector ; Castro, Mario ; Dittrich, Karen ; Lugogo, Njira L ; Moss, Mark H ; Osterhout, Robin ; Ludwig-Sengpiel, Andrea ; Ojanguren, Iñigo ; Dobek, Rafal ; Raghupathi, Kartik

BACKGROUNDProstaglandin D₂ receptor 2 (DP₂) antagonists inhibit prostaglandin D₂-induced effects, including recruitment and activation of cells driving asthma pathogenesis. However, challenges identifying target population and end points persist.RESEARCH QUESTIONWhat is the effect of the DP₂ antagonist GB001 on asthma worsening in patients with moderate to severe eosinophilic asthma?STUDY DESIGN AND METHODSIn this phase IIb, randomized, double-blind, placebo-controlled, dose-ranging, parallel-group, multicenter study, GB001 or placebo was added to standard-of-care treatment in patients with moderate to severe asthma with a blood eosinophil count ≥ 250 cells/μL. Patients aged ≥ 18 years to < 75 years received one of four once-daily treatments (GB001 20 mg, 40 mg, or 60 mg or placebo). The primary end point was the proportion of patients who experienced asthma worsening by 24 weeks. Efficacy analyses were performed for the intention-to-treat population and safety analyses for patients who received at least one dose of study treatment.RESULTSA total of 480 patients were treated. The ORs for asthma worsening for GB001 20 mg, 40 mg, and 60 mg vs placebo were 0.674 (95% CI, 0.398-1.142), 0.677 (95% CI, 0.399-1.149), and 0.651 (95% CI, 0.385-1.100), respectively. Analysis according to baseline blood eosinophil levels and/or fractional exhaled nitric oxide did not show greater treatment effects with higher values. Elevated liver aminotransferase levels and adverse events leading to discontinuation were more frequent for GB001 60 mg than with placebo, GB001 20 mg, and GB001 40 mg.INTERPRETATIONAlthough GB001 did not significantly reduce the odds of asthma worsening, reductions favoring GB001 were observed. Treatment effects were consistent regardless of high/low type 2 phenotype. The overall safety profile was acceptable, although GB001 60 mg was associated with risk of liver injury.CLINICAL TRIAL REGISTRATIONClinicalTrials.gov; No.: NCT03683576; URL: www.CLINICALTRIALSgov.

01 Apr 2020·The Journal of Allergy and Clinical Immunology: In PracticeQ1 · MEDICINE

A Phase 2a Study of DP2 Antagonist GB001 for Asthma

Q1 · MEDICINE

Article

Author: Ichinose, Masakazu ; Sagara, Hironori ; Asano, Koichiro ; Hirata, Masayuki ; Nakajima, Akihiro ; Tohda, Yuji ; Ortega, Hector

BACKGROUNDGB001, a DP₂ antagonist, may inhibit recruitment and activation of inflammatory cells in patients with asthma, consequently reducing airway inflammation.OBJECTIVEExplore the efficacy and safety of GB001 in adults with mild to moderate asthma.METHODSDuring a 4-week run-in period, adult patients with asthma (N = 158) received medium-dose inhaled corticosteroid and placebo and were then randomized to treatment once daily with GB001 5 mg, 20 mg, or placebo for 16 weeks or until asthma worsening/exacerbation. Patients were tapered to and then discontinued from low-dose inhaled corticosteroid at randomization and at 4 weeks postrandomization, respectively. Primary end point was change in morning peak expiratory flow (AM PEF); secondary end points included measures of asthma control. Safety was also assessed.RESULTSBaseline characteristics were similar among GB001 5 mg, 20 mg, and placebo groups. Changes in AM PEF in 5 mg and 20 mg groups versus placebo showed mean differences (95% CI) of 15.2 (3.1-27.4) L/min (P = .02) and 13.7 (1.5-25.8) L/min (P = .03), respectively. The changes in forced expiratory volume in 1 second of 55 mL and 32 mL, respectively, were not significant. There was a significant difference between GB001 20 mg and placebo for the secondary end points of time to asthma worsening/exacerbation (hazard ratio, 0.29), 5-item Asthma Control Questionnaire score (-0.60 point), the percentage of days without asthma symptoms (26%), and the percentage of rescue-free days (22%). Patients with baseline eosinophil levels greater than or equal to 300/μL had larger differences between GB001 20 mg and placebo for changes in AM PEF. Similar effects were seen in a post hoc analysis for time to worsening/exacerbations and 5-item Asthma Control Questionnaire score. The most common nonserious adverse event in the GB001 groups compared with the placebo group was nasopharyngitis.CONCLUSIONSGB001 was well tolerated and although not associated with clinically meaningful changes in lung function, improvements in asthma worsening/exacerbations and markers of asthma control were demonstrated. In addition, greater treatment effects were observed in patients with high baseline blood eosinophils. Further studies are needed to confirm these findings in the context of standard of care treatment.

01 Feb 2020·Clinical & Experimental AllergyQ2 · MEDICINE

A phase 2 study to evaluate the safety, efficacy and pharmacokinetics of DP2 antagonist GB001 and to explore biomarkers of airway inflammation in mild‐to‐moderate asthma

Q2 · MEDICINE

Article

Author: Raghupathi, Kartik ; Dittrich, Karen ; Shen, Jinshan ; Singh, Dave ; Ortega, Hector ; Tompkins, Cindy‐ann ; Fitzgerald, Mary ; Pattwell, Caroline

AbstractBackgroundGB001 is an oral antagonist of the prostaglandin D2 receptor that may inhibit recruitment and activation of airway eosinophils, reducing airway inflammation.ObjectiveTo assess GB001 safety, efficacy and pharmacokinetics from a Phase 2 study and explore the association between type 2 biomarkers (fractional exhaled nitric oxide and blood eosinophils) and asthma control markers following GB001 administration.MethodsA randomized, placebo‐controlled, double‐blind study evaluating 36 patients with mild‐to‐moderate atopic asthma. Patients receiving fluticasone propionate ≤500 mcg/day or equivalent were randomized (2:1) to GB001 (30 mg) or placebo once daily for 28 days. Safety, pharmacokinetics, forced expiratory volume in 1 second, asthma control questionnaire and rescue medication use were assessed. Clinical outcomes were analysed post hoc by baseline fractional exhaled nitric oxide (<35 and ≥35 ppb) and blood eosinophil (<250 and ≥250 cells/µL) subgroups.ResultsGB001 was well tolerated and rapidly absorbed with a 14.5‐hour terminal half‐life. Overall, GB001 demonstrated greater improvement relative to placebo in forced expiratory volume in 1 second at Day 28 (102 mL [95% CI: −110, 314]). Greater effects on forced expiratory volume in 1 second were observed in the high baseline fractional exhaled nitric oxide and blood eosinophil subgroups (207 mL [95% CI: −283, 698];133 mL [95% CI: −422, 687], respectively). These effects were observed as early as Day 2 (229 mL [95% CI: −170, 628]; 163 mL [95% CI: −223, 550] for the high baseline fractional exhaled nitric oxide and blood eosinophil subgroups, respectively) and were sustained through treatment completion.Conclusion and clinical relevanceGB001 was well tolerated, with the estimated half‐life supporting once‐daily (QD) dosing. GB001 may have a rapid and sustained effect on lung function, particularly in patients with type 2 phenotype. Further studies are needed to confirm these findings.

1

News (Medical) associated with Pexopiprant

26 Feb 2021

·endpts.com

Gossamer pushes ahead with failed asthma drug; Cullgen gets $50M Series B for protein degraders

After getting beaten up by investors over the key failure of its lead drug GB001, Gossamer had already indicated that they thought they could move ahead in asthma, though likely through a partnership. And the biotech is pushing forward on that front, according to a Q4 statement today, following talks with regulators. The company reported: Gossamer engaged with the FDA and the EMA about the clinical development path in asthma, and based off those interactions, Gossamer believes that there is a viable clinical development path for GB001, or its backup molecule, in asthma. Gossamer does not currently plan to move forward with GB001, or its backup molecule, in further clinical trials without a partner. That could prove a tough deal to complete, though, after Novartis failed with a similar therapy. In addition, asthma remains a crowded R&D field, with several top players in the mix. — John Carroll Cullgen gets $50M Series B for protein degraders A little less than three years since pulling in a $15 million round, Cullgen now has some new funds to play with. The San Diego and Shanghai-based company closed a $50 million Series B on Thursday as it continues its work in the protein degradation field. This cash will support further development of Cullgen’s platform, as well as fund pipeline programs for targeted protein degraders in oncology and other diseases. Ying Luo There’s also an IND coming later this year for Cullgen’s lead program, chairman Ying Luo said in a statement. The candidate “is a TRK protein degrader for cancer and other disease applications,” he said. Luo added, “We plan to utilize the new capital to help advance this program into human clinical studies, as well as advance our other pipeline products closer to human clinical studies.” Five new investors have backed the company, including 3E Bioventures Capital, Heights Capital Management, Octagon Capital, MSA Capital and South China Venture Capital. — Max Gelman

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100 Deals associated with Pexopiprant

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Nasal Polyps	Discovery	United States	GB001, Inc.	16 May 2019
Nasal Polyps	Discovery	Ukraine	GB001, Inc.	16 May 2019
Nasal Polyps	Discovery	Czechia	GB001, Inc.	16 May 2019
Asthma	Discovery	Czechia	Pulmagen Therapeutics LLP	01 Apr 2013
Asthma	Discovery	United States	Pulmagen Therapeutics LLP	01 Apr 2013
Asthma	Discovery	Poland	Pulmagen Therapeutics LLP	01 Apr 2013
Asthma	Discovery	Croatia	Pulmagen Therapeutics LLP	01 Apr 2013
Asthma	Discovery	Germany	Pulmagen Therapeutics LLP	01 Apr 2013
Asthma	Discovery	Hungary	Pulmagen Therapeutics LLP	01 Apr 2013
Allergic asthma	Discovery	United Kingdom	Pulmagen Therapeutics LLP	01 Sep 2011

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03683576 (CTgov)	Phase 2	Asthma	481	Placebo (Placebo)	srygiautpi(ydreiqjxig) = gqdyngvcia bveetfjqkr (nxccjxicab, jrblikrlix - fcxgtztpyi) View more	-	23 Aug 2021
				GB001 (GB001 20 mg)	srygiautpi(ydreiqjxig) = ymwfcvnnrq bveetfjqkr (nxccjxicab, ydonxrxupp - yuihyshalg) View more
NCT03956862 (CTgov)	Phase 2	Nasal Polyps \| Chronic rhinosinusitis with nasal polyps \| Chronic sinusitis	97	Placebo (Placebo)	ursmqfldge(izglkvkwzp) = zwtkhufuzf zoiejjhlzo (jsczigtuoo, gyoosguvrq - ahajurwjnh) View more	-	30 Jul 2021
				GB001 (GB001)	ursmqfldge(izglkvkwzp) = ckrbihrnsk zoiejjhlzo (jsczigtuoo, mgbclxftou - bucjpwuzza) View more
NCT03956862 (Corporate Publications) Manual	Phase 2	Asthma \| Chronic sinusitis	97	GB001	(uvcuzsyfix) = The safety and tolerability of GB001 40 mg was generally consistent with that observed in the LEDA Study. rneppzyekn (lmmeenrylh )	Negative	13 Oct 2020
NCT01448954 (Pubmed) Manual	Phase 2	Asthma \| Inflammation	36	GB001	(bucpbegvrz) = grcgleolqf rkgjuexbvz (pcsepykarr, -110 to 314) View more	Positive	01 Feb 2020
				Placebo	-