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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
M RIPRETINIB (is an active metabolite)

RIPRETINIB


ATC L01EX19

ANTINEOPLASTIC
KIT PROTO-ONCOGENE RECEPTOR TYROSINE KINASE INHIBITOR
PLATELET DERIVED GROWTH FACTOR RECEPTOR A (PDGFRA) INHIBITOR
TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR (GIST)
INHIBITS PDGFRB, TIE2, VEGFR2, AND BRAF

-

Cmax 1.62 MICROMOLAR

Tmax 15.6 HOUR

VD 507 LITER

PPB 99.8 PERCENT

Cl 17.5 LITER / HOUR

HT 17.8 HOUR

PROTO-ONCOGENE RECEPTOR TYROSINE KINASE (KIT)

Mast,stem cell growth factor receptor Kit UNIPROT P10721 KIT -- Platelet-derived growth factor receptor alpha UNIPROT P16234 PDGFRA

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
RIPRETINIB (has an active metabolite)

RIPRETINIB


ATC L01EX19

ANTINEOPLASTIC
KIT PROTO-ONCOGENE RECEPTOR TYROSINE KINASE INHIBITOR
PLATELET DERIVED GROWTH FACTOR RECEPTOR A (PDGFRA) INHIBITOR
TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR (GIST)
INHIBITS PDGFRB, TIE2, VEGFR2, AND BRAF

ORAL

Cmax 1.49 MICROMOLAR

Tmax 4 HOUR

VD 307 LITER

PPB 99.8 PERCENT

Cl 15.3 LITER / HOUR

HT 14.8 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN WATER

PROTO-ONCOGENE RECEPTOR TYROSINE KINASE (KIT)

Mast,stem cell growth factor receptor Kit UNIPROT P10721 KIT -- Platelet-derived growth factor receptor alpha UNIPROT P16234 PDGFRA

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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