Bilastine

"

GPCR/G ProteinImmunology/Inflammation-

Bilastine?????????H1??????????????????????????????????????????????????????????????????

Histamine Receptor

相關產(chǎn)品

Pitolisant hydrochloride-Perphenazine-Osthole-Clemastine fumarate-Clemizole hydrochloride-Promethazine hydrochloride-Azelastine hydrochloride-Bepotastine Beslilate-Diphenylpyraline hydrochloride-Famotidine-Histamine-Alcaftadine-Cetirizine dihydrochloride-Desloratadine-Ebrotidine-

生物活性

Description

Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].

Clinical Trial

NCT01271075

Charite University, Berlin, Germany-Faes Farma, S.A.

Cold Contact Urticaria

September 2010

Phase 2-Phase 3

NCT01081574

Faes Farma, S.A.

Allergic Rhinoconjunctivitis-Chronic Urticaria

January 2010

Phase 1-Phase 2

NCT01124123

Faes Farma, S.A.

Healthy

May 2010

Phase 1

NCT02576041

Menarini International Operations Luxembourg SA

Allergic Rhinitis-Urticaria

October 2015

Phase 4

NCT00572611

Faes Farma, S.A.-Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd-MDS Pharma Services Switzerland AG

Healthy

November 2007

Phase 1

NCT02513290

Universidade do Sul de Santa Catarina

Allergic Rhinitis

August 2013

Phase 4

NCT02213367

Charite University, Berlin, Germany

Chronic Urticaria

July 2014

Phase 3

NCT02761252

Menarini International Operations Luxembourg SA

Seasonal Allergic Rhinoconjunctivitis-Asthma

April 2016

Phase 4

NCT00574379

Faes Farma, S.A.-Merck Sharp & Dohme Corp.-Allied Research International

Seasonal Allergic Rhinitis-Hay Fever-Allergic Conjunctivitis-Hypersensitivity

December 2007

Phase 2

NCT00574210

Faes Farma, S.A.-Allied Research International

Seasonal Allergic Rhinitis-Hay Fever-Rhinoconjunctivitis

October 2007

Phase 2

NCT01400828

Yuhan Corporation

Seasonal Allergic Rhinitis

June 2011

Phase 3

NCT01108783

Faes Farma, S.A.

Seasonal Allergic Rhinitis

April 2003

Phase 3

NCT00420082

Faes Farma, S.A.

Seasonal Allergic Rhinitis

October 2006

Phase 2

NCT00419783

Faes Farma, S.A.

Healthy

August 2006

Phase 1

NCT01127620

Faes Farma, S.A.

Perennial Allergic Rhinitis

May 2004

Phase 3

NCT00504933

Faes Farma, S.A.

Seasonal Allergic Rhinitis

May 2005

Phase 3

NCT00421109

Faes Farma, S.A.

Urticaria

July 2006

Phase 3

NCT01940393

Grupo de Alergología Clínica y Experimental

Urticaria

August 2013

Phase 4

NCT02557269

Association Asthma, Bulgaria-Nasaleze

Seasonal Allergic Rhinitis

May 2015

Phase 4

NCT01271075

Charite University, Berlin, Germany-Faes Farma, S.A.

Cold Contact Urticaria

September 2010

Phase 2-Phase 3

NCT01081574

Faes Farma, S.A.

Allergic Rhinoconjunctivitis-Chronic Urticaria

January 2010

Phase 1-Phase 2

NCT01124123

Faes Farma, S.A.

Healthy

May 2010

Phase 1

NCT02576041

Menarini International Operations Luxembourg SA

Allergic Rhinitis-Urticaria

October 2015

Phase 4

NCT00572611

Faes Farma, S.A.-Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd-MDS Pharma Services Switzerland AG

Healthy

November 2007

Phase 1

NCT02513290

Universidade do Sul de Santa Catarina

Allergic Rhinitis

August 2013

Phase 4

NCT02213367

Charite University, Berlin, Germany

Chronic Urticaria

July 2014

Phase 3

NCT02761252

Menarini International Operations Luxembourg SA

Seasonal Allergic Rhinoconjunctivitis-Asthma

April 2016

Phase 4

NCT00574379

Faes Farma, S.A.-Merck Sharp & Dohme Corp.-Allied Research International

Seasonal Allergic Rhinitis-Hay Fever-Allergic Conjunctivitis-Hypersensitivity

December 2007

Phase 2

NCT00574210

Faes Farma, S.A.-Allied Research International

Seasonal Allergic Rhinitis-Hay Fever-Rhinoconjunctivitis

October 2007

Phase 2

NCT01400828

Yuhan Corporation

Seasonal Allergic Rhinitis

June 2011

Phase 3

NCT01108783

Faes Farma, S.A.

Seasonal Allergic Rhinitis

April 2003

Phase 3

NCT00420082

Faes Farma, S.A.

Seasonal Allergic Rhinitis

October 2006

Phase 2

NCT00419783

Faes Farma, S.A.

Healthy

August 2006

Phase 1

NCT01127620

Faes Farma, S.A.

Perennial Allergic Rhinitis

May 2004

Phase 3

NCT00504933

Faes Farma, S.A.

Seasonal Allergic Rhinitis

May 2005

Phase 3

NCT00421109

Faes Farma, S.A.

Urticaria

July 2006

Phase 3

NCT01940393

Grupo de Alergología Clínica y Experimental

Urticaria

August 2013

Phase 4

NCT02557269

Association Asthma, Bulgaria-Nasaleze

Seasonal Allergic Rhinitis

May 2015

Phase 4

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References

[1].Corcostegui, R., et al., Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D, 2005. 6(6): p. 371-84.

[2].Jauregizar, N., et al., Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet, 2009. 48(8): p. 543-54.

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