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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 value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
APROCITENTAN (is an active metabolite)

APROCITENTAN


ATC C02KN01

CARDIOVASCULAR
ANTIHYPERTENSIVE
PULMONARY ARTERIAL HYPERTENSION (PAH)
ENDOTHELIN RECEPTOR ANTAGONIST ET-1
PREVENTS THE BINDING OF ET-1 TO ITS RECEPTORS ETA AND ETB
METABOLITE 20 PERCENT AS POTENT AS THE PARENT DRUG IN VITRO

ORAL

Cmax 2.38 MICROMOLAR

Tmax 4.5 HOUR

VD 20 LITER

PPB 99 PERCENT

Cl 0.3 LITER / HOUR

HT 41 HOUR

SOLUBILITY INSOLUBLE IN WATER

ENDOTHELIN RECEPTOR ET-1

-

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank

2 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 value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
MACITENTAN (has an active metabolite)

MACITENTAN


ATC C02KX04
ATC C02KX54

CARDIOVASCULAR
ANTIHYPERTENSIVE
PULMONARY ARTERIAL HYPERTENSION (PAH)
ENDOTHELIN RECEPTOR ANTAGONIST ET-1
PREVENTS THE BINDING OF ET-1 TO ITS RECEPTORS ETA AND ETB

ORAL

VD 50 LITER

PPB 99 PERCENT

Cl 2.1 LITER / HOUR (EQN)

HT 16 HOUR

SOLUBILITY NOT SOLUBLE IN WATER

ENDOTHELIN RECEPTOR ET-1

Endothelin-1 receptor UNIPROT P25101 EDNRA -- Endothelin B receptor UNIPROT P24530 EDNRB

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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