Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. It works by enhancing mucosal defense, scavenging free radicals, and temporarily activating genes encoding cyclooxygenase-2. Rebamipide is used in a number of Asian countries including Japan (marketed as Mucosta), South Korea, China, and India (where it is marketed under the trade name Rebagen). It is not approved by the Food and Drug Administration for use in the United States. Studies have shown that rebamipide can fight the damaging effects of NSAIDs on the GIT mucosa.

Dipyrocetyl (2,3-diacetyloxybenzoic acid) is a drug used as an analgesics and antipyretics. Besides, was shown, that it may be useful in the treatment of acute lung injury (ALI) associated with acute respiratory distress syndrome (ARDS). Dipyrocetyl possesses the anticoagulation properties, which may contribute directly to improve tissue integrity as well as indirectly by the prevention of activation of pro-inflammatory cytokines. In addition, was made a suggestion, that the drug may function as an MMP inhibitor.

Tauroselcholic acid Se-75 (SeHCAT) is an analog of naturally occurring bile acid conjugate taurocholic acid. It contains a radioactive isotope of selenium, which decays with a half-life of 120 days by emitting gamma-radiation. Tauroselcholic acid is used in clinical tests to diagnose bile acid malabsorption. This is achieved by determining either the excretion of activity in feces or the retention of the activity in the body over a period of days. Tauroselcholic acid is useful in the assessment of ileal involvement in, Crohn's disease, in assessing reduction of ileal absorptive function following certain surgical interventions and in assisting in the classification of patients suffering from chronic diarrhea.

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. The dose is 100 mg twice daily, and should not be given to people with porphyria or breastfeeding mothers and is not recommended for children. Aceclofenac is a cytokine inhibitor. Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production of prostaglandins (chemicals in the body which cause pain, swelling and inflammation). Aceclofenac is the glycolic acid ester of diclofenac. The incidence of gastric ulcerogenicity of aceclofenac has been reported to be significantly lower than that of other frequently prescribed NSAIDs: for instance, 2-fold less than naproxen, 4-fold less than diclofenac, and 7-fold less than indomethacin. Aceclofenac is metabolized in human hepatocytes and human microsomes to form [2-(2',6'-dichloro-4'-hydroxy- phenylamino)phenyl] acetoxyacetic acid as the major metabolite, which is then further conjugated.

Lonazolac is a nonsteroidal anti-inflammatory drug. The mononuclear cell response to a synovial stimulus can be abolished by very low concentrations of lonazolac. This blockade can be completely released by the addition of prostaglandin E2. Lonazolac appears therefore as an agent able in addition to modulate the immune response. The release of histamine from human basophils was significantly decreased after preincubation of the cells with lonazolac Ca. Preincubation of human polymorphonuclear leukocytes with lonazolac Ca led to an inhibition of leukotriene generation induced by either the Ca ionophore or opsonized zymosan. Lonazolac Ca affected different enzymes of the platelet activating factor metabolism. After pre- and post-treatment with lonazolac-Ca, the numbers of animals with lung metastases and the score of metastases significantly decreased. Lonazolac-Ca is indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Acute irritation in osteoarthritis and spondylosis. Soft tissue rheumatism. Post-traumatic and postoperative pain and swelling states.

Fentiazac is a non-steroidal anti-inflammatory agent developed for the treatment of pain disorders. The drug was marketed under the name Norvedan, however, its current marketing status is unknown and supposed to be "discontinued".

Alfacalcidol (1-hydroxyvitamin D3) is a synthetic analog of vitamin D introduced clinically in the early 1970s. A prodrug for calcitriol (1,25-dihydroxyvitamin D3), it is one of the most potent and rapidly acting compounds currently used in the prevention and treatment of vitamin D deficiency states and hypocalcemia. The clinical benefit of alfacalcidol is related to the stimulation of calcium and phosphorus absorption, reversal of myopathy, promotion of mineralization in bone and the ability to reabsorb fully mineralized bone. Similar marketed vitamin D compounds include calcitriol and ergocalciferol. Alfacalcidol is indicated in conditions where there is a disturbance of calcium metabolism due to impaired 1-α hydroxylation such as when there is reduced renal function.

Naproxcinod is the first in the class of CINODs and has been evaluated in preclinical and clinical studies. It is metabolized to naproxen and has been shown to donate nitric oxide in vitro and in vivo. It stimulated the expression of heme oxygenase-mRNA in endothelial cells in vitro, a crucial mediator of antioxidant and tissue-protective actions. In preclinical studies, Naproxcinod has been shown to be analgesic and anti-inflammatory. Naproxcinod dose-dependently displayed a noticeable and significant anti-ischemic effect in reperfused ischemic rabbit hearts and did not exhibit the hypertensive effects of naproxen. In a proof of concept study in 31 healthy volunteers with GI tolerance as the primary endpoint, Naproxcinod caused fewer gastric erosions in both the stomach and the duodenum than naproxen, while 0.2 erosions were found with placebo. Naproxcinod caused less of an adverse effect in intestinal permeability than naproxen and was similar to placebo.

Tepoxalin is a nonsteroidal anti-inflammatory drug approved for veterinary use in the United States and many other countries. Marketed under the brand name Zubrin, Tepoxalin is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase.