Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C17H14BrN3O2S |
| Molecular Weight | 404.281 |
| Optical Activity | ( + / - ) |
| Additional Stereochemistry | Yes |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
| Stereo Comments | AXIAL, RACEMIC |
SHOW SMILES / InChI
SMILES
OC(=O)CSC1=NN=C(Br)N1C2=C3C=CC=CC3=C(C=C2)C4CC4
InChI
InChIKey=FGQFOYHRJSUHMR-UHFFFAOYSA-N
InChI=1S/C17H14BrN3O2S/c18-16-19-20-17(24-9-15(22)23)21(16)14-8-7-11(10-5-6-10)12-3-1-2-4-13(12)14/h1-4,7-8,10H,5-6,9H2,(H,22,23)
| Molecular Formula | C17H14BrN3O2S |
| Molecular Weight | 404.281 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Lesinurad (brand name Zurampic) is a urate transporter inhibitor for treating hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone. In gout patients, Lesinurad lowered serum uric acid levels and increased renal clearance and fractional excretion of uric acid. Following single and multiple oral doses of Lesinurad to gout patients, dose-dependent decreases in serum uric acid levels and increases in urinary uric acid excretion were observed. Lesinurad reduces serum uric acid levels by inhibiting the function of transporter proteins involved in uric acid reabsorption in the kidney. Lesinurad inhibited the function of two apical transporters responsible for uric acid reabsorption, uric acid transporter 1 (URAT1) and organic anion transporter 4 (OAT4), with IC50 values of 7.3 and 3.7 µM, respectively. URAT1 is responsible for the majority of the reabsorption of filtered uric acid from the renal tubular lumen. OAT4 is a uric acid transporter associated with diuretic-induced hyperuricemia. Lesinurad does not interact with the uric acid reabsorption transporter SLC2A9 (Glut9), located on the basolateral membrane of the proximal tubule cell. Based on in vitro studies, lesinurad is an inhibitor of OATP1B1, OCT1, OAT1, and OAT3; however, lesinurad is not an in vivo inhibitor of these transporters. In vivo drug interaction studies indicate that lesinurad does not decrease the renal clearance of furosemide (substrate of OAT1/3), or affect the exposure of atorvastatin (substrate of OATP1B1) or metformin (substrate of OCT1). Based on in vitro studies, lesinurad has no relevant effect on P-glycoprotein.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL6120 |
7.3 µM [IC50] | ||
Target ID: CHEMBL2073677 |
3.7 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Secondary | ZURAMPIC Approved UseINDICATIONS AND USAGE. ZURAMPIC is a URAT1 inhibitor indicated in combination with a xanthine oxidase inhibitor for the treatment of hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone Launch Date2015 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.303 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.21 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
22 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.02 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.74 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
7.68 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.54 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.51 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
11.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.7 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.7 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
23.1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
21.9 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5.54 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.787 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
106 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
12.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
14.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
17.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
28.7 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.12 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
30.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
31.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
33.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
56.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
70.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
89.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
29.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.73 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
34.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
8.04 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
10.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
12.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.72 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.99 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
8.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
5.97 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
8.91 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5.19 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
8.91 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
7.48 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.77 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26170627/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
LESINURAD plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| minor [IC50 43.1 uM] | ||||
| no | ||||
| no | ||||
| no | ||||
| weak | likely (co-administration study) Comment: Concomitant use with lesinurad reduced the plasma concentration of sensitive CYP3A4 substrates (e.g., Sildenafil, Amlodipine), and possibly reduce the efficacy of sensitive CYP3A4 substrates Page: 12.0 |
|||
| yes [IC50 13.7 uM] | no (co-administration study) Comment: does not affect exposure of metformin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207988Orig1s000ClinPharmR.pdf#page=44 Page: 44.0 |
|||
| yes [IC50 148 uM] | ||||
| yes [IC50 16.2 uM] | weak (co-administration study) Comment: Coadministration with repaglinide: small increase in AUC (10-31%) Page: 74.0 |
|||
| yes [IC50 3.5 uM] | ||||
| yes [IC50 3.5 uM] | no (co-administration study) Comment: does not affect renal clearance of furosemide Page: 11.0 |
|||
| yes [IC50 384 uM] | ||||
| yes [IC50 4.3 uM] | no (co-administration study) Comment: does not affect renal clearance of furosemide Page: 11.0 |
|||
| yes [IC50 40.7 uM] | weak (co-administration study) Comment: Coadministration with tolbutamide: small increase in AUC (11%); Coadministration with OH-tolbutamide: small increase in AUC (14%) Page: 74.0 |
|||
| yes [IC50 9.3 uM] | ||||
| yes [IC50 >100 uM] | ||||
| yes [IC50 >100 uM] | ||||
| yes [IC50 >100 uM] | ||||
| yes [IC50 >300 uM] | ||||
| yes [IC50 >3000 uM] | ||||
| yes [Inhibition 100 uM] | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| major | ||||
| major | ||||
| minor | ||||
| minor | ||||
| minor | ||||
| no evidence | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | yes (co-administration study) Comment: Lesinurad exposure is increased by 56% when lesinurad is co-administered with fluconazole, an inhibitor of CYP2C9 Page: 70.0 |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Sample Use Guides
ZURAMPIC (Lesinurad ) is recommended at 200 mg once daily in combination with a xanthine oxidase inhibitor, including allopurinol or febuxostat. The maximum daily dose of ZURAMPIC is 200 mg.
Route of Administration:
Oral
OAT1 was expressed in Flp-In 293 cells. [14C]RDEA594 was incubated with cells for 5 minutes at 37C. The reaction was stopped with ice-cold transport medium and cells were lysed with 0.2 ml of 1 N NAOH and radioactivity was measured using liquid scintillation counting. There was saturable uptake of [14C]RDEA594 into oocytes expressing OAT1. The Km was 0.85 μM and Vmax was 13.0 pmol/min/mg protein
| Substance Class |
Chemical
Created
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on
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Fri Dec 15 19:16:11 GMT 2023
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| Record UNII |
09ERP08I3W
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| Record Status |
Validated (UNII)
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M04AB05
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NDF-RT |
N0000192341
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C175109
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1731031
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CHEMBL2105720
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m11920
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90929
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Lesinurad
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SUB93370
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N0000190118
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PRIMARY | Cytochrome P450 3A Inducers [MoA] | ||
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WW-158
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N0000192340
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PRIMARY | Urate Transporter 1 Inhibitors [MoA] | ||
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53465279
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TRANSPORTER -> INHIBITOR |
Based on in vitro studies, lesinurad is a weak inhibitor of OATP1B1, OCT1, OAT1, and OAT3.
WEAK
|
||
|
TRANSPORTER -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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||
|
METABOLIC ENZYME -> INDUCER |
WEAK
|
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|
TRANSPORTER -> INHIBITOR |
Based on in vitro studies, lesinurad is a weak inhibitor of OATP1B1, OCT1, OAT1, and OAT3.
WEAK
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|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
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||
|
|
SALT/SOLVATE -> PARENT | |||
|
|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
|
||
|
TRANSPORTER -> SUBSTRATE |
Based on in vitro studies, lesinurad is a substrate of OAT1 and OAT3.
|
||
|
|
TRANSPORTER -> INHIBITOR |
IC50
|
||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
FECAL
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
|
||
|
TARGET -> INHIBITOR |
inhibits the transport of [14C]uric acid into human embryonic kidney-293 cells expressing OAT4
IC50
|
||
|
TRANSPORTER -> INHIBITOR |
Based on in vitro studies, lesinurad is a weak inhibitor of OATP1B1, OCT1, OAT1, and OAT3.
WEAK
|
||
|
|
TARGET -> INHIBITOR |
IC50
|
||
|
TRANSPORTER -> SUBSTRATE |
Based on in vitro studies, lesinurad is a substrate of OAT1 and OAT3.
|
||
|
ENANTIOMER -> RACEMATE |
|
||
|
TRANSPORTER -> INHIBITOR |
Based on in vitro studies, lesinurad is a weak inhibitor of OATP1B1, OCT1, OAT1, and OAT3.
WEAK
|
||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
ENANTIOMER -> RACEMATE |
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
FECAL
|
||
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
FECAL
|
||
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
FECAL
|
||
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
URINE
|
||
|
METABOLITE -> PARENT |
PLASMA
|
||
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
URINE
|
||
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
URINE
|
||
|
METABOLITE -> PARENT |
PLASMA
|
||
|
METABOLITE -> PARENT |
AMOUNT EXCRETED
FECAL
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Biological Half-life | PHARMACOKINETIC |
|
|
|||
| Volume of Distribution | PHARMACOKINETIC |
|
INTRAVENOUS ADMINISTRATION |
|
||
| Tmax | PHARMACOKINETIC |
|
FED CONDITION |
|
||