TRAPIDIL

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H15N5
Molecular Weight	205.2596
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCN(CC)C1=CC(C)=NC2=NC=NN12

InChI

InChIKey=GSNOZLZNQMLSKJ-UHFFFAOYSA-N

InChI=1S/C10H15N5/c1-4-14(5-2)9-6-8(3)13-10-11-7-12-15(9)10/h6-7H,4-5H2,1-3H3

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Description

Trapidil, a platelet-derived growth factor antagonist, was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease. Used to treat patients with ischemic coronary heart, liver, and kidney disease.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Thrombin-induced Thromboxane formation 1	Inhibitor 8,504	410.0 µM [IC50]
Platelet-derived growth factor receptor beta 56	Antagonist 2,849
C-C motif chemokine 2 2	Inhibitor 8,504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Coronary heart disease 43	Primary		Approved 8,583	Trapidil

C_max

Value	Dose	Analyte	Population
5.14 μg/mL	200 mg single, oral	TRAPIDIL plasma	Homo sapiens
5.01 μg/mL	200 mg 3 times / day steady-state, oral	TRAPIDIL plasma	Homo sapiens
1.5 μg/mL	200 mg single, oral	DESETHYLTRAPIDIL plasma	Homo sapiens
2.7 μg/mL	200 mg 3 times / day steady-state, oral	DESETHYLTRAPIDIL plasma	Homo sapiens
4.74 μg/mL	200 mg 3 times / day steady-state, oral	DESETHYLTRAPIDIL plasma	Homo sapiens
5.67 μg/mL	200 mg 3 times / day steady-state, oral	TRAPIDIL plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
20.5 μg × h/mL	200 mg single, oral	TRAPIDIL plasma	Homo sapiens
13.2 μg × h/mL	200 mg 3 times / day steady-state, oral	TRAPIDIL plasma	Homo sapiens
16.2 μg × h/mL	200 mg single, oral	DESETHYLTRAPIDIL plasma	Homo sapiens
16.9 μg × h/mL	200 mg 3 times / day steady-state, oral	DESETHYLTRAPIDIL plasma	Homo sapiens
34.5 μg × h/mL	200 mg 3 times / day steady-state, oral	DESETHYLTRAPIDIL plasma	Homo sapiens
20.8 μg × h/mL	200 mg 3 times / day steady-state, oral	TRAPIDIL plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
1.31 h	200 mg single, oral	TRAPIDIL plasma	Homo sapiens
1.14 h	200 mg 3 times / day steady-state, oral	TRAPIDIL plasma	Homo sapiens
2.41 h	200 mg 3 times / day steady-state, oral	TRAPIDIL plasma	Homo sapiens

Doses

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Dose	Population	Adverse events
200 mg 3 times / day multiple, oral Studied dose	unhealthy	Other AEs: Weakness...

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AEs

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AE	Significance	Dose	Population
Weakness	1 pt	200 mg 3 times / day multiple, oral Studied dose	unhealthy

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2,252 activator 150	inhibitor 2,438	inhibitor 2,507	inhibitor 2,217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2,153 CYP19A1 429 UMAT 30 CYP2C19 2,057 BSEP 550 BCRP 910 P-gp 1,741

Drug as perpetrator

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Target	Modality	Activity
BCRP 985	inhibitor 4,027	no
CYP19A1 430	inhibitor 4,027	no
CYP2C19 2,141	inhibitor 4,027	no
CYP2C9 2,497	inhibitor 4,027	no
CYP2D6 2,546	inhibitor 4,027	no

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Tox targets

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Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2,263	inhibitor 2,237

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PubMed

Title	Date	PubMed
No data available in table

Patents

Sample Use Guides

In Vivo Use Guide

Adults: Oral: 400-600 mg/day in divided doses

Route of Administration: Oral

In Vitro Use Guide

The addition of 100 to 400 ug/ml Trapidil significantly reduced cell proliferation induced by different growth factors (FCS, PDGF-BB, bFGF, EGF)

Show entries

Name

Type

Language

ROCORNAL

Preferred Name

English

TRAPIDIL

Official Name

English

TRAPIDIL [MI]

Common Name

English

Trapidil [WHO-DD]

Common Name

English

AR 12008

Code

English

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Classification Tree

Code System

Code

Other vasodilators used in cardiac diseases

WHO-VATC

QC01DX11

Enzyme Inhibitor

NCI_THESAURUS

C744

Other vasodilators used in cardiac diseases

WHO-ATC

C01DX11

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Code System

Code

Type

Description

MESH

D014192

PRIMARY

MERCK INDEX

m11005

PRIMARY

Merck Index

DRUG BANK

DB09283

PRIMARY

CAS

15421-84-8

PRIMARY

NCI_THESAURUS

C66615

PRIMARY

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ACTIVE MOIETY


					EYG5Y6355E

TRAPIDIL

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Tox targets

PubMed

Patents

Sample Use Guides

C_max

T_1/2

Drug as perpetrator