ZALTOPROFEN

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H14O3S
Molecular Weight	298.356
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C(O)=O)C1=CC=C2SC3=CC=CC=C3C(=O)CC2=C1

InChI

InChIKey=MUXFZBHBYYYLTH-UHFFFAOYSA-N

InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8,10H,9H2,1H3,(H,19,20)

HIDE SMILES / InChI

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/12065695
Curator's Comment: description was created based on several sources, including, http://www.ncbi.nlm.nih.gov/pubmed/16473424

Zaltoprofen is a non-steroidal anti-inflammatory drug approved in Japan for the treatment of lumbar pain, frozen shoulder, osteoarthritis, musculoskeletal pain, dental pain, post-operative pain. The main mechanism of action involves the inhibition of COX-2. Additional mechanism may be associated with the inhibitory effect of zaltoprofen on bradykinin-induced nociceptive responses that happens without blocking bradykinin receptors.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Prostaglandin G/H synthase 2 51 Target ID: P35354 Gene ID: 5743.0 Gene Symbol: PTGS2 Target Organism: Homo sapiens (Human) Sources: www.ncbi.nlm.nih.gov/pubmed/12065695	Inhibitor 8504		0.34 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Rheumatoid arthritis 320 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33385	Palliative	Approved 8583	SOLETON Approved Use It is usually used for anti-inflammation and analgesia in rheumatoid arthritis, osteoarthritis, low back pain, shoulder periarthritis, cervicobrachial syndrome as well as pain after operation, injuries or tooth removal.
Osteoarthritis 157 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33385	Palliative	Approved 8583	SOLETON Approved Use It is usually used for anti-inflammation and analgesia in rheumatoid arthritis, osteoarthritis, low back pain, shoulder periarthritis, cervicobrachial syndrome as well as pain after operation, injuries or tooth removal.
Low back pain 22 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33385	Palliative	Approved 8583	SOLETON Approved Use It is usually used for anti-inflammation and analgesia in rheumatoid arthritis, osteoarthritis, low back pain, shoulder periarthritis, cervicobrachial syndrome as well as pain after operation, injuries or tooth removal.
Shoulder periarthritis 1 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33385	Palliative	Approved 8583	SOLETON Approved Use It is usually used for anti-inflammation and analgesia in rheumatoid arthritis, osteoarthritis, low back pain, shoulder periarthritis, cervicobrachial syndrome as well as pain after operation, injuries or tooth removal.
Post-operational pain 1 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33385	Primary	Approved 8583	SOLETON Approved Use It is usually used for anti-inflammation and analgesia in rheumatoid arthritis, osteoarthritis, low back pain, shoulder periarthritis, cervicobrachial syndrome as well as pain after operation, injuries or tooth removal.

C_max

Value	Dose	Analyte	Population
5 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530213_1149029F1025_1_1F.pdf#page=16	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.37 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
12.32 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16.41 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.9 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	80 mg 3 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.85 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.46 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.71 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3.52 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

AUC

Value	Dose	Analyte	Population
12.77 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530213_1149029F1025_1_1F.pdf#page=16	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
15.57 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
41.61 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
53.41 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16.54 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	80 mg 3 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
19.66 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.35 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.14 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
20.09 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

T_1/2

Value	Dose	Analyte	Population
9.08 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530213_1149029F1025_1_1F.pdf#page=16	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.83 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.04 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.83 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23554672/	80 mg 3 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.95 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
4.87 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29092729/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530213_1149029F1025_1_1F.pdf#page=16	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:		ZALTOPROFEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
100 mg 3 times / day multiple, oral Highest studied dose Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: https://link.springer.com/article/10.1007%2FBF03259533	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://link.springer.com/article/10.1007%2FBF03259533	Sources: https://link.springer.com/article/10.1007%2FBF03259533
300 mg single, oral Highest studied dose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: https://link.springer.com/article/10.1007%2FBF03259533	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://link.springer.com/article/10.1007%2FBF03259533	Sources: https://link.springer.com/article/10.1007%2FBF03259533

PubMed

Title	Date	PubMed
Preemptive analgesia by zaltoprofen that inhibits bradykinin action and cyclooxygenase in a post-operative pain model.	2005-04	15740805

Patents

Sample Use Guides

In Vivo Use Guide

In general, for adults, take 1 tablet (80 mg of the active ingredient) at a time, 3 times a day. If the medicine is taken as needed, take 1 to 2 tablets (80 mg to 160 mg) at a time.

Route of Administration: Oral

In Vitro Use Guide

The proliferation of rheumatoid synovial cells was studied after incubation with zaltoprofen (300 uM). IC50 value for inhibition of cell viability was 135.2 uM. Zaltoprofen suppressedthecellproliferationin a concentration-dependent manner, with IC50 value of 48.9 uM.

Name

Type

Language

ZALTOPROFEN

Official Name

English

PEON

Preferred Name

English

SORETON

Brand Name

English

CN-100

Code

English

ZALTOPROFEN [MI]

Common Name

English

ZALTOPROFEN [MART.]

Common Name

English

ZALTOPROFEN [JAN]

Common Name

English

Zaltoprofen [WHO-DD]

Common Name

English

zaltoprofen [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C257