FELBINAC

Details

Stereochemistry	ACHIRAL
Molecular Formula	C14H12O2
Molecular Weight	212.2439
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

OC(=O)CC1=CC=C(C=C1)C2=CC=CC=C2

InChI

InChIKey=QRZAKQDHEVVFRX-UHFFFAOYSA-N

InChI=1S/C14H12O2/c15-14(16)10-11-6-8-13(9-7-11)12-4-2-1-3-5-12/h1-9H,10H2,(H,15,16)

HIDE SMILES / InChI

Description

Felbinac, an active metabolite of fenbufen, is two times more potent than the parent drug. Felbinac is used topically to alleviate pain in the joints and muscles caused by injury or inflammation (Trixam 3% gel or foam). The drug is believed to exert its action by inhibiting COX-2 protein.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Prostaglandin G/H synthase 2 51	Inhibitor 8,504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain in the joints and muscles 2	Primary		Approved 8,583	TRAXAM

C_max

Value	Dose	Analyte	Population
1442 ng/mL	11.78 mg single, intravenous	FELBINAC plasma	Homo sapiens
2697 ng/mL	23.56 mg single, intravenous	FELBINAC plasma	Homo sapiens
5772 ng/mL	47.13 mg single, intravenous	FELBINAC plasma	Homo sapiens
11947 ng/mL	94.25 mg single, intravenous	FELBINAC plasma	Homo sapiens
22043 ng/mL	164.92 mg single, intravenous	FELBINAC plasma	Homo sapiens
34889 ng/mL	259.16 mg single, intravenous	FELBINAC plasma	Homo sapiens
44879 ng/mL	377 mg single, intravenous	FELBINAC plasma	Homo sapiens
5817 ng/mL	47.13 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
7530 ng/mL	47.13 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
11474 ng/mL	94.25 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
13568 ng/mL	94.25 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
21230 ng/mL	188.5 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
26473 ng/mL	188.5 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
5.6 mg × h/mL	11.78 mg single, intravenous	FELBINAC plasma	Homo sapiens
10.7 mg × h/mL	23.56 mg single, intravenous	FELBINAC plasma	Homo sapiens
22.2 mg × h/mL	47.13 mg single, intravenous	FELBINAC plasma	Homo sapiens
54 mg × h/mL	94.25 mg single, intravenous	FELBINAC plasma	Homo sapiens
96 mg × h/mL	164.92 mg single, intravenous	FELBINAC plasma	Homo sapiens
119 mg × h/mL	259.16 mg single, intravenous	FELBINAC plasma	Homo sapiens
182 mg × h/mL	377 mg single, intravenous	FELBINAC plasma	Homo sapiens
18 mg × h/mL	47.13 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
28 mg × h/mL	47.13 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
35 mg × h/mL	94.25 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
48 mg × h/mL	94.25 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
65 mg × h/mL	188.5 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
95 mg × h/mL	188.5 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
4.25 h	11.78 mg single, intravenous	FELBINAC plasma	Homo sapiens
5.18 h	23.56 mg single, intravenous	FELBINAC plasma	Homo sapiens
4.8 h	47.13 mg single, intravenous	FELBINAC plasma	Homo sapiens
6.24 h	94.25 mg single, intravenous	FELBINAC plasma	Homo sapiens
5.46 h	164.92 mg single, intravenous	FELBINAC plasma	Homo sapiens
5.46 h	259.16 mg single, intravenous	FELBINAC plasma	Homo sapiens
5.83 h	377 mg single, intravenous	FELBINAC plasma	Homo sapiens
6.12 h	47.13 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
6.59 h	47.13 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
5.79 h	94.25 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
7 h	94.25 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
5.71 h	188.5 mg 1 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens
7.38 h	188.5 mg 3 times / day multiple, intravenous	FELBINAC plasma	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
1 g 2 times / day multiple, topical Recommended	unhealthy, ADULT
1 g 4 times / day multiple, topical Recommended	unhealthy, ADULT	Disc. AE: Rash...

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AEs

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AE	Significance	Dose	Population
Rash	Disc. AE	1 g 4 times / day multiple, topical Recommended	unhealthy, ADULT

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PubMed

Show entries

Title	Date	PubMed
Analgesic effect of percutaneously absorbed non-steroidal anti-inflammatory drugs: an experimental study in a rat acute inflammation model.	2008 Jan 31	18234123
Stepwise two-color laser photolysis studies of alpha-cleavage in highly excited triplet states of alpha-acyl-4-phenylphenols.	2008 Jun	18528556
Mechanisms of drug release in citrate buffered HPMC matrices.	2009 Mar 31	19100822
Incorporating multiple interventions in meta-analysis: an evaluation of the mixed treatment comparison with the adjusted indirect comparison.	2009 Sep 21	19772573
Design, synthesis and evaluation of mutual prodrug of 4-biphenylacetic acid and quercetin tetramethyl ether (BPA-QTME) as gastrosparing NSAID.	2010 Jun	20227799

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Patents

Sample Use Guides

In Vivo Use Guide

The usual dose is about one inch or 2.5cm (which is about one gram) of gel rubbed into the affected area two to four times a day.

Route of Administration: Topical

In Vitro Use Guide

A 0.12 mM concentration of felbinac (BPAA) produces almost complete inhibition of arachidonate-induced aggregation of blood platelets.

Show entries

Name

Type

Language

DOLINAC

Preferred Name

English

FELBINAC

Official Name

English

4-Biphenylacetic acid

Systematic Name

English

(1,1'-BIPHENYL)-4-ACETIC ACID

Systematic Name

English

NSC-16284

Code

English

Showing 1 to 5 of 19 entries

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Classification Tree

Code System

Code

Antiinflammatory preparations, non-steroids for topical use

WHO-ATC

M02AA08

Analgesic and Antipyretic

NCI_THESAURUS

C257

Antiinflammatory preparations, non-steroids for topical use

WHO-VATC

QM02AA08

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Code System

Code

Type

Description

RXCUI

262307

PRIMARY

RxNorm

EVMPD

SUB07527MIG

PRIMARY

SMS_ID

100000092655

PRIMARY

DRUG BANK

DB07477

PRIMARY

WIKIPEDIA

FELBINAC

PRIMARY

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ACTIVE MOIETY


					94WNJ5U8L7

FELBINAC

SALT/SOLVATE (PARENT)


					HA8ZX3VG09

FELBINAC TROMETAMOL

SMILES

InChI

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Doses

AEs

PubMed

Patents

Sample Use Guides

C_max

T_1/2