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| 1 | INN | Class | Route (list) | PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693) | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| M TICAGRELOR (is an active metabolite)
| TICAGRELOR | BLOOD | - | Cmax 0.55 MICROMOLAR (200 MILLIGRAM) DOI:10.1124/DMD.110.032250 F 36 PERCENT VD 88 LITER PPB 99 PERCENT Cl 6.7 LITER / HOUR (EQN) HT 9 HOUR | P2Y12 ADP-RECEPTOR | PURINERGIC RECEPTOR P2Y12 NEGATIVE ALLOSTERIC MODULATOR CHEMBL2001 PURINERGIC RECEPTOR P2Y12 Q9H244 P2Y PURINOCEPTOR 12 HOMO SAPIENS MEMBRANE RECEPTOR 7TM1 SMALLMOL NUCLEOTIDE-LIKE RECEPTOR PURINE RECEPTOR | ANSM (in French) | |||
| 2 | INN | Class | Route (list) | PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693) | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| TICAGRELOR (has an active metabolite)
| TICAGRELOR | BLOOD | ORAL | Cmax 1.76 MICROMOLAR (200 MILLIGRAM) DOI:10.1124/DMD.110.032250 F 36 PERCENT VD 88 LITER PPB 99 PERCENT Cl 8.7 LITER / HOUR (EQN) HT 7 HOUR SOLUBILITY AQUEOUS SOLUBILITY OF APPROXIMATELY 10 MICROGRAM / MILLILITER AT ROOM TEMPERATURE | P2Y12 ADP-RECEPTOR PDB 5ALC (TICAGRELOR ANTIDOTE CANDIDATE FAB 72 IN COMPLEX WITH TICAGRELOR) LIGAND CODE = TIQ (link to the list of PDB complexes) Download experimental 3D coordinates of TIQ with added hydrogens | PURINERGIC RECEPTOR P2Y12 NEGATIVE ALLOSTERIC MODULATOR CHEMBL2001 PURINERGIC RECEPTOR P2Y12 Q9H244 P2Y PURINOCEPTOR 12 HOMO SAPIENS MEMBRANE RECEPTOR 7TM1 SMALLMOL NUCLEOTIDE-LIKE RECEPTOR PURINE RECEPTOR | ANSM (in French) | |||
