H1 Histamine Receptor antagonists, or simply H1 antagonists, are the drugs that block the action of histamine on the HI Histamine Receptor and prevent its pharmacological actions. Histamine is an endogenous chemical produced by the mast cells in the body. Histamine is released by the body in response to any allergic chemical that it encounters, like dust, pollution, or allergens, causing symptoms like runny nose, vomiting, itching, hives, itching, and more. H1 receptor is present in many body parts like the skin, lungs, T-cells, B-cells, brain, and lymphocytes. H1 Antagonists are divided into two generations that differ in the pharmacology of the drugs. 1st generation possesses the main side effect of CNS depression, causing sleepiness, while the 2nd generation is devoid of this. Hence, these are used for the prophylaxis of colds, allergies, Mountain and Morning sickness, Hay fever, Hiives, and more. Antihistamines are the treatment of choice in allergic reactions. Therefore, inhibiting the H1 Receptor might be an approach to treating various diseases associated with the pathway. Research is being conducted globally to discover new and novel molecules to be used as H1 Histamine antagonists. The development and launch of new products will thus increase the revenue of the market in the forecasted years.
A number of these inhibitors are in the market, while many are in ongoing clinical trials. 28 companies have various products in their pipelines, with 50 products in different stages of clinical trials. 6 products are in Phase 4, 12 in Phase 3, 5 in Phase 2, and 2 in Phase 1 of the clinical trials.
Key Developments of H1 Histamine Receptor Antagonists
- In March 2023, Tiefenbacher Pharmaceuticals launched Bilastine as a new OTC product in Germany.
Approved molecules of H1 Histamine Receptor Antagonists
- Rupex (Rupatadine)
- Lastacaft (Alcaftadine)
- Bepreve (Bepotastine Besilate Ophthalmic Solution)
- Diphenhydramine/Naproxen (BAY98-7111)
- Zonalon (Doxepin Cream)
- Daren (Emedastine)
Drugs in the Pipeline of H1 Histamine Receptor Antagonists
- Tonmya (Cyclobenzapb13:B40rine SL)
- Tavegil (Clemastine)
- Alesion (Epinastine)
- Zerviate (Cetirizine Ophthalmic Solution)
- Hydexor (Promethazine/Hydrocodone/Acetaminophen)
- Montelukast/Levocetirizine (HCP1102)
- Quzyttir (Cetirizine Injection)
- Belion CR (Bepotastine Sustained-Release)
- Diphenhydramine/Lorazepam/Zolpidem (SM-1)
- Norketotifen
- Alesion LX (Epinastine)
- Hivenyl (Vapitadine)
- Tussicaps (Hydrocodone/Chlorpheniramine)
- V-0162
- Promethazine/Sumatriptan (CL-H1T)
- Alervil (Pheniramine Maleate)
- Mizollen (Mizolastine)
- Secuado (Asenapine Transdermal)
- Captisol-Enabled Budesonide + Azelastine (LGD-313)
- Opipramol/Nicotine (ND0801)
Clinical Activity and Developments of H1 Histamine Receptor Antagonists
As of June 2023, 28 companies have approximately five products for 306 diseases. For these diseases, 167 trials are being conducted by players globally. For instance,
- In February 2022, Indonesia University completed a Phase 4 trial to evaluate the effect of early radiofrequency turbinate reduction, Intranasal steroid, and Antihistamine H1 on Persistent Allergic Rhinitis.
- In November 2021, Cairo University completed a Phase 3 trial to study the role of topical Cetirizine in Androgenic Alopecia in females.
|
Molecule name |
Number of studies |
|
Rupex (rupatadine) |
21 |
|
Lastacaft (alcaftadine) |
12 |
|
Bepreve (bepotastine besilate ophthalmic solution) |
10 |
|
diphenhydramine/naproxen (BAY98-7111) |
7 |
|
Zonalon (doxepin cream) |
1 |
Target Indication Analysis of H1 Histamine Receptor Antagonists
Drugs like Rupex (rupatadine) and Zonalon (doxepin cream) etc., have been approved by the FDA and other regulatory agencies to treat various indications. These are indicated for use in the treatment of urticaria, Allergic Rhinitis, Nose diseases, Running nose, skin rashes and more. These also show antihistaminic effects by controlling nausea and vomiting, hence, Promethazine and Cyclizine are also used as drugs to prevent Mountain sickness, which can be felt by many people while traveling. Promethazine and Cyclizine are also used for the prophylaxis of Morning sickness, which is a feeling of vomiting during pregnancy. 1st generation H1 Receptor Antagonists like chlorpheniramine, Doxylamine, Promethazine, and others depress the CNS causing sleepiness to many people, which is used when sleep is required by the patient. On the other hand, 2nd generation H1 Receptor Antagonists like Rupatadine, Levocetirizine, Loratadine, and others have negligible CNS depressive effects and can be taken during the day.
H1 Histamine Receptor Antagonists Regional Analysis
H1 Histamine Receptor Antagonists Market
According to a research article, Allergic Rhinitis affects 7.7% of the people in the USA which accounts for nearly 19.2 million of the US population in 2023. It affects nearly 400 million people globally. The prevalence of the disease is increasing over the years due to increasing urbanization, increasing factory and automobile emissions, and increasing environmental pollution globally. The prevalence of urticaria in 2021, according to a research study, was 12% - 23.5%. It is believed that the actual majority is much more than this range, as many people don’t report to the hospital to seek medical help. There is a good opportunity for the market players to launch new products and enter the market with the rising prevalence of allergies and allergic diseases.
Latin America
Europe
Asia Pacific
Middle East
North America
Frequently Asked Questions
Rupex (rupatadine), Lastacaft (alcaftadine), Bepreve (bepotastine besilate ophthalmic solution), and Zonalon (doxepin cream) are approved by various regulatory agencies.
These are being used to treat urticaria, Allergic Rhinitis, Nose diseases, Running nose, skin rashes, and more. Promethazine and Cyclizine are also used for the prophylaxis of Morning sickness and Mountain sickness.
Tonix Pharmaceuticals (USA), Incepta Pharmaceuticals (Bangladesh), Medexus Pharmaceuticals Inc (USA), and GSK plc (UK) are some of the major market players for H1 Histamine Receptor Antagonists.
The development of new, more effective and safer H1 histamine receptor antagonists, The increasing use of H1 histamine receptor antagonists for other indications such as allergic conjunctivitis, urticaria, and motion sickness leading to various kinds of allergies are the key opportunities for H1 Histamine Receptor Antagonists in the market.
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- Tonix Pharmaceuticals
- Medexus Pharmaceuticals
- Gsk Plc
- Boehringer Ingelheim
- J&J
- Abbvie
- Bausch Health
- Nicox
- Santen
- Bayer
- Daiichi Sankyo
- Charleston Labs
- Hanmi
- Tersera Therapeutics
- Hanlim Pharma
- Eusol Biotech
- Emergo Therapeutics
- Novartis
- Kowa
- Merck (Msd)
- Pierre Fabre
- Incepta Pharmaceuticals
- Sanofi
- Mitsubishi Tanabe
- Hisamitsu
- Ligand