H1 histamine receptor — Drug Target

All drugs that target H1 histamine receptor — marketed and clinical-stage. Includes 17 drug classes acting on this target.

Drug classes

First-generation H1 antihistamine · Second-generation H1-receptor antagonist (non-sedating antihistamine) · Selective H1-receptor antagonist / mast cell stabilizer · Selective H1-receptor antagonist · H1 receptor antagonist (first-generation antihistamine) · H1-receptor antagonist (second-generation antihistamine) · Selective H1-receptor antagonist (intranasal antihistamine) · First-generation H1 receptor antagonist (antihistamine) · Selective H1-receptor antagonist (antihistamine) · H1-receptor antagonist (non-sedating antihistamine) · Selective H1-receptor antagonist (second-generation antihistamine) · H1-receptor antagonist (selective, non-sedating antihistamine)

Marketed (10)

• Benadryl demand · University of Pennsylvania · First-generation H1 antihistamine · Allergy/Immunology
  Benadryl (diphenhydramine) is a first-generation antihistamine that blocks H1 histamine receptors to reduce allergic and inflammatory responses.
• fexofenadine HCl · Sanofi · Second-generation H1-receptor antagonist (non-sedating antihistamine) · Allergy/Immunology
  Fexofenadine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without crossing the blood-brain barrier.
• Hydroxyzine HCL · National Cancer Institute (NCI) · First-generation H1 antihistamine · Psychiatry, Dermatology, Allergy/Immunology
  Hydroxyzine is a first-generation antihistamine that blocks H1 receptors to reduce histamine-mediated allergic and anxiety responses.
• Atarax (Hydroxyzine) · University Hospital, Toulouse · First-generation H1 antihistamine · Psychiatry / Dermatology / Allergy
  Hydroxyzine is a first-generation antihistamine that blocks H1 receptors to reduce histamine-mediated allergic and anxiety responses.
• Olopatadine Nasal Spray · ORA, Inc. · Selective H1-receptor antagonist / mast cell stabilizer · Allergy / Immunology
  Olopatadine is a selective H1-receptor antagonist and mast cell stabilizer that blocks histamine-mediated allergic responses in the nasal mucosa.
• alcaftadine 0.25% ophthalmic solution · Allergan · Selective H1-receptor antagonist · Ophthalmology
  Alcaftadine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses in the eye.
• Diphenhydramine 5% · Federal State Budgetary Scientific Institution, Research Institute of Fundamental and Clinical Immunology · H1 receptor antagonist (first-generation antihistamine) · Allergy/Immunology
  Diphenhydramine is a first-generation antihistamine that blocks H1 histamine receptors to reduce allergic and inflammatory responses.
• Antihistamine Cetirizine Hydrochloride · Goldman, Butterwick, Fitzpatrick and Groff · H1-receptor antagonist (second-generation antihistamine) · Immunology / Allergy
  Cetirizine hydrochloride blocks histamine H1 receptors on cells, preventing histamine-mediated allergic responses.
• Azelastine - intranasal application · Association Asthma, Bulgaria · Selective H1-receptor antagonist (intranasal antihistamine) · Allergy/Immunology
  Azelastine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses in the nasal mucosa.
• olopatadine (OLO) · University of Chicago · Selective H1-receptor antagonist / mast cell stabilizer · Allergy / Immunology
  Olopatadine is a selective H1-receptor antagonist and mast cell stabilizer that blocks histamine-mediated allergic responses.

Phase 3 pipeline (15)

• Diphenhydramine IV · Hoffmann-La Roche · First-generation H1 receptor antagonist (antihistamine) · Allergy/Immunology
  Diphenhydramine is a first-generation antihistamine that blocks H1 histamine receptors to reduce allergic and inflammatory responses.
• Comparator: loratadine · Organon and Co · H1-receptor antagonist (second-generation antihistamine) · Allergy/Immunology
  Loratadine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without significant central nervous system penetration.
• Vehicle of Bilastine Ophthalmic Solution · Faes Farma, S.A. · Selective H1-receptor antagonist (antihistamine) · Ophthalmology / Allergy
  Bilastine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses in ocular tissues.
• Non sedating H1-antihistamine · Sanofi · H1-receptor antagonist (non-sedating antihistamine) · Allergy/Immunology
  Selectively blocks H1 histamine receptors on mast cells and basophils without crossing the blood-brain barrier, preventing histamine-mediated allergic responses without causing sedation.
• Comparator: cetirizine · Organon and Co · Selective H1-receptor antagonist (second-generation antihistamine) · Immunology / Allergy
  Cetirizine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without significant central nervous system penetration.
• Placebo-Cetirizine · UCB Pharma · Selective H1-receptor antagonist (second-generation antihistamine) · Immunology / Allergy
  Cetirizine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses in the central and peripheral nervous systems.
• Levocabastine HCL · Chong Kun Dang Pharmaceutical · H1-receptor antagonist (selective, non-sedating antihistamine) · Immunology / Allergy
  Levocabastine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses.
• Fexofenadine, Comparator = Montelukast · Sanofi · Selective H1-receptor antagonist (second-generation antihistamine) · Immunology / Allergy
  Fexofenadine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without crossing the blood-brain barrier.
• Ketotifen Fumarate 0.035% · Bausch & Lomb Incorporated · H1-receptor antagonist and mast cell stabilizer · Ophthalmology / Allergy
  Ketotifen is a selective H1-receptor antagonist and mast cell stabilizer that prevents allergic reactions by blocking histamine release and reducing mast cell degranulation.
• Rescue Medication: Olopatadine ophthalmic drops · ALK-Abelló A/S · Selective H1-receptor antagonist and mast cell stabilizer · Ophthalmology / Allergy
  Olopatadine is a selective H1-receptor antagonist and mast cell stabilizer that blocks histamine-mediated allergic responses in the eye.
• Dexchlorpheniramine 1% gel · Mantecorp Industria Quimica e Farmaceutica Ltd. · H1-receptor antagonist (first-generation antihistamine) · Dermatology / Allergy
  Dexchlorpheniramine is a selective H1-receptor antagonist that blocks histamine-mediated allergic and inflammatory responses in topical form.
• Dexchlorpheniramine 1% lotion · Mantecorp Industria Quimica e Farmaceutica Ltd. · H1-receptor antagonist (first-generation antihistamine) · Dermatology / Allergy
  Dexchlorpheniramine is a first-generation H1-receptor antagonist that blocks histamine binding to reduce allergic and inflammatory responses in the skin.
• Bepotastine besilate formulation · Bausch & Lomb Incorporated · H1-receptor antagonist · Ophthalmology / Allergy
  Bepotastine besilate is a selective H1-receptor antagonist that blocks histamine signaling to reduce allergic symptoms.
• Rescue Medication: Loratadine tablets · ALK-Abelló A/S · H1-receptor antagonist (second-generation/non-sedating antihistamine) · Allergy/Immunology
  Loratadine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without significant central nervous system penetration.
• Bilastine Ophthalmic Solution 0.6% · Faes Farma, S.A. · Selective H1-receptor antagonist (antihistamine) · Ophthalmology / Allergy
  Bilastine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses in the eye.