Oxymetazoline
Kovanaze, Rhofade, Upneeq, Visine (oxymetazoline) is a small molecule pharmaceutical. Oxymetazoline was first approved as Ocuclear on 1986-05-30. It is used to treat common cold, conjunctivitis, rhinitis, and sinusitis in the USA. The pharmaceutical is active against alpha-1A adrenergic receptor and alpha-2A adrenergic receptor. In addition, it is known to target 5-hydroxytryptamine receptor 2C, alpha-2B adrenergic receptor, 5-hydroxytryptamine receptor 1D, alpha-1B adrenergic receptor, 5-hydroxytryptamine receptor 1B, alpha-1D adrenergic receptor, and alpha-2C adrenergic receptor.
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Commercial
Trade Name
FDA
EMA
Rhofade, Upneeq, Visine (generic drugs available since 2021-10-04, discontinued: Ocuclear)
CombinationsKovanaze
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Oxymetazoline hydrochloride
Oxymetazoline hydrochloride
+
Tetracaine hydrochloride
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| KOVANAZE | St Renatus | N-208032 RX | 2016-06-29 | 1 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| kovanaze | New Drug Application | 2018-11-16 |
| rhofade | New Drug Application | 2023-05-09 |
| topcare nasal | OTC monograph final | 2023-04-03 |
| upneeq | New Drug Application | 2020-10-06 |
| visine dry eye relief | OTC monograph final | 2023-01-06 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| common cold | EFO_0007214 | D003139 | J00 |
| conjunctivitis | — | D003231 | H10 |
| rhinitis | EFO_0008521 | D012220 | J31 |
| sinusitis | EFO_0007486 | D012852 | J32 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
OXYMETAZOLINE HYDROCHLORIDE, UPNEEQ, RVL PHARMS | |||
| 2023-07-08 | NP | ||
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Oxymetazoline Hydrochloride, Upneeq, Rvl Pharms | |||
| 10799481 | 2039-12-16 | U-2849 | |
| 10814001 | 2039-12-16 | DP | |
| 10898573 | 2039-12-16 | DP | |
| 10940138 | 2039-12-16 | U-2849 | |
| 11103482 | 2039-12-16 | DP | |
| 11311515 | 2039-12-16 | DP | |
| 11324722 | 2039-12-16 | U-2849 | |
| 11541036 | 2039-12-16 | DP | |
| 8357714 | 2031-08-26 | U-2849 | |
| 9867808 | 2031-08-26 | U-2849 | |
| 10912765 | 2031-08-26 | U-2849 | |
| Oxymetazoline Hydrochloride, Rhofade, Epi Hlth | |||
| 9974773 | 2035-06-11 | U-2306 | |
| 10335391 | 2035-06-11 | U-2567 | |
| 10751325 | 2035-06-11 | U-2921 | |
| 11517560 | 2035-06-11 | U-3494 | |
| 8883838 | 2031-12-01 | DP | |
| 7812049 | 2028-05-02 | U-1959 | |
| 8420688 | 2024-08-02 | U-1959 | |
| 8815929 | 2024-01-22 | U-1959 | |
| Oxymetazoline Hydrochloride / Tetracaine Hydrochloride, Kovanaze, St Renatus | |||
| 8580282 | 2030-04-02 | DP | U-1876 |
| 9308191 | 2030-04-02 | DP | U-1876 |
ATC Codes
D: Dermatologicals
— D11: Other dermatological preparations in atc
— D11A: Other dermatological preparations in atc
— D11AX: Other dermatological preparations in atc
— D11AX27: Oxymetazoline
R: Respiratory system drugs
— R01: Nasal preparations
— R01A: Decongestants and other nasal preparations for topical use
— R01AA: Sympathomimetics, plain
— R01AA05: Oxymetazoline
— R01AB: Sympathomimetics, combinations excl. corticosteroids
— R01AB07: Oxymetazoline
S: Sensory organ drugs
— S01: Ophthalmologicals
— S01G: Decongestants and antiallergics
— S01GA: Sympathomimetics used as decongestants
— S01GA04: Oxymetazoline
HCPCS
No data
Clinical
Clinical Trials
262 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hypotension | D007022 | EFO_0005251 | I95 | 2 | 4 | 4 | 14 | 12 | 34 |
| Anesthesia | D000758 | 1 | 3 | 4 | 4 | 3 | 15 | ||
| Spinal anesthesia | D000775 | — | 2 | — | 7 | 2 | 11 | ||
| Healthy volunteers/patients | — | 2 | — | — | 1 | 6 | 9 | ||
| Allergic rhinitis | D065631 | J30.9 | 2 | 1 | 1 | 3 | 1 | 8 | |
| Blood pressure | D001794 | EFO_0004325 | 2 | 1 | 1 | 1 | 4 | 8 | |
| Rosacea | D012393 | L71 | — | — | 4 | 2 | — | 6 | |
| Common cold | D003139 | EFO_0007214 | J00 | 2 | 1 | 1 | 1 | — | 5 |
| Septic shock | D012772 | A48.3 | — | 3 | — | 2 | — | 5 | |
| Cataract | D002386 | EFO_0001059 | H26.9 | — | — | 1 | 3 | 1 | 5 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Respiratory tract infections | D012141 | J06.9 | 1 | — | 4 | — | — | 5 | |
| Allergic rhinitis seasonal | D006255 | EFO_0003956 | J30 | — | 1 | 3 | — | — | 4 |
| Rhinitis | D012220 | EFO_0008521 | J31 | 1 | 1 | 1 | — | — | 3 |
| Ischemic stroke | D000083242 | 1 | 1 | 1 | — | — | 3 | ||
| Fecal incontinence | D005242 | R15 | 2 | 1 | 1 | — | — | 3 | |
| Erythema | D004890 | HP_0010783 | L53.9 | — | — | 3 | — | — | 3 |
| Cold temperature | D003080 | — | — | 2 | — | — | 2 | ||
| Vasomotor rhinitis | D012223 | EFO_0007533 | J30.0 | — | — | 1 | — | 1 | 2 |
| Eye diseases | D005128 | EFO_0003966 | H44 | — | — | 2 | — | — | 2 |
| Rhinorrhea | D000086722 | — | — | 1 | — | — | 1 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Dental caries | D003731 | EFO_0003819 | K02 | — | 3 | — | — | — | 3 |
| Periapical periodontitis | D010485 | EFO_1001391 | K04.5 | — | 3 | — | — | — | 3 |
| Post-traumatic stress disorders | D013313 | EFO_0001358 | F43.1 | — | 1 | — | — | 1 | 2 |
| Vasovagal syncope | D019462 | R55 | 1 | 1 | — | — | — | 2 | |
| Heart rate | D006339 | EFO_0004326 | 1 | 1 | — | — | — | 1 | |
| Allergic conjunctivitis | D003233 | EFO_0007141 | H10.44 | — | 1 | — | — | — | 1 |
| Mitral valve insufficiency | D008944 | HP_0001653 | 1 | 1 | — | — | — | 1 | |
| Obstetrical anesthesia | D000773 | — | 1 | — | — | — | 1 | ||
| Neoplasms | D009369 | C80 | 1 | 1 | — | — | — | 1 | |
| Spinal cord injuries | D013119 | EFO_1001919 | 1 | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Vasoconstriction | D014661 | 3 | — | — | — | 5 | 8 | ||
| Vasodilation | D014664 | 2 | — | — | — | 3 | 5 | ||
| Cardiovascular diseases | D002318 | EFO_0000319 | I98 | 1 | — | — | — | 3 | 4 |
| Postural orthostatic tachycardia syndrome | D054972 | G90.A | 1 | — | — | — | 2 | 3 | |
| Hypertension | D006973 | EFO_0000537 | I10 | 1 | — | — | — | 1 | 2 |
| Orthostatic hypotension | D007024 | I95.1 | 2 | — | — | — | — | 2 | |
| Therapeutic equivalency | D013810 | 2 | — | — | — | — | 2 | ||
| Vascular diseases | D014652 | EFO_0004264 | I77 | 1 | — | — | — | 1 | 2 |
| Surgical blood loss | D016063 | 1 | — | — | — | 1 | 2 | ||
| Autonomic nervous system diseases | D001342 | EFO_0009532 | G90 | 1 | — | — | — | 1 | 2 |
Show 9 more
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carotid endarterectomy | D016894 | — | — | — | — | 3 | 3 | ||
| Insulin resistance | D007333 | EFO_0002614 | — | — | — | — | 1 | 1 | |
| Microcirculation | D008833 | — | — | — | — | 1 | 1 | ||
| Heart failure | D006333 | EFO_0003144 | I50 | — | — | — | — | 1 | 1 |
| Obstructive sleep apnea | D020181 | EFO_0003918 | G47.33 | — | — | — | — | 1 | 1 |
| Hyperthermic intraperitoneal chemotherapy | D000084262 | — | — | — | — | 1 | 1 | ||
| Low vision | D015354 | — | — | — | — | 1 | 1 | ||
| Hip fractures | D006620 | EFO_0003964 | S72.00 | — | — | — | — | 1 | 1 |
| Cerebrovascular circulation | D002560 | — | — | — | — | 1 | 1 | ||
| Delirium | D003693 | R41.0 | — | — | — | — | 1 | 1 |
Show 18 more
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | OXYMETAZOLINE |
| INN | oxymetazoline |
| Description | Oxymetazoline is a member of the class of phenols that is 2,4-dimethylphenol which is substituted at positions 3 and 6 by 4,5-dihydro-1H-imidazol-2-ylmethyl and tert-butyl groups, respectively. A direct-acting sympathomimetic with marked alpha-adrenergic activity, it is a vasoconstrictor that is used (generally as the hydrochloride salt) to relieve nasal congestion. It has a role as an alpha-adrenergic agonist, a sympathomimetic agent, a nasal decongestant and a vasoconstrictor agent. It is a member of phenols, a carboxamidine and a member of imidazolines. It is a conjugate base of an oxymetazoline(1+). |
| Classification | Small molecule |
| Drug class | antihistamines/local vasoconstrictors (antazoline type) |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | Cc1cc(C(C)(C)C)c(O)c(C)c1CC1=NCCN1 |
Identifiers
| PDB | — |
| CAS-ID | 1491-59-4 |
| RxCUI | 7812 |
| ChEMBL ID | CHEMBL762 |
| ChEBI ID | 7862 |
| PubChem CID | 4636 |
| DrugBank | DB00935 |
| UNII ID | 8VLN5B44ZY (ChemIDplus, GSRS) |
Target
Agency Approved
ADRA1A
ADRA1A
ADRA2A
ADRA2A
Organism
Homo sapiens
Gene name
ADRA1A
Gene synonyms
ADRA1C
NCBI Gene ID
Protein name
alpha-1A adrenergic receptor
Protein synonyms
Alpha-1A adrenoceptor, Alpha-1A adrenoreceptor, Alpha-1C adrenergic receptor, Alpha-adrenergic receptor 1c, G protein coupled receptor
Uniprot ID
Mouse ortholog
Adra1a (11549)
alpha-1A adrenergic receptor (Q8BV77)
Alternate
HTR2C
HTR2C
ADRA2B
ADRA2B
HTR1D
HTR1D
ADRA1B
ADRA1B
HTR1B
HTR1B
ADRA1D
ADRA1D
ADRA2C
ADRA2C
Organism
Homo sapiens
Gene name
HTR2C
Gene synonyms
HTR1C
NCBI Gene ID
Protein name
5-hydroxytryptamine receptor 2C
Protein synonyms
5-HT-1C, 5-HT1C, 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled, 5-hydroxytryptamine receptor 1C, serotonin 5-HT-1C receptor, serotonin 5-HT-2C receptor, Serotonin receptor 2C
Uniprot ID
Mouse ortholog
Htr2c (15560)
5-hydroxytryptamine receptor 2C (Q5WRU6)
Variants
Clinical Variant
No data
Financial
Rhofade - Aclaris Therapeutics
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Rhofade - Novan
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Tabular view
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 1,448 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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356 adverse events reported
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