Nemazoline (A-57219) is a nasal decongestant. It has alpha 1-agonist/alpha 2-antagonist activity and was more effective and long-acting than oxymetazoline on canine nasal mucosa, in-vitro and in-vivo. Upon intranasal administration to dogs, the compound was devoid of systemic effects up to a concentration 1000 times that needed for local decongestant effect (1.65 micrograms, atomized from a 1 microgram mL-1 solution) suggesting limited mucosal absorption. After nasal administration to rats for 15 days at a concentration 1000 times greater than that required for nasal decongestion, no mucosal tissue toxicity or systemic effects were seen.

ISATORIBINE, a guanosine analog, is an immunopotentiating agent. It is a selective agonist of toll‐like receptor 7, a pattern-recognition receptor that activates the innate immune response.

Manitimus (FK778) is a synthetic malononitrilamide (MNA) that has been demonstrated to have both both immunosuppressive and anti-proliferative activities. The MNAs inhibit both T-cell and B-cell function by blocking de novo pyrimidine synthesis, through blockade of the pivotal mitochondrial enzyme dihyroorotic acid dehydrogenase, and the inhibition of tyrosine kinase activity. It directly reduced endothelial adhesion molecule up-regulation, inhibited lymphocyte activation, and attenuated lymphocyte-endothelium interactions, critical early steps in graft rejection. Manitimus has been demonstrated to prevent acute allograft rejection in multiple experimental transplant models in rodents, dogs and primates and to be effective in the rat model of chronic renal allograft rejection. It was in clinical studies for the treatment of transplant rejection. Manitimus development has been discontinued.

Ristianol (Ristianol phosphate) is a bioactive chemical that is registered as an anti-inflammatory agent and immunoregulator (in Europe), but no further information is available.

Forfenimex (also known as forphenicinol), a low molecular weight immunomodifier was studied as an antineoplastic agent. Preclinical experiments in vitro have shown that forfenimex enhanced the antitumor effects of cyclophosphamide in a model of squamous cell carcinoma. Experiments on rodents have revealed that this compound possessed protective effect against P. aeruginosa infection. This influence achieved due to macrophage activation followed by the enhancement of the bactericidal activity of polymorphonuclear cells (PMN).

Procodazole is a non-specific active immunoprotective agent against viral and bacterial infections

Fuprazole was developed as a bronchodilator that has never been marketed. Information about the current use of this compound is not available.

Aplaviroc (GW873140) is a small-molecule noncompetitive allosteric CCR5 antagonist or HIV entry inhibitor (EI) that binds specifically to human CCR5 and exhibits potent anti-HIV activity in vitro in the nanomolar or subnanomolar range. Aplaviroc has exhibited potent in vivo antiviral activity (1.66 log decrease in viral load at nadir) following 10 days of monotherapy. In vitro studies of antiviral activity demonstrate that aplaviroc is active against HIV isolates from a variety of clades as well as those resistant to current HIV therapies targeting RT, PR, and gp41. However, GlaxoSmithKline has decided to terminate Phase III trials of aplaviroc after encountering additional cases of liver damage in patients taking the drug.

Tabilautide (also known as RP 56142) is a tripeptide derivative patented by Rhone-Poulenc Industries S. A. as an immune adjuvant. In preclinical studies, Tabilautide displays potent protective activities against bacterial infections such as K. pneumoniae, L. monocytogenes or S. Typhimurium. Besides that Tabilautide shows antimetastatic activity and induces macrophage activation and enhanced cytotoxicity of natural killer cells in spleen, blood, and liver. These activities correlate with prophylactic and therapeutic effects of Tabilautide on artificial liver metastases of histiocytosarcoma.

Tazofelone (also known as LY 213829), a suppressant, is a cyclo-oxygenase 2 inhibitor that was studied for the treatment of Crohn's disease, irritable bowel syndrome and ulcerative colitis. However, Eli Lilly discontinued the further development of this compound.