Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H21FN6O5 |
Molecular Weight | 444.4163 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)C(O)=C(N=C1C(C)(C)NC(=O)C2=NN=C(C)O2)C(=O)NCC3=CC=C(F)C=C3
InChI
InChIKey=CZFFBEXEKNGXKS-UHFFFAOYSA-N
InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30)
Molecular Formula | C20H21FN6O5 |
Molecular Weight | 444.4163 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Raltegravir (RAL, Isentress, formerly MK-0518) is an antiretroviral drug produced by Merck & Co., used to treat HIV and it is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 4 weeks of age and older. Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required r viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. The provirus is required to direct the production of progeny virus, so inhibiting integration prevents propagation of the viral infection. Raltegravir did not significantly inhibit human phosphoryl transferases including DNA polymerases α, β, and γ. Coadministration with others drugs that are strong inducers of UGT1A1, such as rifampin, may result in reduced plasma concentrations of raltegravir. The most common adverse reactions of moderate to severe intensity (≥2%) are insomnia, headache, dizziness, nausea and fatigue. Severe, potentially life-threatening, and fatal skin reactions have been reported. This include cases of Stevens-Johnson syndrome and toxic epidermal necrolysis. Hypersensitivity reactions have also been reported and were characterized by rash, constitutional findings, and sometimes, organ dysfunction, including hepatic failure. The major mechanism of clearance of raltegravir in humans is UGT1A1-mediated glucuronidation.
CNS Activity
Originator
Sources: https://www.google.com/patents/WO2006060712A2?cl=en
Curator's Comment: Merck & Co. Inc., Istituto Di Ricerche Di Biologia Molecolar # Merck & Co. Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3471 Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=24793360 |
10.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ISENTRESS Approved UseINDICATIONS & USAGE ISENTRESS is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) indicated: In combination with other antiretroviral agents for the treatment of HIV-1 infection (1). The safety and efficacy of ISENTRESS have not been established in children less than 2 years of age (1.2). ISENTRESS® is indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection. This indication is based on analyses of plasma HIV-1 RNA levels in three double-blind controlled studies of ISENTRESS. Two of these studies were conducted in clinically advanced, 3-class antiretroviral (NNRTI, NRTI, PI) treatment-experienced adults through 96 weeks and one was conducted in treatment-naïve adults through 156 weeks. The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response [see Clinical Studies (14) Launch Date1.19214716E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
142 nM |
400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RALTEGRAVIR plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1300 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01785160 |
400 mg 2 times / day steady, oral dose: 400 mg route of administration: oral experiment type: steady co-administered: |
RALTEGRAVIR plasma | Homo sapiens |
|
20163 nM Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03667547 |
1200 mg single, oral dose: 1200 mg route of administration: oral experiment type: single co-administered: |
RALTEGRAVIR plasma | Homo sapiens population: healthy age: sex: M food status: Fasted |
|
830.204 ng/ml Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03537404 |
400 mg 2 times / day steady, oral dose: 400 mg route of administration: oral experiment type: steady co-administered: |
RALTEGRAVIR unknown | Homo sapiens |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
14.3 μM × h |
400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RALTEGRAVIR plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4070 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01785160 |
400 mg 2 times / day steady, oral dose: 400 mg route of administration: oral experiment type: steady co-administered: |
RALTEGRAVIR plasma | Homo sapiens |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9 h |
400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RALTEGRAVIR plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7.5 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03667547 |
1200 mg single, oral dose: 1200 mg route of administration: oral experiment type: single co-administered: |
RALTEGRAVIR plasma | Homo sapiens population: healthy age: sex: M food status: Fasted |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17% |
400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RALTEGRAVIR plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
800 mg single, oral Highest studied dose Dose: 800 mg Route: oral Route: single Dose: 800 mg Sources: Page: p.123 |
healthy, 29 +/- 13 n = 12 Health Status: healthy Age Group: 29 +/- 13 Sex: M+F Population Size: 12 Sources: Page: p.123 |
|
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.123 |
healthy, 29 +/- 13 n = 12 Health Status: healthy Age Group: 29 +/- 13 Sex: M+F Population Size: 12 Sources: Page: p.123 |
|
24000 mg single, oral Overdose Dose: 24000 mg Route: oral Route: single Dose: 24000 mg Sources: Page: p.1 |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: HIV-1 infection Age Group: 42 Sex: M Population Size: 1 Sources: Page: p.1 |
Disc. AE: Nausea, Abdominal pain... AEs leading to discontinuation/dose reduction: Nausea (mild) Sources: Page: p.1Abdominal pain |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.1 |
Disc. AE: Reaction skin, Stevens-Johnson syndrome... AEs leading to discontinuation/dose reduction: Reaction skin (severe|grade 4|grade 5) Sources: Page: p.1Stevens-Johnson syndrome (severe|grade 4|grade 5) Hypersensitivity reaction (severe|grade 4|grade 5) Toxic epidermal necrolysis (severe|grade 4|grade 5) Immune reconstitution syndrome |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Abdominal pain | Disc. AE | 24000 mg single, oral Overdose Dose: 24000 mg Route: oral Route: single Dose: 24000 mg Sources: Page: p.1 |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: HIV-1 infection Age Group: 42 Sex: M Population Size: 1 Sources: Page: p.1 |
Nausea | mild Disc. AE |
24000 mg single, oral Overdose Dose: 24000 mg Route: oral Route: single Dose: 24000 mg Sources: Page: p.1 |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: HIV-1 infection Age Group: 42 Sex: M Population Size: 1 Sources: Page: p.1 |
Immune reconstitution syndrome | Disc. AE | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.1 |
Hypersensitivity reaction | severe|grade 4|grade 5 Disc. AE |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.1 |
Reaction skin | severe|grade 4|grade 5 Disc. AE |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.1 |
Stevens-Johnson syndrome | severe|grade 4|grade 5 Disc. AE |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.1 |
Toxic epidermal necrolysis | severe|grade 4|grade 5 Disc. AE |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.1 |
PubMed
Title | Date | PubMed |
---|---|---|
Raltegravir susceptibility and fitness progression of HIV type-1 integrase in patients on long-term antiretroviral therapy. | 2008 |
|
HIV infection in the elderly. | 2008 |
|
"One pill, once daily": what clinicians need to know about Atriplatrade mark. | 2008 Apr |
|
Raltegravir: first in class HIV integrase inhibitor. | 2008 Apr |
|
HIV-1 drug resistance mutations: an updated framework for the second decade of HAART. | 2008 Apr-Jun |
|
Highlights of the 15th Conference on Retroviruses and Opportunistic Infections. Advances in antiretroviral therapy. | 2008 Apr-May |
|
A conventional LC-MS method developed for the determination of plasma raltegravir concentrations. | 2008 Aug |
|
Raltegravir, an HIV-1 integrase inhibitor for HIV infection. | 2008 Aug |
|
Raltegravir: the first in a new class of integrase inhibitors for the treatment of HIV. | 2008 Aug |
|
Antiretroviral treatment of adult HIV infection: 2008 recommendations of the International AIDS Society-USA panel. | 2008 Aug 6 |
|
Natural variation of HIV-1 group M integrase: implications for a new class of antiretroviral inhibitors. | 2008 Aug 7 |
|
An HPLC-PDA method for the simultaneous quantification of the HIV integrase inhibitor raltegravir, the new nonnucleoside reverse transcriptase inhibitor etravirine, and 11 other antiretroviral agents in the plasma of HIV-infected patients. | 2008 Dec |
|
Integrase and integration: biochemical activities of HIV-1 integrase. | 2008 Dec 17 |
|
Integrase inhibitors for the treatment of HIV infection. | 2008 Jul |
|
How developing world concerns need to be part of drug development plans: a case study of four emerging antiretrovirals. | 2008 Jul |
|
Genetic diversity of integrase (IN) sequences in antiretroviral treatment-naive and treatment-experienced HIV type 2 patients. | 2008 Jul |
|
Atazanavir modestly increases plasma levels of raltegravir in healthy subjects. | 2008 Jul 1 |
|
Ensemble-based virtual screening reveals potential novel antiviral compounds for avian influenza neuraminidase. | 2008 Jul 10 |
|
Severe rhabdomyolysis associated with raltegravir use. | 2008 Jul 11 |
|
Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. | 2008 Jul 24 |
|
Integrase inhibitors: a clinical review of raltegravir and elvitegravir. | 2008 Jun |
|
Trial will evaluate a once-daily dose of raltegravir. | 2008 Nov |
|
Raltegravir phase III study data released. | 2008 Nov |
|
Pharmacologic aspects of new antiretroviral drugs. | 2008 Nov |
|
HIV-2 integrase gene polymorphism and phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitors raltegravir and elvitegravir in vitro. | 2008 Nov |
|
Adverse cutaneous reactions associated with the newest antiretroviral drugs in patients with human immunodeficiency virus infection. | 2008 Nov |
|
Elevated alkaline phosphatase with raltegravir in a treatment experienced HIV patient. | 2008 Nov 12 |
|
An accurate and precise high-performance liquid chromatography method for the rapid quantification of the novel HIV integrase inhibitor raltegravir in human blood plasma after solid phase extraction. | 2008 Nov 3 |
|
Raltegravir for postexposure prophylaxis following occupational exposure to HIV. | 2008 Nov 30 |
|
Raltegravir: the first HIV integrase inhibitor. | 2008 Oct |
|
[New CCR5 inhibitor antiretroviral drugs and integrase inhibitors]. | 2008 Oct |
|
Drug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapy. | 2008 Oct |
|
Discovery of 3-acetyl-4-hydroxy-2-pyranone derivatives and their difluoridoborate complexes as a novel class of HIV-1 integrase inhibitors. | 2008 Oct 1 |
|
Selection of the Q148R integrase inhibitor resistance mutation in a failing raltegravir containing regimen. | 2008 Oct 1 |
|
Emerging resistance profiles of newly approved antiretroviral drugs. | 2008 Oct-Nov |
|
A survey of the syntheses of active pharmaceutical ingredients for antiretroviral drug combinations critical to access in emerging nations. | 2008 Sep |
|
Clade-specific HIV-1 integrase polymorphisms do not reduce raltegravir and elvitegravir phenotypic susceptibility. | 2008 Sep 12 |
|
Exacerbation of depression associated with starting raltegravir: a report of four cases. | 2008 Sep 12 |
|
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. | 2008 Sep 25 |
|
Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants. | 2008 Sep 9 |
|
Comparing two integrase inhibitors. The first head-to-head study comparing raltegravir and elvitegravir. | 2008 Sep-Oct |
|
Emerging pharmacology: inhibitors of human immunodeficiency virus integration. | 2009 |
|
Quantitative prediction of human clearance guiding the development of Raltegravir (MK-0518, isentress) and related HIV integrase inhibitors. | 2009 Apr |
|
Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. | 2009 Apr |
|
Pharmacologic aspects of new antiretroviral drugs. | 2009 Feb |
|
Is dual therapy with raltegravir and protease inhibitors a feasible option in rescue strategy in HIV-1 infection? | 2009 Feb 1 |
|
Effects of omeprazole on plasma levels of raltegravir. | 2009 Feb 15 |
|
Quantification of the HIV-integrase inhibitor raltegravir and detection of its main metabolite in human plasma, dried blood spots and peripheral blood mononuclear cell lysate by means of high-performance liquid chromatography tandem mass spectrometry. | 2009 Feb 20 |
|
Implications of HIV-1 M group polymorphisms on integrase inhibitor efficacy and resistance: genetic and structural in silico analyses. | 2009 Jan 13 |
|
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. | 2009 Mar |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022145s035,203045s012,205786s003lbl.pdf
Curator's Comment: in Children and Adolescents: If at least 25 kg: One 400 mg film-coated tablet orally, twice daily. For patients weighing between 11 and 20 kg, either the
chewable tablet or the formulation for oral suspension can be used.
400 mg film-coated tablet orally, twice daily. During coadministration with rifampin in adults, 800 mg twice daily
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25629256
The antiviral activity of Raltegravir was determined in a cell-based HIV-1 replication assay with HeLa-CD4-LTR-β-gal cells. The highest compound concentration tested was 50 μM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 16 19:02:53 UTC 2022
by
admin
on
Fri Dec 16 19:02:53 UTC 2022
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Record UNII |
22VKV8053U
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C281
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WHO-ATC |
J05AX08
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NDF-RT |
N0000175887
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WHO-ATC |
J05AR16
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EMA ASSESSMENT REPORTS |
ISENTRESS (AUHTORIZED: HIV INFECTIONS)
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LIVERTOX |
NBK548313
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WHO-VATC |
QJ05AX08
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NDF-RT |
N0000000127
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SUB25667
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518048-05-0
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54671008
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C72837
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82960
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22VKV8053U
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C507898
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2352
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8124
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Raltegravir
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M9486
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TT-71
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DB06817
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CHEMBL254316
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RALTEGRAVIR
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22VKV8053U
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719872
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PRIMARY | RxNorm |
Related Record | Type | Details | ||
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EXCRETED UNCHANGED |
Following administration of a single dose of 200 mg [14 C] raltegravir to young healthy subjects (Protocol 011), approximately 83.0% of the radioactivity dose was recovered, with 51.1% in feces and 31.8% in-urine over a 10-day period.
AMOUNT EXCRETED
URINE
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TARGET ORGANISM->INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE | |||
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LABELED -> NON-LABELED |
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TARGET -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT |
MAJOR
FECAL; URINE
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
This is a process impurity controlled in the drug substance and not monitored in the drug product [USP]
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IMPURITY -> PARENT |
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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Biological Half-life | PHARMACOKINETIC |
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Elimination PHARMACOKINETIC |
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