Page last updated: 2024-12-11

apricoxib

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

apricoxib: a COX-2 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9820073
CHEMBL ID1835207
SCHEMBL ID346028
MeSH IDM0503331

Synonyms (37)

Synonym
apricoxib
197904-84-0
apricoxib (usan/inn)
D08657
5x5hb3vz3z ,
r 109339
apricoxib [usan:inn]
4-(2-(4-ethoxyphenyl)-4-methyl-1h-pyrrol-1-yl)benzenesulfonamide
cs 706
unii-5x5hb3vz3z
cs706 cpd
2-(4-ethoxyphenyl)-4-methyl 1-(4-sulfamoylphenyl)-1h-pyrrole
benzenesulfonamide, 4-(2-(4-ethoxyphenyl)-4-methyl-1h-pyrrol-1-yl)-
tg 01
tg01
CHEMBL1835207
r-109339
tg-01
cs-706
kymena
capoxigem
tp-1001
tp-2001
apricoxib [usan]
apricoxib [who-dd]
4-[2-(4-ethoxyphenyl)-4-methyl-1h-pyrrol-1-yl]benzenesulfonamide
apricoxib [inn]
SCHEMBL346028
JTMITOKKUMVWRT-UHFFFAOYSA-N
2-(4-ethoxyphenyl)-4-methyl-1-(4-sulfamoylphenyl)pyrrole
DTXSID60173502
DB12378
4-[2-(4-ethoxyphenyl)-4-methylpyrrol-1-yl]benzenesulfonamide
Q18209480
cs 706; r 109339; tg 01
4-methyl-2-(4-ethoxyphenyl)-1-(4-sulfamoylphenyl)pyrrole
cs701

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"A predictive population pharmacokinetic model was developed for a novel cyclooxygenase-2 (COX-2) inhibitor CS-706, using data from 130 subjects in 3 phase 1 trials after single or multiple doses of CS-706 (2- to 800-mg doses daily, up to 14 days) and validated using sparse data from a separate study."( Development of a predictive pharmacokinetic model for a novel cyclooxygenase-2 inhibitor.
Gao, Y; Kastrissios, H; Kawabata, K; Moberly, J; Rohatagi, S; Salazar, D; Takahashi, M; Truitt, K; Wada, R, 2006
)
0.33
"The objectives of these analyses were to (1) develop a population pharmacokinetic/pharmacodynamic model for a novel COX-2 inhibitor (CS-706) using data from primarily Caucasian subjects, (2) predict responses in subpopulations of interest (including Japanese subjects), and (3) correlate pharmacodynamic parameters to safety outcomes."( Predictive population pharmacokinetic/pharmacodynamic model for a novel COX-2 inhibitor.
Gao, Y; Kastrissios, H; Moberly, J; Rohatagi, S; Salazar, D; Takahashi, M; Truitt, K; Wada, R; Xu, J; Yoshihara, K; Zhang, N, 2007
)
0.34

Compound-Compound Interactions

Apricoxib, a novel once-daily selective cyclooxygenase-2 inhibitor, was investigated in combination with erlotinib for recurrent stage IIIB/IV nonsmall cell lung cancer.

ExcerptReferenceRelevance
" Administration of 30 mg/kg CS-706 from Day 7 combined with a single intravenous treatment of 10 mg/kg cisplatin on Day 7 completely regressed the tumors in all tumor-bearing mice examined, whereas only in 1 of 10 mice tumor was regressed with cisplatin treatment."( CS-706, a novel cyclooxygenase-2 selective inhibitor, prolonged the survival of tumor-bearing mice when treated alone or in combination with anti-tumor chemotherapeutic agents.
Fujiwara, K; Hanai, M; Inoue, S; Ishida, S; Kimura, T; Kurakata, S; Senzaki, M; Yada, A, 2008
)
0.35
"Apricoxib, a novel once-daily selective cyclooxygenase-2 inhibitor, was investigated in combination with erlotinib for recurrent stage IIIB/IV nonsmall cell lung cancer to determine the maximum tolerated dose, dose-limiting toxicity, and recommended phase II dose (RP2D) based on changes in urinary prostaglandin E₂ metabolite (PGE-M)."( Biomarker-based phase I dose-escalation, pharmacokinetic, and pharmacodynamic study of oral apricoxib in combination with erlotinib in advanced nonsmall cell lung cancer.
Chen, LC; Gitlitz, B; Jezior, D; Milne, G; Patel, R; Reckamp, K; Syto, M; Zaknoen, S, 2011
)
2.03
"Patients received escalating doses of apricoxib (100, 200, and 400 mg/day) in combination with erlotinib 150 mg/day until disease progression or unacceptable toxicity."( Biomarker-based phase I dose-escalation, pharmacokinetic, and pharmacodynamic study of oral apricoxib in combination with erlotinib in advanced nonsmall cell lung cancer.
Chen, LC; Gitlitz, B; Jezior, D; Milne, G; Patel, R; Reckamp, K; Syto, M; Zaknoen, S, 2011
)
0.86
" This randomized phase 2 trial evaluated apricoxib, a novel COX-2 inhibitor, in combination with erlotinib in biomarker-selected patients."( A randomized, placebo-controlled, multicenter, biomarker-selected, phase 2 study of apricoxib in combination with erlotinib in patients with advanced non-small-cell lung cancer.
Bernstein, E; Burrows, F; Gitlitz, BJ; Milne, G; Otterson, GA; Santos, ES; Syto, M; Zaknoen, S, 2014
)
0.89
" Docetaxel 75 mg/m(2) or pemetrexed 500 mg/m(2) once every 21 days per the investigator was administered with apricoxib or placebo 400 mg once per day."( Randomized, double-blind, placebo-controlled, multicenter phase II study of the efficacy and safety of apricoxib in combination with either docetaxel or pemetrexed in patients with biomarker-selected non-small-cell lung cancer.
de Mayolo, JA; Edelman, MJ; Evans, TL; Feliciano, J; Fidler, MJ; Keresztes, R; Medeiros, M; Otterson, G; Rogers, JS; Sanborn, RE; Schneider, BJ; Sequist, LV; Tan, MT; Yang, Y; Zaknoen, SL, 2015
)
0.84

Bioavailability

ExcerptReferenceRelevance
" Bioavailability increased by 42% after nighttime doses and decreased saturably with increasing dose (50% reduction at 221 mg)."( Development of a predictive pharmacokinetic model for a novel cyclooxygenase-2 inhibitor.
Gao, Y; Kastrissios, H; Kawabata, K; Moberly, J; Rohatagi, S; Salazar, D; Takahashi, M; Truitt, K; Wada, R, 2006
)
0.33

Dosage Studied

ExcerptRelevanceReference
" In contrast, naproxen nearly completely inhibited COX-1 over the dosing interval."( A randomized, double-blind, one-week study comparing effects of a novel COX-2 inhibitor and naproxen on the gastric mucosa.
Breese, T; Dale, JC; Harris, SI; Lawson, J; McLaughlin, P; Moberly, JB; Riff, DS; Truitt, KE; Wan, Y; Xu, J, 2007
)
0.34
" The onset of analgesia (PID >or= 1) for all CS-706 doses occurred within 1 hour after dosing (P<0."( A randomized, double-blind, celecoxib- and placebo-controlled study of the effectiveness of CS-706 in acute postoperative dental pain.
Bandy, DP; Daniels, SE; Desjardins, PJ; Lawson, JE; Link, AJ; Moberly, JB; Truitt, KE; Xu, J, 2007
)
0.34
"The set of models developed permitted compilation of multiple dose-response curves for dose selection of CS-706 in Westerners and facilitated scaling of doses to a Japanese population."( Pain relief model for a COX-2 inhibitor in patients with postoperative dental pain.
Kastrissios, H; Moberly, JB; Rohatagi, S; Salazar, DE; Sasahara, K; Truitt, K; Wada, R, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID623148Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells assessed as PGE2 level per 1000 cells at 10 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 3.15 +/- 0.19 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623146Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells assessed as PGE2 level per 1000 cells at 0.1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 3.15 +/- 0.19 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623151Inhibition of sodium arachidonate-induced PGE2 production in human SUM190 cells assessed as PGE2 level per 1000 cells at 10 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 6.43 +/- 1.87 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623150Inhibition of sodium arachidonate-induced PGE2 production in human SUM190 cells assessed as PGE2 level per 1000 cells at 1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 6.43 +/- 1.87 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623154Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells at 10 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623153Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells at 1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623149Inhibition of sodium arachidonate-induced PGE2 production in human SUM190 cells assessed as PGE2 level per 1000 cells at 0.1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 6.43 +/- 1.87 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623147Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells assessed as PGE2 level per 1000 cells at 1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 3.15 +/- 0.19 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID623152Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells at 100 nM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's11 (57.89)29.6817
2010's8 (42.11)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.77

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.77 (24.57)
Research Supply Index3.30 (2.92)
Research Growth Index4.44 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (36.84%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (57.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]