Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H19ClN2 |
| Molecular Weight | 310.821 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C2C(CCC3=C(N=CC=C3)C2=C4CCNCC4)=C1
InChI
InChIKey=JAUOIFJMECXRGI-UHFFFAOYSA-N
InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
| Molecular Formula | C19H19ClN2 |
| Molecular Weight | 310.821 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11243504Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021165s017,021300s014,021312s015,021563s003lbl.pdf
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11243504
Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021165s017,021300s014,021312s015,021563s003lbl.pdf
Desloratadine is an active, descarboethoxy metabolite of loratadine. It acts by selective inhibition of H1 histamine receptor and thus provides relief to patients with allergic rhinitis and chronic idiopathic urticaria. Desloratadine was approved by FDA and it is currently marketed under the name Clarinex (among the others).
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL231 |
0.87 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | CLARINEX Approved UseDesloratadine Tablets are indicated for: Seasonal Allergic Rhinitis, Perennial Allergic Rhinitis, Chronic Idiopathic Urticaria. Launch Date2001 |
|||
| Palliative | CLARINEX Approved UseDesloratadine Tablets are indicated for: Seasonal Allergic Rhinitis, Perennial Allergic Rhinitis, Chronic Idiopathic Urticaria. Launch Date2001 |
|||
| Palliative | CLARINEX Approved UseDesloratadine Tablets are indicated for: Seasonal Allergic Rhinitis, Perennial Allergic Rhinitis, Chronic Idiopathic Urticaria. Launch Date2001 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4 ng/mL |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
56.9 ng × h/mL |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
27 h |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
84.5% |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1.25 mg 1 times / day steady, oral Dose: 1.25 mg, 1 times / day Route: oral Route: steady Dose: 1.25 mg, 1 times / day Sources: |
unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sex: M+F Sources: |
Disc. AE: Somnolence, Abdominal pain... AEs leading to discontinuation/dose reduction: Somnolence (1 patient) Sources: Abdominal pain (1 patient) |
45 mg 1 times / day multiple, oral Highest studied dose Dose: 45 mg, 1 times / day Route: oral Route: multiple Dose: 45 mg, 1 times / day Sources: |
healthy, adult Health Status: healthy Age Group: adult Sex: M+F Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Abdominal pain | 1 patient Disc. AE |
1.25 mg 1 times / day steady, oral Dose: 1.25 mg, 1 times / day Route: oral Route: steady Dose: 1.25 mg, 1 times / day Sources: |
unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sex: M+F Sources: |
| Somnolence | 1 patient Disc. AE |
1.25 mg 1 times / day steady, oral Dose: 1.25 mg, 1 times / day Route: oral Route: steady Dose: 1.25 mg, 1 times / day Sources: |
unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sex: M+F Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| likely | ||||
| likely | ||||
| likely | ||||
| likely | no (pharmacogenomic study) Comment: pharmacogenotype 2C19 does not correlate with systemic exposure Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-165_Clarinex_biopharmr_P1.pdf#page=19 Page: 19.0 |
|||
| likely | no (pharmacogenomic study) Comment: lack of correlation in between 2D6 genotype and 3-OH DCL formation Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-165_Clarinex_biopharmr_P1.pdf#page=10 Page: 10.0 |
|||
| likely | weak (co-administration study) Comment: Coadministration of ketonconazole, mean drug Cmax and AUC0-24 values at steady state were increased by 29-45% and 21-39%, respectively; Coadministration with erythromycin, mean drug Cmax and AUC 0-24 at steady state were increased by 24% and 14%, respectively. Page: 10.0 |
|||
Sources: https://dmd.aspetjournals.org/content/43/9/1294 Page: 1.0 |
yes | |||
| yes | weak (co-administration study) Comment: Coadministration of ketonconazole, mean drug Cmax and AUC0-24 values at steady state were increased by 29-45% and 21-39%, respectively; Coadministration with erythromycin, mean drug Cmax and AUC 0-24 at steady state were increased by 24% and 14%, respectively. |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Improvements in simulated real-world relevant performance for patients with seasonal allergic rhinitis: impact of desloratadine. | 2004-04 |
|
| High-performance liquid chromatographic method for the bioequivalence evaluation of desloratadine fumarate tablets in dogs. | 2004-03-10 |
|
| Gateways to clinical trials. | 2004-02-28 |
|
| Inhibition of cold urticaria by desloratadine. | 2004-01 |
|
| Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research. | 2004-01 |
|
| Gateways to clinical trials. | 2003-12 |
|
| Interactions of olopatadine and selected antihistamines with model and natural membranes. | 2003-12 |
|
| Desloratadine for allergic rhinitis. | 2003-11-15 |
|
| [Modern antihistaminics against allergic rhinitis. Better breathing without side effects]. | 2003-10-30 |
|
| Reliable and specific high-performance liquid chromatographic method for simultaneous determination of loratadine and its metabolite in human plasma. | 2003-10-25 |
|
| Loratadine, desloratadine and pregnancy: don't use, risk of hypospadias. | 2003-10 |
|
| A comparison of the effect of diphenhydramine and desloratadine on vigilance and cognitive function during treatment of ragweed-induced allergic rhinitis. | 2003-10 |
|
| Efficacy and safety profile of fexofenadine HCl: a unique therapeutic option in H1-receptor antagonist treatment. | 2003-10 |
|
| Comparison of the effects of desloratadine and levocetirizine on histamine-induced wheal, flare and itch in human skin. | 2003-10 |
|
| Twenty-four-hour activity and consistency of activity of levocetirizine and desloratadine in the skin. | 2003-10 |
|
| Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine. | 2003-08-13 |
|
| Pharmacokinetic properties of single-dose loratadine and ambroxol alone and combined in tablet formulations in healthy men. | 2003-08 |
|
| Efficacy of azelastine nasal spray in patients with an unsatisfactory response to loratadine. | 2003-08 |
|
| Studies on performance and sleepiness with the H1-antihistamine, desloratadine. | 2003-08 |
|
| Validation of a sensitive and automated 96-well solid-phase extraction liquid chromatography-tandem mass spectrometry method for the determination of desloratadine and 3-hydroxydesloratadine in human plasma. | 2003-07-25 |
|
| Comparison of ketotifen fumarate ophthalmic solution alone, desloratadine alone, and their combination for inhibition of the signs and symptoms of seasonal allergic rhinoconjunctivitis in the conjunctival allergen challenge model: a double-masked, placebo- and active-controlled trial. | 2003-07 |
|
| Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects. | 2003-07 |
|
| Desloratadine inhibits allergen-induced airway inflammation and bronchial hyperresponsiveness and alters T-cell responses in murine models of asthma. | 2003-07 |
|
| [Safety of new antihistamines]. | 2003-06 |
|
| [Clinical aspects of anti-inflammatory action of antihistamines]. | 2003-06 |
|
| The effects of histamine and leukotriene receptor antagonism on nasal mannitol challenge in allergic rhinitis. | 2003-06 |
|
| Effects of mediator antagonism on mannitol and adenosine monophosphate challenges. | 2003-06 |
|
| Comparison of the effects of desloratadine 5-mg daily and placebo on nasal airflow and seasonal allergic rhinitis symptoms induced by grass pollen exposure. | 2003-06 |
|
| [Multicenter study of the effectiveness and tolerability of desloratadine in seasonal allergic rhinitis]. | 2003-05-25 |
|
| First do no harm: managing antihistamine impairment in patients with allergic rhinitis. | 2003-05 |
|
| Comparative effects of desloratadine versus montelukast on asthma symptoms and use of beta 2-agonists in patients with seasonal allergic rhinitis and asthma. | 2003-04 |
|
| Efficacy and safety of desloratadine 5 mg once daily in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebo-controlled trial. | 2003-04 |
|
| Gateways to clinical trials. March 2003. | 2003-03 |
|
| Double-stranded RNA viruses in a mycocinogenic strain of Cystofilobasidium infirmominiatum. | 2003-03 |
|
| Decongestant effects of antihistamines: a class effect? | 2003-03 |
|
| Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. | 2003-03 |
|
| P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. | 2003-03 |
|
| Comparative in vivo bioactivity of modern H1-antihistamines on AMP challenge in atopic asthma. | 2003-02 |
|
| Desloratadine: a nonsedating antihistamine. | 2003-02 |
|
| The effect of ketotifen on inflammatory markers in allergic conjunctivitis: an open, uncontrolled study. | 2003-01-06 |
|
| Severe hepatotoxicity after application of desloratadine and fluconazole. | 2003 |
|
| Desloratadine: an update of its efficacy in the management of allergic disorders. | 2003 |
|
| Chronic urticaria: a role for newer immunomodulatory drugs? | 2003 |
|
| Comparative pharmacology of H1 antihistamines: clinical relevance. | 2002-12-16 |
|
| Treatment of allergic rhinitis. | 2002-12-16 |
|
| The new antihistamines--desloratadine and levocetirizine: a review. | 2002-12 |
|
| [The place of new antihistamines in allergy management. Apropos of desloratadine]. | 2002-12 |
|
| Desloratidine for the treatment of chronic urticaria. | 2002-10 |
|
| Second-generation antihistamines in asthma therapy: is there a protective effect? | 2002 |
|
| Poor sleep and daytime somnolence in allergic rhinitis: significance of nasal congestion. | 2002 |
Patents
Sample Use Guides
Adults and Adolescents 12 Years of Age and Over:
take 5 mg tablet once daily. Children 6 to Years of Age: take 2.5 mg tablet once daily. Children 12 Months to 5 Years of Age: take 1.25 mg tablet once daily. Children 6 to 11 Months of Age: 1 mg tablet once daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7677235
Nasal epithelial cells (activated by 1 uM of histamine) were treated with 10 uM of desloratadine and the inhibitory activity of the drug on expression of ICAM-1 and HLA-DR was studied.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Apr 02 06:53:05 GMT 2025
by
admin
on
Wed Apr 02 06:53:05 GMT 2025
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| Record UNII |
FVF865388R
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| Record Status |
Validated (UNII)
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| Record Version |
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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EMA ASSESSMENT REPORTS |
DESLORATADINE TEVA (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
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LIVERTOX |
NBK548831
Created by
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WHO-VATC |
QR06AX27
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EMA ASSESSMENT REPORTS |
OPULIS (WITHDRAWN: RHINITIS, URTICARIA)
Created by
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NCI_THESAURUS |
C29578
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NDF-RT |
N0000175587
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EMA ASSESSMENT REPORTS |
ALLEX(WITHDRAWN: RHINITIS, ALLERGIC, SEASONAL)
Created by
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EMA ASSESSMENT REPORTS |
DASSELTA (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
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EMA ASSESSMENT REPORTS |
DESLORATADINE RATIOPHARM (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
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EMA ASSESSMENT REPORTS |
DESLORATADINE ACTAVIS (AUTHORIZED: RHINITIS, URTICARIA)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
AZOMYR (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
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WHO-ATC |
R06AX27
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EMA ASSESSMENT REPORTS |
AERINAZE (AUTHORIZED: RHINITIS)
Created by
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EMA ASSESSMENT REPORTS |
AERIUS(AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
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EMA ASSESSMENT REPORTS |
NEOCLARITYN (AUTHORIZED: RHINITIS, URTICARIA)
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NDF-RT |
N0000000190
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CHEMBL1172
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DB00967
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1370280
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C121345
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291342
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7817
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275635
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100000089395
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DTXSID1044196
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Desloratadine
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C47474
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FVF865388R
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FVF865388R
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Desloratadine
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m4193
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
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TRANSPORTER -> INHIBITOR |
Ki
|
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METABOLIC ENZYME -> NON-INHIBITOR |
|
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METABOLIC ENZYME -> NON-INHIBITOR |
|
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|
BINDER->LIGAND |
BINDING
|
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|
|
TARGET -> INHIBITOR |
Desloratadine bound to membranes expressing the recombinant human histamine H1 receptor in Chinese hamster ovary cells (CHO-H1).
Kd
|
||
|
BINDER->LIGAND |
BINDING
|
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|
METABOLIC ENZYME -> NON-INHIBITOR |
|
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|
METABOLIC ENZYME -> SUBSTRATE |
|
||
|
METABOLIC ENZYME -> INHIBITOR |
WEAK
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
|
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|
METABOLIC ENZYME -> SUBSTRATE |
|
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|
|
SALT/SOLVATE -> PARENT |
|
||
|
METABOLIC ENZYME -> INHIBITOR |
WEAK
|
||
|
TARGET -> INHIBITOR |
Kd
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
|
||
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SALT/SOLVATE -> PARENT |
|
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METABOLIC ENZYME -> SUBSTRATE |
|
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> INHIBITOR |
WEAK
|
||
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METABOLIC ENZYME -> SUBSTRATE |
|
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|
METABOLIC ENZYME -> NON-INHIBITOR |
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
METABOLITE -> PARENT |
IN VITRO
|
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METABOLITE -> PARENT |
IN VITRO
|
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PARENT -> METABOLITE ACTIVE |
MAJOR
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METABOLITE -> PARENT |
IN VITRO
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| Related Record | Type | Details | ||
|---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
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|
IMPURITY -> PARENT |
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Tmax | PHARMACOKINETIC |
|
DOSE |
|
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| Biological Half-life | PHARMACOKINETIC |
|
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