Absorption, Distribution and Excretion
Rapidly absorbed under fasting conditions, and peak plasma levels of 50 µg/mL are achieved within 2 hours after oral administration of 600 mg doses.
...RAPIDLY ABSORBED AFTER ORAL ADMIN; PEAK PLASMA LEVEL OCCURS WITHIN 90 MIN. ...ABSORPTION & AVAILABILITY ARE REDUCED WHEN...AGENT IS GIVEN WITH FOOD, BUT ARE NOT AFFECTED BY CONCOMITANT ADMIN OF AN ANTACID...
...FENOPROFEN...IS WELL ABSORBED FROM GI TRACT AS NA OR CA SALT, & IS RAPIDLY CLEARED BY KIDNEYS...
IN USUAL DOSES, FENOPROFEN...WELL ABSORBED (OVER 80%), RAPIDLY /ACHIEVES/... STEADY-STATE BLOOD LEVELS...HIGHLY PROTEIN BOUND (95-99%). ...BIOTRANSFORMED IN LIVER, & METABOLITES ARE EXCRETED IN URINE. ...T/2...2.5-3 HR...
FOLLOWING ABSORPTION, FENOPROFEN IS METAB & EXCRETED ALMOST EXCLUSIVELY IN URINE IN CONJUGATED FORM. ...IS HIGHLY BOUND TO PLASMA PROTEIN, & IT MAY DISPLACE OTHER PROTEIN-BOUND DRUGS FROM THEIR BINDING SITES, LEADING TO DRUG INTERACTIONS.
HUMAN PLASMA & URINE PHARMACOKINETICS AFTER ORAL & IV ADMIN OF FENOPROFEN.

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Metabolism / Metabolites
About 90% of a single oral dose is eliminated within 24 hours as fenoprofen glucuronide and 4'-hydroxyfenoprofen glucuronide, the major urinary metabolites of fenoprofen.
...FENOPROFEN...FOUND TO YIELD 2 URINARY GLUCURONIDES IN MAN. ONE...ACCOUNTING FOR ALMOST 1/2 THE DOSE, IS THE ACYL GLUCURONIDE... THE SECOND...ACCOUNTING FOR THE OTHER 1/2 OF THE DOSE, IS A GLUCURONIDE OF THE PHENOLIC DERIVATIVE /OF FENOPROFEN/...AN ACYL GLUCURONIDE WITH A FREE PHENOLIC GROUP.
...FENOPROFEN...FOUND TO YIELD SMALL AMT OF ACID-LABILE CONJUGATE BEING NEITHER A GLYCINE NOR A GLUTAMINE CONJUGATE...

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Biological Half-Life
Plasma half-life is approximately 3 hours.
...RAPIDLY ABSORBED AFTER ORAL ADMIN; PEAK PLASMA LEVEL OCCURS WITHIN 90 MIN. IT HAS PLASMA T/2 OF ABOUT 160 MIN, WHICH DOES NOT APPEAR...DOSE DEPENDENT. ABSORPTION & AVAILABILITY ARE REDUCED WHEN...AGENT IS GIVEN WITH FOOD, BUT ARE NOT AFFECTED BY CONCOMITANT ADMIN OF AN ANTACID...
...T/2...2.5-3 HR...

Hepatotoxicity
Prospective studies show that up to 15% of patients taking fenoprofen experience at least transient serum aminotransferase elevations. These elevations are generally transient, mild and asymptomatic, and may resolve even with drug continuation. Marked aminotransferase elevations (>3 fold elevated) occur in
Likelihood score: D (possible rare cause of clinically apparent liver injury).

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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Some reviewers consider fenoprofen to be acceptable during breastfeeding. Because there is little published experience with fenoprofen during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
99% to albumin.

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Interactions
WHEN FENOPROFEN WAS ADDED TO REGIMEN OF...PT WITH RHEUMATOID ARTHRITIS WHO WERE RECEIVING CORTICOSTEROID OR GOLD THERAPY, THERE WAS SOME EVIDENCE THAT DOSE OF STEROID COULD BE REDUCED & COMBINATION WITH GOLD WAS MORE EFFECTIVE.
FOOD DELAYS ABSORPTION...& REDUCES PEAK PLASMA CONCN (ABOUT 30%) & TOTAL ABSORPTION (ABOUT 20%), AS DOES COADMIN OF...ANTACIDS.
/PLASMA PROTEIN/ BINDING OF FENOPROFEN IS INHIBITED BY CONCOMITANT ADMIN OF INDOMETHACIN & PHENYLBUTAZONE... PLASMA T/2 OF FENOPROFEN IS DECR BY ASPIRIN...
FENPROFEN & PROPOXYPHENE ARE ADDITIVE WHEN GIVEN TOGETHER.

[1]. A universal methodology for reliable predicting the non-steroidal anti-inflammatory drug solubility in supercritical carbon dioxide. Sci Rep. 2022 Jan 20;12(1):1043.

[2]. Fenoprofen-An Old Drug Rediscovered as a Biased Allosteric Enhancer for Melanocortin Receptors. ACS Chem Neurosci. 2019 Mar 20;10(3):1066-1074.

Fenoprofen is a monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. It has a role as a non-steroidal anti-inflammatory drug, a cyclooxygenase 2 inhibitor, a cyclooxygenase 1 inhibitor, an antipyretic, a non-narcotic analgesic and a drug allergen. It is a conjugate acid of a fenoprofen(1-).
An anti-inflammatory analgesic and antipyretic highly bound to plasma proteins. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding.
Fenoprofen is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of fenoprofen is as a Cyclooxygenase Inhibitor.
Fenoprofen is a nonsteroidal antiinflammatory drug (NSAID) used in the treatment of acute pain and chronic arthritis. Fenoprofen has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury.
Fenoprofen is a propionic acid derivative with analgesic, non-steroidal antiinflammatory and antirheumatic properties. Fenoprofen inhibits both isozymes of cyclooxygenase; resulting in prostaglandin synthesis inhibition, thereby blocking the conversion of arachidonic acid to prostaglandins. In addition, fenoprofen activates both peroxisome proliferator activated receptors (PPAR)-alpha and -gamma, by which it may down-regulate leukotriene B4 production.
A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.
See also: Fenoprofen Calcium (has salt form); Fenoprofen Sodium (has salt form).

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Drug Indication
For relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis. Also for the relief of mild to moderate pain.
FDA Label

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Mechanism of Action
Fenoprofen's exact mode of action is unknown, but it is thought that prostaglandin synthetase inhibition is involved. Fenoprofen has been shown to inhibit prostaglandin synthetase isolated from bovine seminal vesicles.
LIKE ASPIRIN, FENOPROFEN INHIBITS PROSTAGLANDIN SYNTHETASE, BUT SIGNIFICANCE OF THIS ACTION IN RELATION TO CLINICAL EFFECTS PRODUCED IS NOT KNOWN.

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Therapeutic Uses
Cyclooxygenase Inhibitors; Anti-Inflammatory Agents, Non-Steroidal
...FENOPROFEN...MAY BE TRIED IN PT WHO CANNOT TOLERATE ASPIRIN BECAUSE OF GI DISTURBANCES. .../HAS/ ANTIINFLAMMATORY, ANALGESIC, & ANTIPYRETIC ACTIONS. ... EFFECTIVENESS IN RHEUMATOID ARTHRITIS APPEARS...COMPARABLE TO...ASPIRIN &...GI REACTIONS & AMT OF GI BLEEDING IS LESS...
...FENOPROFEN...FOUND TO BE EFFECTIVE IN TREATMENT OF RHEUMATOID ARTHRITIS AS JUDGED BY DECR IN PAIN, JOINT STIFFNESS, SWELLING, & TENDERNESS. ...IN PT WITH RHEUMATOID ARTHRITIS...EFFICACY OF DAILY DOSES OF 2.4 G FENOPROFEN WAS APPROX EQUIVALENT TO...3.9 G ASPIRIN.
WHEN FENOPROFEN WAS ADDED TO REGIMEN OF...PT WITH RHEUMATOID ARTHRITIS WHO WERE RECEIVING CORTICOSTEROID OR GOLD THERAPY, THERE WAS SOME EVIDENCE THAT DOSE OF STEROID COULD BE REDUCED & COMBINATION WITH GOLD WAS MORE EFFECTIVE.
For more Therapeutic Uses (Complete) data for FENOPROFEN (7 total), please visit the HSDB record page.

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Drug Warnings
...CLINICAL EXPERIENCE WITH...NEWER AGENTS /INCL FENOPROFEN/ IS NOT YET SUFFICIENT TO DETERMINE THEIR COMPARATIVE EFFICACIES & ULTIMATE ROLE IN THERAPY OF RHEUMATIC DISEASES.
.../FENOPROFEN/ SHOULD NOT BE USED IN PT WITH BLEEDING DISORDERS & SHOULD BE USED WITH CAUTION IN PT RECEIVING ANTICOAGULANTS.
.../FENOPROFEN/ IS HIGHLY BOUND TO PLASMA PROTEIN, & IT MAY DISPLACE OTHER PROTEIN-BOUND DRUGS FROM THEIR BINDING SITES, LEADING TO DRUG INTERACTIONS.

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Pharmacodynamics
Fenoprofen is a propionic acid derivative with analgesic, antiinflammatory and antipyretic properties. Fenoprofen inhibits prostaglandin synthesis by decreasing the enzyme needed for biosynthesis. In patients with rheumatoid arthritis, the anti-inflammatory action of fenoprofen has been evidenced by relief of pain, increase in grip strength, and reductions in joint swelling, duration of morning stiffness, and disease activity (as assessed by both the investigator and the patient). In patients with osteoarthritis, the anti-inflammatory and analgesic effects of fenoprofen have been demonstrated by reduction in tenderness as a response to pressure and reductions in night pain, stiffness, swelling, and overall disease activity (as assessed by both the patient and the investigator). These effects have also been demonstrated by relief of pain with motion and at rest and increased range of motion in involved joints. In patients with rheumatoid arthritis and osteoarthritis, clinical studies have shown fenoprofen to be comparable to aspirin in controlling the aforementioned measures of disease activity, but mild gastrointestinal reactions (nausea, dyspepsia) and tinnitus occurred less frequently in patients treated with fenoprofen than in aspirin-treated patients. It is not known whether fenoprofen causes less peptic ulceration than does aspirin. In patients with pain, the analgesic action of fenoprofen has produced a reduction in pain intensity, an increase in pain relief, improvement in total analgesia scores, and a sustained analgesic effect.

C15H14O3

242.2699

242.094

29679-58-1

Fenoprofen Calcium hydrate;71720-56-4;Fenoprofen Calcium;34597-40-5;Fenoprofen-13C6 sodium hydrate

3342

Colorless to light yellow viscous liquid

1.2±0.1 g/cm3

381.3±25.0 °C at 760 mmHg

168-171

141.7±16.7 °C

0.0±0.9 mmHg at 25°C

1.583

3.84

1

3

4

18

271

0

O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])(C(=O)O[H])C([H])([H])[H]

RDJGLLICXDHJDY-UHFFFAOYSA-N

InChI=1S/C15H14O3/c1-11(15(16)17)12-6-5-9-14(10-12)18-13-7-3-2-4-8-13/h2-11H,1H3,(H,16,17)

2-(3-phenoxyphenyl)propanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~412.76 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)