Clocinizine is an antihistamine derivative of diphenylmethylpiperazine. Clocinizine is a competitive and reversible H1 receptor antagonist. The drug is marketed in Spain under tradename Senioral in combination with phenylpropanolamine for temporary relief of nasal congestion in colds, rhinitis, and sinusitis.

Mapinastine (E 4716) is a selective antagonist of histamine H1 receptors. In animal models, mapinastine exerts antiallergic and anti-asthmatic properties. It demonstrated a lack of central effects. Mapinastine development has been discontinued.

Tasquinimod is a drug, developed by Active Biotech Research and tested in phase III of clinical trials for the treatment of Castrate Resistant Prostate Cancer. The drug acts by targeting the tumor microenvironment with S100A9 being one of molecular targets.

Resatorvid (TAK-242) is a Toll-like receptor 4 (TLR4) antagonist that was designed for the treatment of severe sepsis because of its inhibitory effect on suppressing cytokine levels. This compound suppresses production of inflammatory mediators by inhibiting signal transduction through TLR4. It has also been shown that topical resatorvid, in a UV-induced skin tumorigenesis model, displays photochemopreventive activity, suppressing tumor area and multiplicity. Resatorvid has furthermore shown neuroprotective effects after traumatic brain injury (in a mouse model). Phase III studies evaluating the effects of resatorvid on sepsis have been completed. One such study was ended after it was determined that there was insufficient cytokine suppression in the first stage of the study.

Etoloxamine is an antihistamine.

Cis-isomer of loxanast (IG-10) or 1-methyl-4-isohexylcyclohexane carboxylic acid has been reported as an inhibitor of delayed hypersensitivity reaction in animal models. It inhibited macrophage chemotaxis.

Minocromil was studied as a histamine receptor antagonist for the treatment of asthma. However, further development of the drug was discontinued.

Cycliramine is a substituted piperidine derivative discovered by Schering Corp. The drug is claimed to have antihistamine, antispasmodic, antiacetylcholine and analgesic activity.

Altoqualine (458L) is a derivative of benzylisoquinoline, it inhibited kidney histidine decarboxylase and decreased the passive anaphylactic bronchospasm in guinea pigs. Altoqualine is an antihistamine and antiallergic agent.

Almurtide (CGP 11637) is a synthetic muramyl dipeptide (MDP) analogue with potential immunostimulating and antineoplastic activity. As a derivative of the mycobacterial cell wall component MDP, almurtide activates both monocytes and macrophages. This results in the secretion of cytokines and induces the recruitment and activation of other immune cells, which may result in indirect tumoricidal or cytostatic effects. CGP 11637 has been shown to prevent oncogenic viral infections in mice.