Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H18ClN3O5S |
Molecular Weight | 435.881 |
Optical Activity | ( - ) |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C(S1)C(=O)NC[C@H]2CN(C(=O)O2)C3=CC=C(C=C3)N4CCOCC4=O
InChI
InChIKey=KGFYHTZWPPHNLQ-AWEZNQCLSA-N
InChI=1S/C19H18ClN3O5S/c20-16-6-5-15(29-16)18(25)21-9-14-10-23(19(26)28-14)13-3-1-12(2-4-13)22-7-8-27-11-17(22)24/h1-6,14H,7-11H2,(H,21,25)/t14-/m0/s1
Molecular Formula | C19H18ClN3O5S |
Molecular Weight | 435.881 |
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
http://www.biospace.com/News/bayer-healthcares-xarelto-rivaroxaban-becomes/244131
Curator's Comment: description was created based on several sources, including
http://www.biospace.com/News/bayer-healthcares-xarelto-rivaroxaban-becomes/244131
Rivaroxaban (trade name Xarelto) is an oral anticoagulant. It is the first available orally active direct factor Xa inhibitor. Upon oral administration, rivaroxaban selectively binds to both free factor Xa and factor Xa bound in the prothrombinase complex. This interferes with the conversion of prothrombin (factor II) to thrombin and eventually prevents the formation of cross-linked fibrin clots. Rivaroxaban does not affect existing thrombin levels. Activation of factor X to factor Xa (FXa) via the intrinsic and extrinsic pathways plays a central role in the cascade of blood coagulation. Xarelto is indicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, treatment and prophylaxis of deep vein thrombosis (DVT) which may lead to PE in patients undergoing knee or hip replacement surgery, pulmonary embolism (PE) and for the reduction in the risk of recurrence of deep vein thrombosis and of pulmonary embolism following initial 6 months treatment for DVT and/or PE.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23999929
Curator's Comment: Rivaroxaban is distributed heterogeneously to tissues and organs, exhibiting only moderate tissue affinity and does not substantially penetrate the blood-brain barrier.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL244 |
0.4 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | XARELTO Approved UseIndicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, for the treatment of deep vein thrombosis (DVT), pulmonary embolism (PE), and for the reduction in the risk of recurrence of DVT and of PE for the prophylaxis of DVT, which may lead to PE in patients undergoing knee or hip replacement surgery. Launch Date2011 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
138.4 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23999929/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIVAROXABAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.114 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23999929/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIVAROXABAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10.77 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23999929/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIVAROXABAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
9 h |
20 mg 1 times / day unknown, oral dose: 20 mg route of administration: Oral experiment type: UNKNOWN co-administered: |
RIVAROXABAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5% |
20 mg 1 times / day unknown, oral dose: 20 mg route of administration: Oral experiment type: UNKNOWN co-administered: |
RIVAROXABAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
80 mg single, oral Highest studied dose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: Page: p.419 |
healthy, 19-45 n = 6 Health Status: healthy Age Group: 19-45 Sex: M Population Size: 6 Sources: Page: p.419 |
|
50 mg single, oral Studied dose Dose: 50 mg Route: oral Route: single Dose: 50 mg Sources: Page: p.2759, p.2760 |
healthy, 60-76 n = 12 Health Status: healthy Age Group: 60-76 Sex: M+F Population Size: 12 Sources: Page: p.2759, p.2760 |
|
20 mg 1 times / day multiple, oral (max) Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: Page: p.1, p.12 |
unhealthy n = 7111 Health Status: unhealthy Condition: Atrial Fibrillation Sex: M+F Population Size: 7111 Sources: Page: p.1, p.12 |
Disc. AE: Bleeding... AEs leading to discontinuation/dose reduction: Bleeding (grade 3-5, 4.3%) Sources: Page: p.1, p.12 |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: Page: p.1, p.14 |
unhealthy Health Status: unhealthy Condition: Deep Vein Thrombosis|Pulmonary Embolism Sex: M+F Sources: Page: p.1, p.14 |
Disc. AE: Bleeding... AEs leading to discontinuation/dose reduction: Bleeding (2%) Sources: Page: p.1, p.14 |
20 mg 1 times / day multiple, oral (max) Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Atrial Fibrillation|Deep Vein Thrombosis| Sources: Page: p.1 |
Disc. AE: Spinal epidural hematoma... AEs leading to discontinuation/dose reduction: Spinal epidural hematoma Sources: Page: p.1 |
20 mg 2 times / day multiple, oral (max) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1, p.14 |
unhealthy n = 4130 Health Status: unhealthy Condition: Deep Vein Thrombosis|Pulmonary Embolism Sex: M+F Population Size: 4130 Sources: Page: p.1, p.14 |
Disc. AE: Bleeding... AEs leading to discontinuation/dose reduction: Bleeding (1.7%) Sources: Page: p.1, p.14 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Bleeding | grade 3-5, 4.3% Disc. AE |
20 mg 1 times / day multiple, oral (max) Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: Page: p.1, p.12 |
unhealthy n = 7111 Health Status: unhealthy Condition: Atrial Fibrillation Sex: M+F Population Size: 7111 Sources: Page: p.1, p.12 |
Bleeding | 2% Disc. AE |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: Page: p.1, p.14 |
unhealthy Health Status: unhealthy Condition: Deep Vein Thrombosis|Pulmonary Embolism Sex: M+F Sources: Page: p.1, p.14 |
Spinal epidural hematoma | Disc. AE | 20 mg 1 times / day multiple, oral (max) Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Atrial Fibrillation|Deep Vein Thrombosis| Sources: Page: p.1 |
Bleeding | 1.7% Disc. AE |
20 mg 2 times / day multiple, oral (max) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1, p.14 |
unhealthy n = 4130 Health Status: unhealthy Condition: Deep Vein Thrombosis|Pulmonary Embolism Sex: M+F Population Size: 4130 Sources: Page: p.1, p.14 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no | |||
Page: 17.0 |
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 9.0 |
yes | |||
Page: 9.0 |
yes | |||
Page: 9.0 |
yes | yes (co-administration study) Comment: ketoconazole increased cmax of rivaroxaban 0.7x, auc 1.6x Page: 9.0 |
||
Page: 9.0 |
yes | yes (co-administration study) Comment: ketoconazole increased cmax of rivaroxaban 0.7x, auc 1.6x Page: 9.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 248.0 |
PubMed
Title | Date | PubMed |
---|---|---|
New antithrombotics in the prevention of thromboembolic disease. | 2005 Aug |
|
Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct factor Xa inhibitor. | 2005 Oct |
|
Pharmacokinetics of BAY 59-7939--an oral, direct Factor Xa inhibitor--in rats and dogs. | 2005 Sep |
|
Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. | 2005 Sep 22 |
|
Gateways to clinical trials. | 2006 Apr |
|
New oral anticoagulants show promise. | 2006 Feb 15 |
|
[Haemostasis and antithrombotic drugs: pharmacology and novel therapeutic approaches]. | 2006 May |
|
Effect of food, an antacid, and the H2 antagonist ranitidine on the absorption of BAY 59-7939 (rivaroxaban), an oral, direct factor Xa inhibitor, in healthy subjects. | 2006 May |
|
Safety, tolerability, pharmacodynamics, and pharmacokinetics of rivaroxaban--an oral, direct factor Xa inhibitor--are not affected by aspirin. | 2006 Sep |
|
Stroke in atrial fibrillation: update on pathophysiology, new antithrombotic therapies, and evolution of procedures and devices. | 2007 |
|
Investigational treatments of venous thromboembolism. | 2007 Apr |
|
Rivaroxaban (BAY 59-7939)--an oral, direct Factor Xa inhibitor--has no clinically relevant interaction with naproxen. | 2007 Apr |
|
Anithrombotic prevention in vascular disease: bases for a new strategy in antithrombotic therapy. | 2007 Aug 29 |
|
Ultrasound screening for asymptomatic deep vein thrombosis after major orthopaedic surgery: the VENUS study. | 2007 Jul |
|
Treatment of proximal deep-vein thrombosis with the oral direct factor Xa inhibitor rivaroxaban (BAY 59-7939): the ODIXa-DVT (Oral Direct Factor Xa Inhibitor BAY 59-7939 in Patients With Acute Symptomatic Deep-Vein Thrombosis) study. | 2007 Jul 10 |
|
A replacement for warfarin: the search continues. | 2007 Jul 10 |
|
Beyond unfractionated heparin and warfarin: current and future advances. | 2007 Jul 31 |
|
Population model of the pharmacokinetics and pharmacodynamics of rivaroxaban--an oral, direct factor xa inhibitor--in healthy subjects. | 2007 Jun |
|
Rivaroxaban for thromboprophylaxis after orthopaedic surgery: pooled analysis of two studies. | 2007 Jun |
|
Oral, direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases. | 2007 Jun |
|
Rivaroxaban. | 2007 Mar |
|
Effects of the oral, direct factor xa inhibitor rivaroxaban on platelet-induced thrombin generation and prothrombinase activity. | 2007 Nov |
|
Rivaroxaban. A novel, oral, direct factor Xa inhibitor in clinical development for the prevention and treatment of thromboembolic disorders. | 2007 Sep |
|
New issues in oral anticoagulants. | 2008 |
|
Pharmacological strategies for inhibition of thrombin activity. | 2008 |
|
Population pharmacokinetics and pharmacodynamics of rivaroxaban--an oral, direct factor Xa inhibitor--in patients undergoing major orthopaedic surgery. | 2008 |
|
Potent anticoagulants are associated with a higher all-cause mortality rate after hip and knee arthroplasty. | 2008 Aug |
|
[Perioperative venous thromboembolism prophylaxis: short review and recommendations]. | 2008 Dec |
|
The laboratory diagnosis and clinical management of patients with heparin-induced thrombocytopenia: an update. | 2008 Feb |
|
Current and future prospects for anticoagulant therapy: inhibitors of factor Xa and factor IIa. | 2008 Feb |
|
New oral anticoagulants in atrial fibrillation. | 2008 Jan |
|
Gateways to clinical trials. | 2008 Jan-Feb |
|
Extended duration rivaroxaban versus short-term enoxaparin for the prevention of venous thromboembolism after total hip arthroplasty: a double-blind, randomised controlled trial. | 2008 Jul 5 |
|
New anticoagulants--the path from discovery to clinical practice. | 2008 Jun 26 |
|
Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty. | 2008 Jun 26 |
|
New anticoagulants for treatment of venous thromboembolism. | 2008 Mar |
|
[Rivaroxaban. The first factor Xa inhibitor]. | 2008 Nov |
|
Rivaroxaban for thromboprophylaxis. | 2008 Nov 13 |
|
Rivaroxaban for thromboprophylaxis. | 2008 Nov 13 |
|
Orally administered factor xa inhibitor, rivaroxaban: a novel thromboembolic prophylaxis agent. | 2008 Oct |
|
[Always more amputations in Germany?]. | 2008 Oct |
|
Polyphosphate as a general procoagulant agent. | 2008 Oct |
|
Determination of rivaroxaban--a novel, oral, direct Factor Xa inhibitor--in human plasma by high-performance liquid chromatography-tandem mass spectrometry. | 2008 Sep 1 |
Sample Use Guides
15 mg and 20 mg tablets with food; take 10 mg tablets with or without food. For patients with CrCl >50 mL/min 20 mg orally, once daily and for patients with CrCl 15 - 50 mL/min 15 mg orally, once daily with the evening meal.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=23578206
To evaluate the influence of prothrombin complex concentrate (PCC) on the anticoagulant effects of rivaroxaban as measured by prothrombin time (PT) and thrombin generation tests plasma and whole blood samples from healthy volunteers were spiked with Rivaroxaban (up to 800 ug/L) and prothrombin complex concentrate (PCC) was added to these samples in concentration ranges as used clinically to reverse the effects of vitamin K antagonists. Prothrombin complex concentrate does not neutralize the
lengthening effect on PT and TGT lag time/T-Lag of rivaroxaban anticoagulated blood in vitro; however, total thrombin potential could be normalized.
Substance Class |
Chemical
Created
by
admin
on
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Fri Dec 15 15:52:28 GMT 2023
by
admin
on
Fri Dec 15 15:52:28 GMT 2023
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Record UNII |
9NDF7JZ4M3
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Record Status |
Validated (UNII)
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Record Version |
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EMA ASSESSMENT REPORTS |
XARELTO (AUTHORIZED: ARTHROPLASTY, REPLACEMENT)
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NCI_THESAURUS |
C263
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WHO-ATC |
B01AF01
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NDF-RT |
N0000175637
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EMA ASSESSMENT REPORTS |
XARELTO (AUTHORIZED: VENOUS THROMBOEMBOLISM)
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WHO-ATC |
B01AX06
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WHO-VATC |
QB01AF01
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LIVERTOX |
NBK548015
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LOINC |
74871-5
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C77995
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9NDF7JZ4M3
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RIVAROXABAN
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1114195
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Rivaroxaban
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SUB29263
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
COMPETITIVE INHIBITOR
IC50
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TARGET -> INHIBITOR |
COMPETITIVE INHIBITOR
Ki
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE |
Related Record | Type | Details | ||
---|---|---|---|---|
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METABOLITE -> PARENT |
MINOR
FECAL; URINE
|
||
|
METABOLITE -> PARENT |
IN-VITRO
FECAL; URINE
|
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METABOLITE -> PARENT |
MINOR
FECAL; URINE
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
excreta 2.5% radio acitivty
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||
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METABOLITE -> PARENT |
IN-VIVO
FECAL; URINE
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METABOLITE -> PARENT |
Related Record | Type | Details | ||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
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||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
|
||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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