Disease relevance of Loxoprofen

• Loxoprofen sodium and survival in older people with advanced non-small cell lung cancer [1].
• In this study it was shown that the most popular NSAID in Japan, loxoprofen sodium (LOX), inhibited in vivo growth of implanted Lewis lung carcinoma (LLC), whereas LOX did not affect the proliferation and viability of LLC cells in vitro [2].
• The phototoxicity study involving treatment with 10% solution of KP, its enantiomers (R-KP and S-KP), loxoprofen, and flurbiprofen revealed no phototoxic reactions [3].
• These results suggest that the chemical structure of the benzophenone chromophore in KP would be one of the important factors for induction of the photoallergy since both loxoprofen and flurbiprofen do not possess this structure and hence lack photoallergenic potential [3].
• Effectiveness of an anti-inflammatory drug, loxoprofen, for patients with nocturia [4].

High impact information on Loxoprofen

• The dihydrodiol dehydrogenases also showed lower Km values for haloperidol and loxoprofen than did carbonyl reductase [5].
• Results were compared with those for loxoprofen, a non-selective COX inhibitor [6].
• Comparison of pharmacokinetics of loxoprofen and its active metabolites after an intravenous, intramuscular, and oral administration of loxoprofen in rats: evidence for extrahepatic metabolism [7].
• After the intragastric, intravenous, or intramuscular administration, AUC for loxoprofen and the metabolites at a dose of 10 mg/kg were not statistically different for the different routes of administration [7].
• The objective of this study was to characterize the extent of the formation of the active (trans-alcohol form) and inactive (cis-alcohol) metabolites of loxoprofen and to compare the kinetics after its intragastric, intravenous, and intramuscular administrations in rats [7].

Chemical compound and disease context of Loxoprofen

• The cause of hyperkalemia was considered to be several doses of loxoprofen, a nonsteroidal anti-inflammatory drug (NSAID), prescribed for her lumbago by an orthopedic specialist, in addition to the long-term intake of imidapril, an angiotensin-converting enzyme inhibitor (ACEI), prescribed for her hypertension by a cardiologist [8].

Biological context of Loxoprofen

• Thus, approximately 22% of the loxoprofen may have been converted to the active metabolite in the liver and the extraheptic tissue(s) and the pharmacokinetics of the active metabolite was independent of the route of administration [7].
• Decreased oral bioavailability of loxoprofen at second administration in human subjects [9].
• The intramuscular ED50 values of loxoprofen sodium in carrageenan edema and vascular permeability tests are 1.15 and 7.8 mg/kg, respectively, which represent more potent than in case of oral application [10].

Anatomical context of Loxoprofen

• Purification and some properties of ketone reductase forming an active metabolite of sodium 2-[4-(2-oxocyclopentylmethyl)-phenyl]propionate dihydrate (loxoprofen sodium), a new anti-inflammatory agent, in rabbit liver cytosol [11].
• Ulcerogenicity and effect on inhibition of prostaglandin generation of indometacin farnesil, a prodrug of indomethacin, in rat gastric mucosa: comparison with indomethacin or loxoprofen [12].
• We made a diagnosis of CRPS type II, and the patient received stellate ganglion blockade, cervical epidural blockade, and administration of amitriptyline and loxoprofen [13].

Associations of Loxoprofen with other chemical compounds

• A method for simultaneously quantitating the enantiomers in the alpha-substituted propionic acid moiety of loxoprofen and its two monohydroxy metabolites, trans- and cis-alcohols, by column liquid chromatography was described [14].
• The drugs were given by twice daily oral administration for 10 days beginning 15 days after adjuvant injection, with celecoxib at 0.01-3 mg/kg/day and loxoprofen at 0.01-3 mg/kg/day [6].
• A controlled double blind study on the incidence of nonsteroidal antiinflammatory drug (NSAID) gastropathy was performed in 29 healthy volunteers administered diclofenac Na (10 subjects) or a prodrug (loxoprofen Na in 10 subjects and proglumetacin maleate in 9 subjects) [15].
• Loxoprofen sodium (sodium 2[4-(2-oxocyclopentylmethyl) phenyl] dehydrate; CAS #68767-14-6) is a nonsteroidal, inflammatory drug marketed only in Japan. A case report describes its association with an acute asthmatic death with features resembling those evoked by similar drugs [16].
• These findings suggest that loxoprofen retards the elimination of methotrexate, at least in part, by inhibiting hOAT1 and hOAT3 [17].

Gene context of Loxoprofen

• Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2 [18].
• These findings suggest that the COX inhibitory activity of loxoprofen sodium is attributable to its active metabolite, loxoprofen-SRS, and that loxoprofen-SRS shows non-selective inhibition for COX [19].
• Loxoprofen, its trans-alcohol and cis-alcohol metabolites were evaluated for selectivity of inhibition of COX-2 over COX-1 [18].
• Loxoprofen sodium suppresses mouse tumor growth by inhibiting vascular endothelial growth factor [2].
• The relationship between loxoprofen, cardiomyopathy and RPF remains unclear [20].

Analytical, diagnostic and therapeutic context of Loxoprofen

• Stereospecific analysis of loxoprofen in plasma by chiral column liquid chromatography with a circular dichroism-based detector [21].
• The effect of pretreatment (i.e., oral administration of loxoprofen for 3 consecutive days followed by a 7-day washout) on the pharmacokinetics and metabolism of the drug was studied in humans [22].
• The method allows the determination of the stereoisomers of loxoprofen in human plasma after the administration of therapeutic dose of the racemic drug, thus HPLC with CD detector is useful for the stereospecific determination of loxoprofen products in biological samples [21].
• The chiral separation of loxoprofen was achieved on a chiral column with UV and circular dichroism (CD) detection [21].
• Postoperative pain was evaluated at the clinic on the 1st, 7th and 14th postoperative day (POD) using a visual analogue scale (VAS), as was the number of loxoprofen tablets consumed, and the results were compared among the 3 groups with statistical significance of P<0.05 [23].

References