Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H21NO2 |
Molecular Weight | 259.3434 |
Optical Activity | ( - ) |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC(=O)NCC[C@@H]1CCC2=CC=C3OCCC3=C12
InChI
InChIKey=YLXDSYKOBKBWJQ-LBPRGKRZSA-N
InChI=1S/C16H21NO2/c1-2-15(18)17-9-7-12-4-3-11-5-6-14-13(16(11)12)8-10-19-14/h5-6,12H,2-4,7-10H2,1H3,(H,17,18)/t12-/m0/s1
Molecular Formula | C16H21NO2 |
Molecular Weight | 259.3434 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.takeda.com/news/2011/20111007_3902.html
Curator's Comment: description was created based on several sources, including
https://www.takeda.com/news/2011/20111007_3902.html
Ramelteon was approved by the United States (U.S.) in July 2005, and the Japanese Ministry of Health, Labour and Welfare in April 2010. It is currently available in the USA and Japan as ROZEREM and is indicated for the treatment of insomnia characterized by difficulty with sleep onset. In October 7, 2011, Takeda has decided to discontinue the development of ramelteon in Europe for the treatment of insomnia in order to best optimize Takeda’s resources for its research and development activities. Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor. Ramelteon demonstrates full agonist activity in vitro in cells expressing human MT1 or MT2 receptors, and high selectivity for human MT1 and MT2 receptors compared to the MT3 receptor. The activity of ramelteon at the MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties since these receptors are acted upon by endogenous melatonin and are thought to be involved in the maintenance of the circadian rhythm underlying normal sleep-wake cycles. Ramelteon has no appreciable affinity for the GABA receptor complex or for receptors that bind neuropeptides, cytokines, serotonin, dopamine, noradrenaline, acetylcholine, and opiates.
Originator
Sources: https://www.takeda.com/news/2011/20111007_3902.html
Curator's Comment: # Takeda
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094268 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15494157 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ROZEREM Approved UseROZEREM is indicated for the treatment of insomnia characterized by difficulty with sleep onset. The clinical trials performed in support of efficacy were up to 6 months in duration. The final formal assessments of sleep latency were performed after 2 days of treatment during the crossover study (elderly only), at 5 weeks in the 6-week studies (adults and elderly), and at the end of the 6-month study (adults and elderly) [see Clinical Studies (14) Launch Date1.12199034E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
25.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432265 |
64 mg single, oral dose: 64 mg route of administration: Oral experiment type: SINGLE co-administered: |
RAMELTEON serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
36.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432265 |
64 mg single, oral dose: 64 mg route of administration: Oral experiment type: SINGLE co-administered: |
RAMELTEON serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432265 |
64 mg single, oral dose: 64 mg route of administration: Oral experiment type: SINGLE co-administered: |
RAMELTEON serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432265 |
64 mg single, oral dose: 64 mg route of administration: Oral experiment type: SINGLE co-administered: |
RAMELTEON serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
32 mg 1 times / day multiple, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: multiple Dose: 32 mg, 1 times / day Sources: |
unhealthy, 42.8 years n = 63 Health Status: unhealthy Condition: chronic primary insomnia Age Group: 42.8 years Sex: M+F Population Size: 63 Sources: |
Other AEs: Somnolence, Malaise... Other AEs: Somnolence (12.7%) Sources: Malaise (1.6%) Dizziness (3.2%) Nasopharyngitis (4.8%) |
40 mg 1 times / day multiple, oral Overdose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, 47 years n = 1 Health Status: unhealthy Condition: insomnia Age Group: 47 years Sex: F Population Size: 1 Sources: |
|
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Disc. AE: Somnolence, Dizziness... AEs leading to discontinuation/dose reduction: Somnolence (0.8%) Sources: Dizziness (0.5%) Nausea (0.3%) Fatigue (0.3%) Headache (0.3%) Insomnia (0.3%) |
160 mg single, oral Highest studied dose Dose: 160 mg Route: oral Route: single Dose: 160 mg Sources: |
unknown Health Status: unknown Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Malaise | 1.6% | 32 mg 1 times / day multiple, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: multiple Dose: 32 mg, 1 times / day Sources: |
unhealthy, 42.8 years n = 63 Health Status: unhealthy Condition: chronic primary insomnia Age Group: 42.8 years Sex: M+F Population Size: 63 Sources: |
Somnolence | 12.7% | 32 mg 1 times / day multiple, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: multiple Dose: 32 mg, 1 times / day Sources: |
unhealthy, 42.8 years n = 63 Health Status: unhealthy Condition: chronic primary insomnia Age Group: 42.8 years Sex: M+F Population Size: 63 Sources: |
Dizziness | 3.2% | 32 mg 1 times / day multiple, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: multiple Dose: 32 mg, 1 times / day Sources: |
unhealthy, 42.8 years n = 63 Health Status: unhealthy Condition: chronic primary insomnia Age Group: 42.8 years Sex: M+F Population Size: 63 Sources: |
Nasopharyngitis | 4.8% | 32 mg 1 times / day multiple, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: multiple Dose: 32 mg, 1 times / day Sources: |
unhealthy, 42.8 years n = 63 Health Status: unhealthy Condition: chronic primary insomnia Age Group: 42.8 years Sex: M+F Population Size: 63 Sources: |
Fatigue | 0.3% Disc. AE |
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Headache | 0.3% Disc. AE |
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Insomnia | 0.3% Disc. AE |
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Nausea | 0.3% Disc. AE |
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Dizziness | 0.5% Disc. AE |
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Somnolence | 0.8% Disc. AE |
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 3594 Health Status: unhealthy Condition: insomnia Age Group: adult Population Size: 3594 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 60.0 |
inconclusive | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 11, 13 |
major | yes (co-administration study) Comment: fluvoxamine increased ramelteon AUC 190-fold and Cmax 70-fold; rifampin decreased total expsoure to ramelteon by 80% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 11, 13 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 11, 13 |
minor | yes (co-administration study) Comment: rifampin decreased total expsoure to ramelteon by 80% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 11, 13 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 11, 13 |
minor | yes (co-administration study) Comment: ketaconazole increased ramelteon AUC by 84% and Cmax 36%; rifampin decreased total expsoure to ramelteon by 80% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 11, 13 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 13.0 |
yes | yes (co-administration study) Comment: fluconazole increased AUC by 150% and Cmax by 150%; rifampin decreased total expsoure to ramelteon by 80% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_biopharmr.pdf Page: 13.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021782s000_Rozerem_pharmr_CORRECTED_REVIEW.pdf Page: 53, 66 |
PubMed
Title | Date | PubMed |
---|---|---|
Gateways to clinical trials. | 2004 Dec |
|
Gateways to clinical trials. | 2004 Nov |
|
The sleep-promoting action of ramelteon (TAK-375) in freely moving cats. | 2004 Nov 1 |
|
Ramelteon: TAK 375. | 2005 |
|
Gateways to clinical trials. | 2005 Apr |
|
Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. | 2005 Feb |
|
Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats. | 2005 Feb |
|
TAK-375 Takeda. | 2005 Jan |
|
Fresh from the pipeline: Ramelteon. | 2005 Nov |
|
Ramelteon (Rozerem) for insomnia. | 2005 Nov 7 |
|
Gateways to clinical trials. | 2005 Oct |
|
New drugs and dosage forms. | 2005 Sep 15 |
|
Depression and sleep: pathophysiology and treatment. | 2006 |
|
Use of sleep-promoting medications in nursing home residents : risks versus benefits. | 2006 |
|
Practical considerations of new drugs: new choices for old problems. | 2006 Apr |
|
Ramelteon (rozerem) a novel approach for insomnia treatment. | 2006 Apr |
|
Consultation corner. Are the new sleep aids right for you? | 2006 Apr |
|
New drugs 06, part II. | 2006 Aug |
|
Treating insomnia: Current and investigational pharmacological approaches. | 2006 Dec |
|
An efficacy, safety, and dose-response study of Ramelteon in patients with chronic primary insomnia. | 2006 Jan |
|
New drugs: ramelteon, tipranavir, nepafenac, and deferasirox. | 2006 Jan-Feb |
|
Searching for new options for treating insomnia: are melatonin and ramelteon beneficial? | 2006 Jul |
|
Ramelteon: a novel treatment for the treatment of insomnia. | 2006 Jul |
|
Effect of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist, on motor performance in mice. | 2006 Jul 24 |
|
Gateways to clinical trials. | 2006 Jul-Aug |
|
Management of chronic insomnia in elderly persons. | 2006 Jun |
|
Acute and chronic effects of ramelteon in rhesus monkeys (Macaca mulatta): dependence liability studies. | 2006 Jun |
|
Effects of ramelteon on patient-reported sleep latency in older adults with chronic insomnia. | 2006 Jun |
|
Treatment of sleep dysfunction and psychiatric disorders. | 2006 Sep |
|
[Recent and potential drugs for treatment of insomnia]. | 2007 Jan |
|
Therapeutic options for sleep-maintenance and sleep-onset insomnia. | 2007 Jan |
|
[New hypnotics: perspectives from sleep physiology]. | 2007 Jul-Aug |
|
The management of insomnia in the older adult. | 2007 Jun |
|
In search of novel and therapeutically significant melatoninergic ligands. | 2007 Nov |
|
Gateways to clinical trials. | 2007 Oct |
|
Melatonin therapy to improve nocturnal sleep in critically ill patients: encouraging results from a small randomised controlled trial. | 2008 |
|
Melatonergic drugs in clinical practice. | 2008 |
|
Efficacy and clinical safety of ramelteon: an evidence-based review. | 2008 Aug |
|
Jet lag: therapeutic use of melatonin and possible application of melatonin analogs. | 2008 Jan-Mar |
|
Ramelteon: a melatonin receptor agonist for the treatment of insomnia. | 2008 Jan-Mar |
|
Stimulatory effects of a melatonin receptor agonist, ramelteon, on BDNF in mouse cerebellar granule cells. | 2008 Jul 4 |
|
Melatonin and its agonists: an update. | 2008 Oct |
|
Circadian phase-shifting effects of repeated ramelteon administration in healthy adults. | 2008 Oct 15 |
|
Possibility that certain hypnotics might cause cancer in skin. | 2008 Sep |
|
Ramelteon: a novel approach in the treatment of insomnia. | 2008 Sep |
|
Acute sleep-promoting action of the melatonin agonist, ramelteon, in the rat. | 2008 Sep |
|
Melatonin receptor agonist ramelteon activates the extracellular signal-regulated kinase 1/2 in mouse cerebellar granule cells. | 2008 Sep 9 |
|
The effect of melatonergic and non-melatonergic antidepressants on sleep: weighing the alternatives. | 2009 |
|
The effects of ramelteon in a first-night model of transient insomnia. | 2009 Jan |
|
The effects of ramelteon on respiration during sleep in subjects with moderate to severe chronic obstructive pulmonary disease. | 2009 Mar |
Patents
Sample Use Guides
The recommended dose 8 mg taken within 30 minutes of going to bed. It is recommended that drug not be taken with or immediately after a high fat meal.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15695169
Curator's Comment: Ramelteon inhibited forskolin-stimulated cAMP production in the CHO cells that express the human MT1 or MT2 receptors.
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:28:50 UTC 2023
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on
Wed Jul 05 23:28:50 UTC 2023
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Record UNII |
901AS54I69
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Record Status |
Validated (UNII)
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WHO-ATC |
N05CH02
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LIVERTOX |
NBK548437
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N0000000250
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QN05CH02
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N0000175743
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NCI_THESAURUS |
C47795
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100000085617
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Ramelteon
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RAMELTEON
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901AS54I69
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196597-26-9
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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EXCRETED UNCHANGED |
FECAL; URINE
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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TARGET -> AGONIST |
AGONIST
Ki
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TARGET -> AGONIST |
HUMAN RECEPTOR IN CHO CELLS
Ki
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BINDER->LIGAND |
independent of concentration
BINDING
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METABOLIC ENZYME -> SUBSTRATE |
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Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT | |||
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METABOLITE INACTIVE -> PARENT | |||
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METABOLITE ACTIVE -> PARENT |
metabolite M-II, has a longer half-life and greater systemic exposure than ramelteon. Hence, M-II may contribute significantly to the hypnotic benefits of ramelteon. S-ISOMER represents 94% of M-II.
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT | |||
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METABOLITE INACTIVE -> PARENT | |||
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METABOLITE ACTIVE -> PARENT |
major isozyme metabolizes to S-isomer
MAJOR
PLASMA
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METABOLITE -> PARENT | |||
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METABOLITE ACTIVE -> PARENT |
minor isozyme
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Elimination PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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FASTED ORAL ADMINISTRATION |
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ORAL BIOAVAILABILITY | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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