Clinical targeting of MCs or their products
| Target MC product . | Example . | Mechanism and indications . | Reference(s) . |
|---|---|---|---|
| Inhibition of MCs or their products | |||
| Antihistamines | First generation, for example, diphenhydramine | Mainstay of treatment for allergic disorders such as mastocytosis, chronic idiopathic urticaria, and acquired cold urticaria | 126 |
| Second generation, for example, loratadine, cetirizine, etc | Are nonsedating because they do not cross the blood-brain barrier, have proven especially effective in both perennial and seasonal allergic rhinitis | ||
| Antileukotrienes | Montelukast and the related agents Zafirlukast and Pranlukast | Inhibit the cysteinyl leukotriene receptor CysLT1 which is widely expressed, therefore effects of these drugs are not exclusive to the endothelium | 127 |
| Zileuton | Inhibits 5-lipoxygenase, the enzyme that converts arachidonic acid to LTA4 as the first step of leukotriene synthesis | ||
| Protease inhibition | Tryptase inhibition: developmental phase | Appears promising for allergic inflammation | 128 |
| Chymase inhibition: developmental phase | Animal models of aneurysm, atherosclerosis, myocardial infarction | 47,129 | |
| Anti-TNF agents | Etanercept | A soluble TNF receptor-Fc fusion protein indicated for rheumatoid arthritis, inflammatory bowel disease, and a variety of other inflammatory conditions | 130 |
| Infliximab | Anti-TNF monoclonal antibody indicated for rheumatoid arthritis, inflammatory bowel disease, and a variety of other inflammatory conditions | ||
| MC stabilizers | Cromolyn, Ketotifen and others prevent degranulation and limit MC activation | Asthma and allergic rhinitis | 131 |
| Kit receptor-targeting drugs | Imatinib and other tyrosine kinase inhibitors | Effective in some subsets of human patients with MC neoplastic disease. | 132 |
| Promoting MC function | |||
| MC-activating agents | Developmental phase | Small-molecule MC activators are being explored as adjuvants | 133 |
| Target MC product . | Example . | Mechanism and indications . | Reference(s) . |
|---|---|---|---|
| Inhibition of MCs or their products | |||
| Antihistamines | First generation, for example, diphenhydramine | Mainstay of treatment for allergic disorders such as mastocytosis, chronic idiopathic urticaria, and acquired cold urticaria | 126 |
| Second generation, for example, loratadine, cetirizine, etc | Are nonsedating because they do not cross the blood-brain barrier, have proven especially effective in both perennial and seasonal allergic rhinitis | ||
| Antileukotrienes | Montelukast and the related agents Zafirlukast and Pranlukast | Inhibit the cysteinyl leukotriene receptor CysLT1 which is widely expressed, therefore effects of these drugs are not exclusive to the endothelium | 127 |
| Zileuton | Inhibits 5-lipoxygenase, the enzyme that converts arachidonic acid to LTA4 as the first step of leukotriene synthesis | ||
| Protease inhibition | Tryptase inhibition: developmental phase | Appears promising for allergic inflammation | 128 |
| Chymase inhibition: developmental phase | Animal models of aneurysm, atherosclerosis, myocardial infarction | 47,129 | |
| Anti-TNF agents | Etanercept | A soluble TNF receptor-Fc fusion protein indicated for rheumatoid arthritis, inflammatory bowel disease, and a variety of other inflammatory conditions | 130 |
| Infliximab | Anti-TNF monoclonal antibody indicated for rheumatoid arthritis, inflammatory bowel disease, and a variety of other inflammatory conditions | ||
| MC stabilizers | Cromolyn, Ketotifen and others prevent degranulation and limit MC activation | Asthma and allergic rhinitis | 131 |
| Kit receptor-targeting drugs | Imatinib and other tyrosine kinase inhibitors | Effective in some subsets of human patients with MC neoplastic disease. | 132 |
| Promoting MC function | |||
| MC-activating agents | Developmental phase | Small-molecule MC activators are being explored as adjuvants | 133 |