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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that the equation t1/2 = VD / Cl * 0.693 was usedPrimary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
LESINURAD DISCONTINUED

LESINURAD


ATC M04AB05

MUSCULO-SKELETAL
URAT1 INHIBITOR (KI = 7.3 MICROMOLAR)
TREATMENT OF HYPERURICEMIA ASSOCIATED WITH GOUT
REDUCES SERUM URIC ACID LEVELS BY INHIBITING THE FUNCTION OF TRANSPORTER PROTEINS INVOLVED IN URIC ACID REABSORPTION IN THE KIDNEY

ORAL

Cmax 14.8 MICROMOLAR

Tmax 2.5 HOUR

F 100 PERCENT

VD 20 LITER

PPB 98 PERCENT

Cl 6 LITER / HOUR

HT 5 HOUR

SOLUBILITY SOLUBLE IN WATER

URIC ACID TRANSPORTER 1 (URAT1)
ORGANIC ANION TRANSPORTER 4 (OAT4)

PDB 9B1H (HUMAN URATE TRANSPORTER 1 URAT1 IN COMPLEX WITH LESINURAD)

LIGAND CODE = A1AIL (link to the list of PDB complexes)

Download experimental 3D coordinates of A1AIL with added hydrogens

Solute carrier family 22 member 12 UNIPROT Q96S37 SLC22A12

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

VigiAccess
SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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