| Candidate ID: | R0460 |
| Source ID: | DB01234 |
| Source Type: | approved; investigational; vet_approved |
| Compound Type: |
small molecule
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| Compound Name: |
Dexamethasone
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| Synonyms: |
1-Dehydro-16alpha-methyl-9alpha-fluorohydrocortisone; 1-Dehydro-16α-methyl-9α-fluorohydrocortisone; 16alpha-Methyl-9alpha-fluoro-1-dehydrocortisol; 16α-Methyl-9α-fluoro-1-dehydrocortisol; 9alpha-Fluoro-16alpha-methylprednisolone; 9α-Fluoro-16α-methylprednisolone; Dexamethasone
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| Molecular Formula: |
C22H29FO5
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| SMILES: |
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
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| Structure: |
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| DrugBank Description: |
Dexamethasone, or MK-125, is a corticosteroid fluorinated at position 9 used to treat endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions. Developed in 1957, it is structurally similar to other corticosteroids like and .
Dexamethasone was granted FDA approval on 30 October 1958. In a press release for the Randomized Evaluation of COVID-19 Therapy (RECOVERY) trial on 16 June 2020, dexamethasone was recommended for use in COVID-19 patients with severe respiratory symptoms. Dexamethasone reduced deaths by approximately one third in patients requiring ventilation and by one fifth in those requiring oxygen.
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| CAS Number: |
50-02-2
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| Molecular Weight: |
392.4611
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| DrugBank Indication: |
Dexamethasone and otic suspension is indicated for bacterial infections with inflammation in acute otitis media and acute otitis externa. Intramuscular and intravenous injections are indicated for a number of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions. Oral tablets are indicated for the treatment of multiple myeloma. An intravitreal implant is indicated for some forms of macular edema and non-infectious posterior uveitis affecting the posterior of the eye. Various ophthalmic formulations are indicated for inflammatory conditions of the eye.
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| DrugBank Pharmacology: |
Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Dexamethasone's duration of action varies depending on the route. Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces. Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.
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| DrugBank MoA: |
The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.
Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.
Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.
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| Targets: |
Glucocorticoid receptor agonist; Nuclear receptor subfamily 0 group B member 1 stimulator; Annexin A1 agonist; Nitric oxide synthase, inducible negative modulator; Nuclear receptor subfamily 1 group I member 2 agonist
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| Inclusion Criteria: |
Therapeutic strategy associated
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